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Mutant EGFR inhibitor is a potent and selective mutant EGFR inhibitor extracted from patent WO 2013014448 A1; inhibits EGFR L858R , EGFR Exon 19 deletion and EGFR T790M. Uses: Scientific research. Group: Signaling pathways. CAS No. 1421373-62-7. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg. Product ID: HY-13984.
Mutant EGFR inhibitor
Mutant EGFR inhibitor is a potent and selective mutant EGFR inhibitor extracted from patent WO 2013014448 A1. It inhibits EGFRL858R, EGFRExon 19 deletionand EGFRT790M. Synonyms: MDK3627; MDK 3627; MDK-3627; Mutant EGFR inhibitor. Grades: >98%. CAS No. 1421373-62-7. Molecular formula: C27H30ClN7O2. Mole weight: 520.03.
1-Methyl-4-(4-nitrophenyl)piperazine
1-methyl-4-(4-nitrophenyl)piperazine was a reagent in the preparation of diaminopyrimidines as reversible and irreversible inhibitors of mutant EGFR tyrosine kinases for treatment of non-small-cell lung cancer. It was also used in the prepn. of disubstituted pyrimidine compds. as EGFR or/and ALK inhibitors useful in the treatment of diseases. Group: Biochemicals. Grades: Highly Purified. CAS No. 16155-03-6. Pack Sizes: 500mg, 1g. Molecular Formula: C11H15N3O2, Molecular Weight: 221.26. US Biological Life Sciences.
Worldwide
ALW-II-41-27
ALW-II-41-27 is a Eph receptor tyrosine kinase inhibitor. pharmacologic inhibition of EPHA2 by the small-molecule inhibitor ALW-II-41-27 decreased both survival and proliferation of erlotinib-resistant tumor cells and inhibited tumor growth in vivo. ALW-II-41-27 was also effective in decreasing viability of cells with acquired resistance to the third-generation EGFR TKI AZD9291. Collectively, these data define a role for EPHA2 in the maintenance of cell survival of TKI-resistant, EGFR-mutant lung cancer and indicate that EPHA2 may serve as a useful therapeutic target in TKI-resistant tumors. Uses: Designed for use in research and industrial production. Additional or Alternative Names: ALW-II-41-27; ALW II-41-27; ALWII-41-27; ALW-II-4127; ALW II-4127; ALWII-4127. Product Category: Inhibitors. Appearance: Solid powder. CAS No. 1186206-79-0. Molecular formula: C32H32F3N5O2S. Mole weight: 607.7. Purity: >98%. IUPACName: N-(5-((4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)carbamoyl)-2-methylphenyl)-5-(thiophen-2-yl)nicotinamide. Canonical SMILES: O=C(NC1=CC(C(NC2=CC=C(CN3CCN(CC)CC3)C(C(F)(F)F)=C2)=O)=CC=C1C)C4=CN=CC(C5=CC=CS5)=C4. Product ID: ACM1186206790. Alfa Chemistry ISO 9001:2015 Certified.
AP-26113
AP26113 is an orally available inhibitor of receptor tyrosine kinases anaplastic lymphoma kinase (ALK) and the epidermal growth factor receptor (EGFR) with potential antineoplastic activity. AP26113 binds to and inhibits ALK kinase and ALK fusion proteins as well as EGFR and mutant forms. AP26113 appears to overcome mutation-based resistance. ALK belongs to the insulin receptor superfamily and plays an important role in nervous system development. Synonyms: AP-26113; AP 26113; AP26113; (2-((5-chloro-2-((4-(4-(dimethylamino)piperidin-1-yl)-2-methoxyphenyl)amino)pyrimidin-4-yl)amino)phenyl)dimethylphosphine oxide; AP26113-analog; AP-26113-analog; AP 26113-analog, Brigatinib-analog. Grades: 0.98. CAS No. 1197958-12-5. Molecular formula: C26H34ClN6O2P. Mole weight: 529.01.
AST-1306
AST-1306 is a selective irreversible inhibitor of the epidermal growth factor receptor (EGFR) 1 and 2. Studies show that AST-1306 inhibited the enzymatic activities of wild-type EGF) and ErbB2 as well as EGFR resistant mutant in both cell-free and cell-based systems. AST-1306 was more effective in inhibiting tumors with ErbB2-overexpressing cells than EGFR-overexpressing tumor. Group: Biochemicals. Alternative Names: N- [4- [ [3-Chloro-4- [ (3-fluorobenzyl) oxy] phenyl] amino] quinazolin-6-yl] acrylamide; N-[4-[[3-Chloro-4-[ (3-fluorophenyl) methoxy]phenyl]amino]-6-quinazolinyl]-2-propenamide; ALS1306; AST 1306; AST 6. Grades: Highly Purified. CAS No. 897383-62-9. Pack Sizes: 5mg. US Biological Life Sciences.
