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Btkinhibitor 1 is a pyrazolo[3,4-d]pyrimidine derivative as a Btk kinase inhibitor. Synonyms: Btkinhibitor 1. Grades: >98%. CAS No. 1412418-47-3. Molecular formula: C22H22N6O. Mole weight: 386.45.
BTKinhibitor 1 (Compound 27)
BTKinhibitor 1 is an inhibitor of BTK with IC50 of 0.11 nM for Btk and inhibits B cell activation in hWB with IC50 of 2 nM. Synonyms: DC20199; Compound 27. Grades: ≥98%. CAS No. 2230724-66-8. Molecular formula: C24H23FN8O2. Mole weight: 474.49.
Btkinhibitor 1 R enantiomer
Btkinhibitor 1 R enantiomer is a pyrazolo[3,4-d]pyrimidine derivative as a Btk kinase inhibitor. Synonyms: 3-(4-phenoxyphenyl)-1-[(3R)-3-piperidinyl]-1H-pyrazolo[3,4-d]pyrimidin-4-amine; (R)-3-(4-Phenoxyphenyl)-1-(piperidin-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine; 1H-Pyrazolo[3,4-d]pyrimidin-4-amine, 3-(4-phenoxyphenyl)-1-(3R)-3-piperidinyl-. Grades: ≥98% by HPLC. CAS No. 1022150-12-4. Molecular formula: C22H22N6O. Mole weight: 386.45.
Btkinhibitor 1 R enantiomer hydrochloride
Btkinhibitor 1R enantiomer Hcl is a pyrazolo[3,4-d]pyrimidine derivative as a Btkkinase inhibitor. Synonyms: Btkinhibitor 1 R enantiomer hydrochloride. Grades: >98%. CAS No. 1553977-42-6. Molecular formula: C22H23ClN6O. Mole weight: 422.91.
BTKinhibitor 2
Bruton's tyrosine kinase (BTK), also known as tyrosine-protein kinase BTK, is an enzyme that in humans is encoded by the BTK gene. BTK is a kinase that plays a crucial role in B-cell development. Btkinhibitor 2 is a BTKinhibitor. Grades: ≥98%. CAS No. 1558036-85-3. Molecular formula: C24H25N5O3. Mole weight: 431.49.
1-Boc-pyrazole-4-boronic Acid Pinacol Ester
1-Boc-pyrazole-4-boronic Acid Pinacol Ester is used as a reagent in the synthesis of several inhibitors including thieno[3,2-c]pyridin-4-amines which are a novel series of Brutons tyrosine kinase (BTK) inhibitors which can be used in drug design. Group: Biochemicals. Grades: Highly Purified. CAS No. 552846-17-0. Pack Sizes: 1g, 2.5g. Molecular Formula: C14H23BN2O4, Molecular Weight: 294.149999999999. US Biological Life Sciences.
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2-Aminomethyl-3-chloropyrazine
2-Aminomethyl-3-chloropyrazine is used in the discovery of 8-Amino-imidazo[1,5-a]pyrazine-based Brutons tyrosine kinase (BTK) inhibitors for treating rheumatoid arthritis. Group: Biochemicals. Grades: Highly Purified. CAS No. 771581-15-8. Pack Sizes: 50mg, 250mg. Molecular Formula: C5H6ClN3, Molecular Weight: 143.57. US Biological Life Sciences.
(2E)-4-(1-Pyrrolidinyl)-2-butenoic Acid is used in the preparation of pyridine and pyrimidine compounds as BTKinhibitors. Group: Biochemicals. Grades: Highly Purified. CAS No. 848133-09-5. Pack Sizes: 100mg, 1g. Molecular Formula: C8H14ClNO2, Molecular Weight: 191.66. US Biological Life Sciences.
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3-Chloro-4-nitrophenol
3-Chloro-4-nitrophenol was used as a reactant in the synthetic preparation of highly potent BTK and JAK3 dual inhibitors and it may also have antifungal activity. Group: Biochemicals. Grades: Highly Purified. CAS No. 491-11-2. Pack Sizes: 250mg, 500mg. Molecular Formula: C6H4ClNO3, Molecular Weight: 173.55. US Biological Life Sciences.
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Acalabrutinib
Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTKinhibitor. Acalabrutinib binds covalently to Cys481 in the ATP-binding pocket of BTK. Acalabrutinib demonstrates potent on-target effects and efficacy in mouse models of chronic lymphocytic leukemia (CLL) [1] [2]. Acalabrutinib is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. Uses: Scientific research. Group: Signaling pathways. Alternative Names: ACP-196. CAS No. 1420477-60-6. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg; 200 mg. Product ID: HY-17600.
Acalabrutinib
Acalabrutinib, also known as ACP-196, is an orally available inhibitor of Bruton's tyrosine kinase (BTK) with potential antineoplastic activity. It inhibits the activity of BTK and prevents the activation of the B-cell antigen receptor (BCR) signaling pathway. Synonyms: ACP-196; ACP196; ACP 196; Acalabrutinib; 4-[8-amino-3-[(2S)-1-but-2-ynoylpyrrolidin-2-yl]imidazo[1,5-a]pyrazin-1-yl]-N-pyridin-2-ylbenzamide. Grades: >98%. CAS No. 1420477-60-6. Molecular formula: C26H23N7O2. Mole weight: 465.52.
Acalabrutinib-[d4]
Acalabrutinib-[d4] is a labelled version of Acalabrutinib. Acalabrutinib, also known as ACP-196, is an orally available inhibitor of Bruton's tyrosine kinase (BTK) with potential antineoplastic activity. It inhibits the activity of BTK and prevents the activation of the B-cell antigen receptor (BCR) signaling pathway. Synonyms: (S)-4-(8-amino-3-(1-(but-2-ynoyl)pyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1-yl)-N-(pyridin-2-yl-d4)benzamide. Grades: > 98%. Molecular formula: C26H19D4N7O2. Mole weight: 469.53.
A cell-permeable furopyrimidine that acts as a potent, ATP-binding site-targeting, Ack1-selective inhibitor (IC50 = 22nM) and effectively prevents receptor-mediated Ack1 activation (by >90% in MEF & LAPC4 cultures; 16h 800nM), while exhibiting much reduced potency against Lyn, Lck, Abl1 and BTK (IC50 ≥346.7nM) and no inhibitory activity toward 25 other kinases. Shown to completely inhibit EGF-induced, but not androgen DHT- (dihydrotestosterone) stimulated, AR transcription activity in serum- and androgen-deprived prostate cancer LAPC4 cutlures. Effectively inhibits androgen-independent LNCaP prostate cancer growth both in vitro (by 60%; 72h 8uM) and in castrated mice in vivo (4mg/kg/96h injections on day 7/11/15/19/23/27 post tumor transplant). Group: Biochemicals. Grades: Highly Purified. CAS No. 873305-35-2. Pack Sizes: 10mg. US Biological Life Sciences.
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ACP-5862
ACP-5862 is a metabolite of Acalabrutinib, a second-generation BTKinhibitor used as a medication indicated for the treatment of non-Hodgkin lymphoma known as mantle cell lymphoma. Synonyms: ACP 5862; ACP5862. CAS No. 2230757-47-6. Molecular formula: C26H23N7O3. Mole weight: 481.52.
ARQ 531
ARQ-531 is a potent and orally active BTKinhibitor with potential antineoplastic activity. ARQ 531 is a reversible non-covalent inhibitor of Bruton's Tyrosine Kinase (BTK), with IC50s of 0.85 nM and 0.39 nM for WT-BTK and C481S-BTK, respectively. It also has a distinct kinase selectivity profile with strong inhibitory activity against several key oncogenic drivers from TEC, Trk and Src family kinases. In GCB-DLBCL cell lines (SUDHL-4 and DOHH-2), ARQ 531 potently suppressed expression of anti-apoptotic c-Myc and BCL6 oncoproteins in a dose-dependent fashion, and concomitantly induced apoptotic cleavage of PARP protein. Synonyms: ARQ-531. Grades: ≥98%. CAS No. 2095393-15-8. Molecular formula: C25H23ClN4O4. Mole weight: 478.93.
Aurora Kinase Inhibitor III
Aurora kinase inhibitor III is a potent ATP-competitive aurora related kinase inhibitor with IC50 of 42 nM. Aurora kinase inhibitor III is a cell-permeable, 2,4-dianilinopyrimidine compound which has been used to study a variety of tumor types. It is selective for Aurora A over BMX, BTK, IGF-1R, c-Src, TRKB, SYK, and EGFR (IC50s = 386, 3,550, 591, 1,980, 2,510, 887, and >10,000 nM, respectively). Aurora kinase protein levels are elevated in c-myc-driven B-cell lymphomas in both mice and humans. Study of the inhibition of Aurora kinase proteins could lead to potential treatments for malignancies. Synonyms: Aurora Kinase Inhibitor III; AKI-7169; AKI 7169; AKI7169. Grades: ≥98%. CAS No. 879127-16-9. Molecular formula: C21H18F3N5O. Mole weight: 413.4.
Avitinib
Avitinib (Abivertinib) is a third-generation, irreversible and orally active selective EGFR inhibitor, with IC 50 values of 0.18 nM, 0.18 nM, 7.68 nM and against EGFR L858R , EGFR T790M and wild-type EGFR. Avitinib is also a BTKinhibitor that induces apoptosis and inhibits phosphorylation of BTK in mantle cell lymphoma. Avitinib shows anticancer effects [1] [2]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: Abivertinib; AC0010. CAS No. 1557267-42-1. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg. Product ID: HY-19816.
Avitinib maleate
Avitinib (Abivertinib) maleate is a third-generation, irreversible and orally active selective EGFR inhibitor, with IC 50 values of 0.18 nM, 0.18 nM, 7.68 nM and against EGFR L858R , EGFR T790M and wild-type EGFR. Avitinib maleate is also a BTKinhibitor that induces apoptosis and inhibits phosphorylation of BTK in mantle cell lymphoma. Avitinib maleate shows anticancer effects [1] [2]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: Abivertinib maleate; AC0010 maleate. CAS No. 1557268-88-8. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-19816A.
AVL-292
AVL-292, also known as CC-292, is an orally bioavailable, selective inhibitor of Bruton's agammaglobulinemia tyrosine kinase (BTK), with potential antineoplastic activity. Upon administration, AVL-292 targets and covalently binds to BTK, thereby preventing its activity. Uses: Protein kinase inhibitors. Synonyms: CC-292; CC292; CC 292; AVL292; AVL 292; spebrutinib. Grades: 98%. CAS No. 1202757-89-8. Molecular formula: C22H22FN5O3. Mole weight: 423.44.
AVL-292 benzenesulfonate
AVL-292 benzenesulfonate is a covalent, highly selective, orally active small molecule inhibitor of Btk with IC50 value of 0.5 nM; >1400-fold selectivity over the other kinases assayed. Synonyms: Spebrutinib besylate; CC-292 besylate; AVL-292 benzenesulfonate; CC 292 besylate; AVL 292 benzenesulfonate; CC292 besylate; AVL292 benzenesulfonate. Grades: >98%. CAS No. 1360053-81-1. Molecular formula: C28H28FN5O6S. Mole weight: 581.62.
BAY 61-3606
BAY 61-3606 is a potent, ATP-competitive, reversible, and highly selective inhibitor of Syk tyrosine kinase activity with no inhibitory effect against Btk, Fyn, Itk, Lyn, and Src. Synonyms: BAY 61-3606; BAY 613606; BAY 61 3606; BAY-61-3606; BAY613606; BAY61 3606. Grades: >98%. CAS No. 732983-37-8. Molecular formula: C20H18N6O3. Mole weight: 390.4.
BAY 61-3606 dihydrochloride
BAY 61-3606 is a potent, ATP-competitive, reversible, and highly selective inhibitor of Syk tyrosine kinase activity with no inhibitory effect against Btk, Fyn, Itk, Lyn, and Src. Synonyms: BAY 61-3606 dihydrochloride; BAY-61-3606 dihydrochloride; BAY61-3606 dihydrochloride. Grades: >98%. CAS No. 648903-57-5. Molecular formula: C20H18N6O3.2HCl. Mole weight: 463.32.
BAY 61-3606 hydrochloride
BAY 61-3606 is a cell-permeable, reversible inhibitor of spleen tyrosine kinase (Syk; Ki=7.5 nM; IC50=10 nM). It is 700 to >1,000-fold more selective for Syk over Src, Lyn, Fyn, Itk, and Btk. BAY 61-3606 can inhibit degranulation (IC50 = 5-46 nM) and block cytokine release from mast cells. It shows good in vivo efficacy in the treatment of various allergy and asthma conditions in rat models. This compound has been used in a pre-clinical model to explore the feasibility of targeting Syk in the treatment of retinoblastoma. Synonyms: 2-[[7-(3,4-dimethoxyphenyl)imidazo[1,2-c]pyrimidin-5-yl]amino]-3-pyridinecarboxamide monohydrochloride; BAY 61-3606 HCl. Grades: ≥98%. CAS No. 1615197-10-8. Molecular formula: C20H18N6O3·HCl. Mole weight: 426.9.
Bay 61-3606 Hydrochloride (2-[[7- (3, 4-Dimethoxyphenyl) imidazo[1, 2-c]pyrimidin-5-yl]amino]pyridine-3-carboxamide, HCl)
Cell-permeable. A potent, ATP-competitive and reversible inhibitor of spleen tyrosine kinase (Syk) (IC50 = 10nM). Displays excellent selectivity against many other kinases including Btk, Fyn, Itk, Lyn and Src up to concentrations of 4.7uM. Shows good in vivo efficacy in the treatment of various allergy and asthma conditions in rat models. Group: Biochemicals. Alternative Names: 2-[[7- (3, 4-Dimethoxyphenyl) imidazo[1, 2-c]pyrimidin-5-yl]amino]pyridine-3-carboxamide, HCl. Grades: Highly Purified. CAS No. 732938-37-8. Pack Sizes: 1mg. US Biological Life Sciences.
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BGB-3111
BGB-3111 is a potent, selective and orally available Bruton's tyrosine kinase (Btk) inhibitor that demonstrates superior oral bioavailability, achieving higher exposure and more complete target inhibition in the tissues than ibrutinib. Uses: Antineoplastic agents. Synonyms: 2-(4-phenoxyphenyl)-7-(1-prop-2-enoylpiperidin-4-yl)-1,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide; SCHEMBL16208602; BDBM249900; BGB-3111; BGB 3111; BGB3111. CAS No. 1633350-06-7. Molecular formula: C27H29N5O3. Mole weight: 471.55.
BIIB091
BIIB091 is a potent, selective, orally active and reversible BTKinhibitor, with an IC 50 of <0.5 nM. BIIB091 binds the BTK protein to sequester TYR-551 into an inactive conformation with excellent affinity. BIIB091 can be used for the research of multiple sclerosis [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 2247614-80-6. Pack Sizes: 10 mM * 1 mL; 1 mg; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-139984.
BMS-935177
BMS-935177 is a potent and selective reversible inhibitor of Bruton's tyrosine kinase (BTK) with an IC50 of 3 nM and demonstrates good kinase selectivity. It is more potent against BTK than other kinase, including the other Tec family kinases (TEC, BMX, ITK, and TXK) over which the compound is between 5- and 67-fold selective. BMS-935177 inhibited calcium flux in human Ramos B cells with IC50 of 27 nM and inhibited CD69 surface expression in peripheral B cells stimulated with anti-IgM and anti-IgG. Synonyms: BMS-935177; BMS935177. Grades: ≥98%. CAS No. 1231889-53-4. Molecular formula: C31H26N4O3. Mole weight: 502.56.
BMS-986142
BMS-986142 is a potent and highly selective reversible small molecule inhibitor of BTK with an IC50 of 0.5 nM. In a panel of 384 kinases, only five kinases were inhibited by BMS-986142 with less than 100-fold selectivity for BTK (TEC, ITK, BLK, TXK and BMX). Group: Fluorinated apis. CAS No. 1643368-58-4. Molecular formula: C32H30F2N4O4. Mole weight: 572.62. Appearance: White to off-white solid powder. Purity: >98%. IUPACName: (7S)-3-fluoro-4-[3-(8-fluoro-1-methyl-2,4-dioxoquinazolin-3-yl)-2-methylphenyl]-7-(2-hydroxypropan-2-yl)-6,7,8,9-tetrahydro-5H-carbazole-1-carboxamide. Catalog: OFC1643368584.
BMS-986142
Bruton's tyrosine kinase (BTK) is a nonreceptor tyrosine kinase. It is a member of the Tec family of kinases. BTK plays an essential role in B cell receptor (BCR)-mediated signaling as well as Fcγ receptor signaling in monocytes and Fcε receptor signaling. BMS-986142 is a potent, selective and reversible BTKinhibitor with IC50 of 0.5 nM. It potently inhibits BCR-stimulated expression of CD69 on B cells in human whole blood with IC50 of 90 nM. Synonyms: BMS-986142; BMS986142. Grades: ≥98%. CAS No. 1643368-58-4. Molecular formula: C32H30F2N4O4. Mole weight: 572.60.
BMS-986195
BMS-986195 is a Bruton's tyrosine kinase (BTK) inhibitor with IC50 of 0.1 nM. Synonyms: Branebrutinib; BMS 986195; BMS986195. Grades: ≥98% by HPLC. CAS No. 1912445-55-6. Molecular formula: C20H23FN4O2. Mole weight: 370.42.
BMS986195 R-isomer
An R isomer of BMS-986195, a potent and selective inhibitor of Bruton's tyrosine kinase (BTK). Synonyms: (R)-4-(3-(But-2-ynamido)piperidin-1-yl)-5-fluoro-2,3-dimethyl-1H-indole-7-carboxamide; (R)-Branebrutinib; (R)-BMS-986195. CAS No. 1912445-70-5. Molecular formula: C20H23FN4O2. Mole weight: 370.42.
BMX-IN-1
A cell-permeable tricyclic quinoline-acrylamide compound that potently inhibits BMX and BTK kinase activity (IC50 = 8 and 10.4nM, respectively) by covalently targeting ATP-binding site cysteine, while being less potent against TEC family kinases TEC, JAK3, BLK with the same conserved cysteine (IC50 = 175, 377, and 653nM, respectively). Only PI 3-K gamma/PIK3CG, SBK1, PIP5K2C (by ≥94% at 1uM), and TXK (by 75% at 1uM) are significantly inhibited by BMX-IN-1 in a selectivity profiling against 437 other kinase constructs. Potently inhibits the proliferation of TEL-BMX transformed Ba/F3 Ba/F3 (GI50 = 25nM), while being much less effective against TEL-BLK, TEL-JAK1, TEL-JAK2, TEL-JAK3, or TEL-TYK2E957D transformed Ba/F3 (GI50 = ≥3.64uM) or a panel of 5 prostate cancer cell lines (GI50 ≥2.46uM). Group: Biochemicals. Alternative Names: N- (2-Methyl-5- (9- (4- (methylsulfonamido) phenyl) -2-oxobenzo[h][1, 6]naphthyridin-1 (2H) -yl) phenyl) acrylamide, BMX/BTKInhibitor, Bruton's Tyrosine Kinase Inhibitor IV, BLK Inhibitor I, BMX Inhibitor I, JAK3 Inhibitor XIII, PI 3-K Inhibitor XX, PIP5K2C Inhibitor I, SBK1 Inhibitor I, TEC Inhibitor I, TXK Inhibitor I. Grades: Highly Purified. CAS No. 1431525-23-4. Pack Sizes: 10mg. Molecular Formula: C??H??N?O?S. US Biological Life Sciences.
Worldwide
Branebrutinib
Branebrutinib (BMS-986195) is a highly potent, selective covalent, irreversible inhibitor of Brutons tyrosine kinase (BTK) , with an IC 50 of 0.1 nM [1] [2]. Branebrutinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. Uses: Scientific research. Group: Signaling pathways. Alternative Names: BMS-986195. CAS No. 1912445-55-6. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-112161.
Branebrutinib
Branebrutinib / BMS-986195 is a potent, covalent, irreversible inhibitor of Bruton's tyrosine kinase (BTK), a member of the Tec family of non-receptor tyrosine kinases essential in antigen-dependent B-cell signaling and function. BMS-986195 is more than 5000-fold selective for BTK over all kinases outside of the Tec family, and selectivity ranges from 9- to 1010-fold within the Tec family. Group: Fluorinated apis. Alternative Names: BMS-986195. CAS No. 1912445-55-6. Molecular formula: C20H23FN4O2. Mole weight: 370.43. Appearance: White to off-white solid powder. Purity: >98%. IUPACName: 4-[(3S)-3-(but-2-ynoylamino)piperidin-1-yl]-5-fluoro-2,3-dimethyl-1H-indole-7-carboxamide. Catalog: OFC1912445556.
CGI1746
CGI1746 is a small-molecule Btkinhibitor chemotype with a new binding mode that stabilizes an inactive nonphosphorylated enzyme conformation. CGI1746 has exquisite selectivity for Btk and inhibits both auto- and transphosphorylation steps necessary for enzyme activation. Group: Inhibitors. Alternative Names: CGI1746; CGI-1746; CGI 1746. CAS No. 910232-84-7. Molecular formula: C34H37N5O4. Mole weight: 579.69. Appearance: White to off-white solid powder. Purity: >98%. IUPACName: 4-(tert-butyl)-N-(2-methyl-3-(4-methyl-6-((4-(morpholine-4-carbonyl)phenyl)amino)-5-oxo-4,5-dihydropyrazin-2-yl)phenyl)benzamide. Canonical SMILES: O=C (NC1=CC=CC (C (N=C2NC3=CC=C (C (N4CCOCC4)=O)C=C3)=CN (C)C2=O)=C1C)C5=CC=C (C (C) (C)C)C=C5. Catalog: ACM910232847.
CGI1746
CGI1746 is a small-molecule Btkinhibitor chemotype with a new binding mode that stabilizes an inactive nonphosphorylated enzyme conformation. CGI1746 has exquisite selectivity for Btk and inhibits both auto- and transphosphorylation steps necessary for enzyme activation. Synonyms: CGI1746; CGI-1746; CGI 1746. 4-(tert-Butyl)-N-(2-methyl-3-(4-methyl-6-((4-(morpholine-4-carbonyl)phenyl)amino)-5-oxo-4,5-dihydropyrazin-2-yl)phenyl)benzamide. Grades: 98%. CAS No. 910232-84-7. Molecular formula: C34H37N5O4. Mole weight: 579.69.
CGI560
CGI560 is a potent BTKinhibitor with IC50 = 400 nM for BTK. Synonyms: CGI-560; CGI 560; 4-(tert-Butyl)-N-(3-(8-(phenylamino)imidazo[1,2-a]pyrazin-6-yl)phenyl)benzamide. CAS No. 845269-74-1. Molecular formula: C29H27N5O. Mole weight: 461.57.
CHMFL-BMX-078
CHMFL-BMX-078 is a highly potent and selective type II irreversible BMX kinase inhibitor that exhibits an IC50 of 11 nM against BMX kinase and exhibits great selectivity over kinases such as BTK, JAK3, EGFR, and MAP2K7 that bore a structurally identical cysteine residue in BMX kinase. Uses: Protein kinase inhibitors. Synonyms: CHMFL-BMX-078; CHMFL-BMX 078;CHMFL BMX 078; CHMFLBMX078; 4- (methylamino) -2-[4-methyl-3- (prop-2-enoylamino) anilino]-N-[2-methyl-5-[ (3, 4, 5-trimethoxybenzoyl) amino]phenyl]pyrimidine-5-carboxamide; 2-((3-acrylamido-4-methylphenyl)amino)-N-(2-methyl-5-(3,4,5-trimethoxybenzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide. CAS No. 1808288-51-8. Molecular formula: C33H35N7O6. Mole weight: 625.67.
CHMFL-FLT3-122
CHMFL-FLT3-122 is a potent and selective FLT3 inhibitor (IC50 = 40 nM) with >10-fold and 170-fold selectivity for FLT3 over BTK kinase and c-KIT kinase. It causes apoptosis via cell cycle arrest in G0/G1 phase in vitro. In MV4-11 cell inoculated xenograft model, it suppressed tumor growth. Uses: Antitumor agent. Synonyms: CHMFL-FLT3-122; CHMFL FLT3 122; CHMFLFLT3122; 1-[(3R)-3-[4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-1-piperidinyl]-2-(dimethylamino)-ethanone. CAS No. 1839150-56-9. Molecular formula: C26H29N7O2. Mole weight: 471.55.
CNX-500
CNX-500 is a probe consisting of a covalent Btkinhibitor (CC-292) chemically linked to biotin. CNX-500 retains inhibitory activity against Btk ( IC 50 of 0.5 nM) and the ability to form a covalent bond with Btk. CNX-500 has low inhibitory effects on kinase epidermal growth factor receptor, and upstream Src-family kinases including Syk and Lyn [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 1202758-21-1. Pack Sizes: 1 mg; 5 mg; 10 mg; 25 mg. Product ID: HY-100338.
CNX-774
CNX-774 is a potent Btkinhibitor (IC50 < 1 nM). Synonyms: CNX-774; CNX 774; CNX774. CAS No. 1202759-32-7. Molecular formula: C26H22FN7O3. Mole weight: 499.49638.
CTA056
CTA056 is a potent and selective ITK inhibitor (interleukin-2-inducible T-cell kinase inhibitor). ITK is a member of the Btk (Bruton's tyrosine kinase) family of tyrosine kinases, plays an important role in normal T-cell functions and in the pathophysiology of both autoimmune diseases and T-cell malignancies. CTA056 exhibits the highest inhibitory effects toward Itk, followed by Btk and endothelial and epithelial tyrosine kinase. Among the 41 cancer cell lines analyzed, CTA056 selectively targets acute lymphoblastic T-cell leukemia and cutaneous T-cell lymphoma. CTA056 may be potential therapeutic agent for the treatment of T-cell leukemia and lymphoma. Synonyms: CTA-056; CTA 056; 1,5-Dihydro-7-(phenylmethyl)-1-[3-(1-piperidinyl)propyl]-2-[4-(4-pyridinyl)phenyl]-6H-imidazo[4,5-g]quinoxalin-6-one. Grades: 98%. CAS No. 1265822-30-7. Molecular formula: C35H34N6O. Mole weight: 554.69.
CZC-8004
CZC-8004 is an aminopyrimidine which is a pan-kinase inhibitor that binds a range of tyrosine kinases, including ABL, BTK, FAK, FER, JAK1, SRC, SYK, TEC, TNK1, TYK2, and YES. Synonyms: Dianilinopyrimidine-01; CZC-00008004. Grades: ≥98%. CAS No. 916603-07-1. Molecular formula: C17H16FN5. Mole weight: 309.3.
EDA-m7GTP - DYQ-660
EDA-m7GTP, a guanosine triphosphate derivative, acts as a ligand, facilitating the study of mRNA cap recognition mechanisms and development of antiviral drugs effective against RNA virus-caused diseases. Meanwhile, DYQ-660, a reversible BTKinhibitor, provides therapeutic relief against autoimmune diseases. An exploration of the compounds' inherent properties may offer novel ailments, presenting newfound potential in drug development. Synonyms: 2'/3'-O-(2-Aminoethyl-carbamoyl)-7-methyl-guanosine-5'-triphosphate, labeled with DYQ 660, Triethylammonium salt. Grades: ≥ 95 % by HPLC. Molecular formula: C53H66N9O20P3S (free acid). Mole weight: 1274.13 (free acid).
(E)-Rilzabrutinib
Rilzabrutinib (PRN1008) is a reversible covalent, selective and oral active inhibitor of Brutons Tyrosine Kinase (BTK) , with an IC 50 of 1.3 nM. Uses: Scientific research. Group: Signaling pathways. Alternative Names: (E)-PRN1008. CAS No. 1575596-29-0. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-112166.
Evobrutinib
Evobrutinib (M2951) is an orally active, potent, highly selective and irreversibly covalent BTKinhibitor, with an IC 50 of 8.9 nM. Evobrutinib (M2951) can be used for the research of autoimmune diseases [1]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: M2951; MSC2364447C. CAS No. 1415823-73-2. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-101215.
Fenebrutinib
Fenebrutinib (GDC-0853) is a potent, selective, orally available, and noncovalent bruton's tyrosine kinase ( Btk ) inhibitor with K i s of 0.91 nM, 1.6, 1.3, 12.6, and 3.4 nM for WT Btk, and the C481S, C481R, T474I, T474M mutants. Fenebrutinib has the potential for rheumatoid arthritis and systemic lupus erythematosus research [1]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: GDC-0853. CAS No. 1434048-34-6. Pack Sizes: 10 mM * 1 mL; 2 mg; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-19834.
GDC-0834
GDC-0834 is a potent and selective inhibitor of Bruton's tyrosine kinase (BTK), investigated as a potential treatment for rheumatoid arthritis. In vitro metabolite identification studies in hepatocytes revealed predominant formation of an inactive metabolite (M1) via amide hydrolysis in human. Synonyms: GDC-0834; GDC0834; GDC 0834. CAS No. 1133432-46-8. Molecular formula: C33H36N6O3S. Mole weight: 596.74.
GDC-0837
GDC-0834 is a small molecule inhibitor of Btk potentially useful in the treatment of RA and lymphoid malignancies. Administration of GDC-0834 (30 -- 100 mg/kg) in a rat CIA model induced a decrease of ankle swelling and reduction of morphologic pathology in a dose-dependent manner. Synonyms: GDC-0837; GDC 0837; GDC0837. CAS No. 1133432-49-1. Molecular formula: C33H36N6O3S. Mole weight: 596.74.
GDC-0853
GDC-0853 is a Bruton's tyrosine kinase (BTK) inhibitor originated by Genentech. GDC-0853 can inhibit the activity of BTK and prevent the activation of the B-cell antigen receptor (BCR) signaling pathway. This leads to the inhibition of the growth of malignant B-cells that overexpress BTK. Phase III clinical trials for the treatment of Multiple sclerosis and Phase II clinical trials for the treatment of Chronic urticaria and Systemic lupus erythematosus are on-going. Uses: Rheumatoid arthritis; autoimmune disorders. Synonyms: Fenebrutinib; RG 7845; RG7845; GDC0853; RG-7845; GDC 0853; (S)-2-(3'-(hydroxymethyl)-1-methyl-5-((5-(2-methyl-4-(oxetan-3-yl)piperazin-1-yl)pyridin-2-yl)amino)-6-oxo-1,6-dihydro-[3,4'-bipyridin]-2'-yl)-7,7-dimethyl-3,4,7,8-tetrahydro-2H-cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-1(6H)-one. Grades: 98%. CAS No. 1434048-34-6. Molecular formula: C37H44N8O4. Mole weight: 664.81.
GSK 2250665A
GSK 2250665A is an Itk inhibitor (pKi = 9.2) displaying selectivity for Itk over Aurora B kinase and Btk (pIC50 = 6.4 and 6.5, respectively) and a panel of other kinases. GSK 2250665A was shown to inhibit IFNγ production in PBMCs. Synonyms: GSK-2250665A; GSK 2250665A; GSK2250665A; GSK-2250665; GSK 2250665; GSK2250665; trans-4-[[4-[(6-Ethyl-2-benzothiazolyl)amino]-6-(phenylmethyl)-2-pyrimidinyl]amino]cyclohexanol. Grades: ≥97% by HPLC. CAS No. 1246030-96-5. Molecular formula: C26H29N5OS. Mole weight: 459.61.
Ibrutinib
Ibrutinib is a potent and selective BTKinhibitor (IC50=0.5 nM). Synonyms: PCI-32765; PCI 32765; (R)-1-(3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one. Grades: ≥95%. CAS No. 936563-96-1. Molecular formula: C25H24N6O2. Mole weight: 440.50.
Ibrutinib
Ibrutinib (PCI-32765) is a selective, irreversible Btkinhibitor with an IC 50 of 0.5 nM [1]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: PCI-32765. CAS No. 936563-96-1. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg; 200 mg; 500 mg. Product ID: HY-10997.
Ibrutinib-d4
Ibrutinib-d4 is the labelled analogue of Ibrutinib (I124970). Ibrutinib is a highly selective BrutonÂs tyrosine kinase (Btk) irreversible inhibitor. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 1mg. Molecular Formula: C25H20D4N6O2, Molecular Weight: 444.52. US Biological Life Sciences.
Worldwide
Ibrutinib deacryloylpiperidine
Ibrutinib deacryloylpiperidine (IBT4A) is an impurity of Ibrutinib [1]. Ibrutinib is a selective, irreversible Btkinhibitor with an IC 50 of 0.5 nM [2]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: IBT4A. CAS No. 330786-24-8. Pack Sizes: 10 mM * 1 mL; 100 mg; 500 mg; 1 g; 5 g. Product ID: HY-78727.
Ibrutinib, Free Base
Ibrutinib, also known as PCI-32765, is a selective and irreversible inhibitor of the enzyme Bruton's tyrosine kinase (BTK). It inhibited BTK potently, with an IC50 of 0.72 nM in enzymology assays and with an IC50 of 10 nM in cellular assay with Ramos cells. It demonstrated preference toward BTK over closely related kinases, blocked B cell function and BTK-dependent processes, and demonstrated clear efficacy in a mouse arthritis model. Young P.R., et al. "Discovery of selective irreversible inhibitors for Bruton's tyrosine kinase." ChemMedChem. 2: 58-61 (2007). Group: Biochemicals. Alternative Names: 1-[(3R)-3-[4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-1-piperidinyl]-2-propen-1-one; PCI 32765; PCI 32765-00; CRA 032765; (R)-1-(3-(4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one; Imbruvica. Grades: Purified. CAS No. 936563-96-1. Pack Sizes: 5mg, 25mg, 50mg. US Biological Life Sciences.
Worldwide
Ibrutinib Impurity 8
Ibrutinib Impurity 8 is a useful synthetic intermediate in the synthesis of Ibrutinib, a highly selective Bruton's tyrosine kinase (BTK) irreversible inhibitor. Synonyms: 3-(4-Phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine; 5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-ylamine; 4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidine; 1H-Pyrazolo[3,4-d]pyrimidin-4-amine, 3-(4-phenoxyphenyl)-; Ibrutinib intermeidate N-2. Grades: ≥97% by HPLC. CAS No. 330786-24-8. Molecular formula: C17H13N5O. Mole weight: 303.33.
Ibrutinib Racemate
Ibrutinib Racemate (PCI-32765 Racemate) is the racemate of Ibrutinib. Ibrutinib is a selective, irreversible Btkinhibitor with IC 50 value of 0.5 nM. Uses: Scientific research. Group: Signaling pathways. Alternative Names: PCI-32765 Racemate. CAS No. 936563-87-0. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-10997A.
JH-X-119-01
Jh-X-119-01 is a novel potent and selective interleukin-1 receptor-associated kinases 1 (IRAK1) inhibitor. JH-X-119-01 irreversibly labels IRAK1 at C302. This compound exhibited cytotoxic activity at single digit micromolar concentrations in a panel of WM, DLBCL, and lymphoma cell lines expressing MYD88. Cotreatment of JH-X-119-01 with the BTKinhibitor ibrutinib resulted in synergistic killing effects in these systems. Group: Inhibitors. Alternative Names: JH-X-119-01; JH-X119-01; JH-X 119-01; JH-X-11901; JH-X11901; JH-X 11901; JHX-11901; JHX11901; JHX 11901. CAS No. 2227368-54-7. Molecular formula: C25H20N6O3. Mole weight: 452.47. Appearance: Solid powder. Purity: >98%. IUPACName: N-(4-(3-Acrylamidobenzamido)phenyl)-6-(1H-pyrazol-5-yl)picolinamide. Canonical SMILES: O=C (NC1=CC=C (NC (C2=CC=CC (NC (C=C)=O)=C2)=O)C=C1)C3=NC (C4=CC=NN4)=CC=C3. Catalog: ACM2227368547.
JNJ-64264681
JNJ-64264681 is a potent, orally active, selective and irreversible covalent BTKinhibitor. JNJ-64264681 exhibits good pharmacokinetic characteristics and can be used for cancer and autoimmune diseases research [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 2101524-34-7. Pack Sizes: 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-153245.
JS25
JS25 is a selective and covalent inhibitor of BTK that inactivates BTK with an IC 50 value of 5.8 nM by chelating Tyr551. JS25 inhibits cancer cells proliferation, pronounces cell death, and promotes murine xenograft model of Burkitts lymphoma. JS25 effectively crosses the blood-brain barrier [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 2411771-95-2. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg. Product ID: HY-151808.
Lck inhibitor 2
Lck inhibitor 2 is a bis-anilinopyrimidine inhibitor of tyrosine kinases including LCK, BTK, LYN, SYK, and TXK. It inhibited 48 kinases with control less than 1%(33 of them tyrosine kinases, almost half of the 71 tyrosine kinases in the panel). Synonyms: Benzamide, 3-[[4-[(5-hydroxy-2-methylphenyl)amino]-2-pyrimidinyl]amino]-. Grades: >98%. CAS No. 944795-06-6. Molecular formula: C18H17N5O2. Mole weight: 335.36.
LFM-A13
LFM-A13 is a potent and selective inhibitor of Bruton's tyrosine kinase (BTK). LFM-A13 may be useful as a new class of chemosensitizing and apoptosis-promoting antileukemic agents for treatment of patients with chemotherapy-resistant B-lineage leukemias or lymphomas. Synonyms: 2-Butenamide, 2-cyano-N-(2,5-dibromophenyl)-3-hydroxy-; 2-Cyano-N-(2,5-dibromophenyl)-3-hydroxy-2-butenamide; 2-Cyano-3-hydroxy-but-2-enoic acid (2,5-dibromo-phenyl)-amide; LFM-A13/DDE-28; α-Cyano-β-hydroxy-β-methyl-N-(2,5-dibromophenyl)propenamide. Grades: ≥95%. CAS No. 62004-35-7. Molecular formula: C11H8Br2N2O2. Mole weight: 360.00.
LFM-A13
LFM-A13 is a potent BTK , JAK2 , PLK inhibitor, inhibits recombinant BTK, Plx1 and PLK3 with IC 50 s of 2.5 μM, 10 μM and 61 μM. LFM-A13 has antiproliferative activity and anticancer activity. LFM-A13 can be used in cancer-related research [1] [3] [4]. Uses: Scientific research. Group: Biochemical assay reagents. CAS No. 62004-35-7. Pack Sizes: 5 mg; 10 mg. Product ID: HY-110002.
N1,N6 [ 1,3-(1-Oxopropylene)] Ibrutinib
N1,N6 [ 1,3-(1-Oxopropylene)] Ibrutinib is an impurity of Ibrutinib (I124970), a highly selective BrutonÂs tyrosine kinase (Btk) irreversible inhibitor. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 5mg, 10mg. Molecular Formula: C28H26N6O3, Molecular Weight: 494.54. US Biological Life Sciences.
Worldwide
Nemtabrutinib
ARQ 531 (MK-1026) is a reversible non-covalent and orally active inhibitor of Brutons Tyrosine Kinase ( BTK ), with IC 50 s of 0.85 nM and 0.39 nM for WT-BTK and C481S-BTK, respectively. Uses: Scientific research. Group: Signaling pathways. Alternative Names: ARQ-531; MK-1026. CAS No. 2095393-15-8. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-112215.
Olmutinib
Olmutinib, also called as HM61713 and BI-1482694, is an orally available, mutant-selective third-generation epidermal growth factor receptor tyrosine kinase inhibitor (EGFR TKI) that is being developed for treatment of advanced and metastatic EGFR mutation-positive non-small cell lung cancer (NSCLC). In May 2016, olmutinib received its first global approval in South Korea for the treatment of EGFR T790M mutation-positive lung cancer. Olmutinib is also a potent small molecule inhibitor of Bruton's tyrosine kinase (BTK). Synonyms: N-(3-((2-((4-(4-methylpiperazin-1-yl)phenyl)amino)thieno[3,2-d]pyrimidin-4-yl)oxy)phenyl)acrylamide; HM61713; HM 61713; HM-61713; BI 1482694; BI-1482694; BI1482694; Olmutinib. Grades: >98%. CAS No. 1353550-13-6. Molecular formula: C26H26N6O2S. Mole weight: 486.18.
ONO-4059
ONO-4059, a BTKinhibitor, has been found to have potential effect against sorts of malignancies by influencing the B-cell development. It is currently under Phase II trail to study its effect against Chronic lymphocytic leukaemia. IC50: 2.2 nM. Synonyms: (R)-6-amino-9-(1-(but-2-ynoyl)pyrrolidin-3-yl)-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8-one; ONO-4059; ONO4059; ONO 4059; ONO-4059; GS 4059; GS-4059; GS4059; ONO-WG-307; Tirabrutinib. Grades: 98%. CAS No. 1351636-18-4. Molecular formula: C25H22N6O3. Mole weight: 454.48.
ONO-4059 analog
ONO-4059 analog is an analogue of ONO-4059, and ONO-4059 (HY-15771) is a highly potent and selective Btkinhibitor. Uses: Scientific research. Group: Signaling pathways. CAS No. 1351635-67-0. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-18951.
ONO-4059 analogue
ONO-4059 analogue is an analogue of ONO-4059, which is a highly potent and selective oral BTKinhibitor with IC50 of 23.9 nM. Phase 1. Synonyms: ONO-WG-307; ONO-4059 analogue; ONO 4059 analogue; ONO4059 analogue. Grades: 98%. CAS No. 1351635-67-0. Molecular formula: C25H24N6O3. Mole weight: 456.5.
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