Worldwide
Avitinib
Avitinib (AC0010) is a third generation inhibitor of the EGFR (epidermal growth factor receptor) that was permitted parallel phase I clinical trials in the US. It is a pyrrolopyrimidine-based irreversible EGFR inhibitor that is mutation-selective with IC50 value of 0.18 nM against EGFR L858R/T790M double mutations. Upon oral administration, avitinib covalently binds to and inhibits the activity of mutant forms of EGFR. Uses: Tyrosine kinase inhibitors. Synonyms: AC0010. Grades: ≥98%. CAS No. 1557267-42-1. Molecular formula: C26H26FN7O2. Mole weight: 487.5.
Avitinib maleate
Avitinib maleate, the maleate salt form of avitinib, is a pyrrolopyrimidine-based, irreversible epidermal growth factor receptor (EGFR) mutant-selective inhibitor (IC50 = 7.68 nM), with potential antineoplastic activity. Uses: Tyrosine kinase inhibitors. Synonyms: Avitinib maleate; AC0010MA; AC-0010MA; AC 0010MA; AC0010; AC-0010; AC 0010. CAS No. 1557268-88-8. Molecular formula: C30H30FN7O6. Mole weight: 603.6.
AZD3759
AZD3759 is a n orally available inhibitor of the epidermal growth factor receptor (EGFR), with potential antineoplastic activity. Upon oral administration, AZD3759 binds to and inhibits the activity of EGFR as well as certain mutant forms of EGFR. Synonyms: AZD3759; AZD-3759; AZD 3759. Grades: 98%. CAS No. 1626387-80-1. Molecular formula: C22H23ClFN5O3. Mole weight: 459.91.
Brigatinib
Brigatinib, also known as AP-26113, is an orally active, potent and selective dual ALK/EGFR inhibitor. AP26113 is an orally bioavailable inhibitor of anaplastic lymphoma kinase (ALK; IC50 < 100 nM in Ba/F3 cells). AP26113 binds to and inhibits ALK kinase and ALK fusion proteins as well as EGFR and mutant forms. It blocks ALK activity and reduces growth in neuroblastoma cells, mouse xenograft, and Drosophila model systems harboring constitutively active ALK variants. Synonyms: AP26113. Grades: ≥98%. CAS No. 1197953-54-0. Molecular formula: C29H39ClN7O2P. Mole weight: 584.10.
CNX-2006
CNX-2006 is a potent and mutant-selective EGFR inhibitor with excellent in vitro activity in cells with activating EGFR mutations, as well as in cells harbouring the T790M mutation. CNX-2006 is the prototype for CO-1686, which is currently in a Phase I clinical trial for the treatment of EGFR-mutant lung cancer. Synonyms: CNX2006; CNX 2006; N-[3-[[2-[4-[[1-(2-fluoroethyl)azetidin-3-yl]amino]-2-methoxyanilino]-5-(trifluoromethyl)pyrimidin-4-yl]amino]phenyl]prop-2-enamide. Grades: 98%. CAS No. 1375465-09-0. Molecular formula: C26H27F4N7O2. Mole weight: 545.543.
Depatuxizumab
Depatuxizumab is a brain-penetrant and humanized tumor-specific anti EGFR monoclonal antibody. Depatuxizumab inhibits the growth of xenograft models of mutant EGFRvIII and wild-type EGFR. Depatuxizumab can be used for research on cancer [1]. Uses: Scientific research. Group: Inhibitory antibodies. Alternative Names: ABT-806. CAS No. 1471999-69-5. Pack Sizes: 1 mg; 5 mg; 10 mg. Product ID: HY-P99849.
EAI045
EAI045 is an allosteric, non-ATP competitive inhibitor of mutant EGFR. In vitro studies proved that EAI045 is active and selective for T790M- harboring EGFR mutants that are in a monomer state. In vivo the combination of EAI045 and cetuximab caused a marked tumor shrinkage in a mouse model carrying the EGFR mutant with L858R/T790M/C797S. Therefore, EAI045 is the first allosteric inhibitor that targets T790M and C797S EGFR mutants but it is effective only in combination with cetuximab. Synonyms: 2-(5-fluoro-2-hydroxyphenyl)-2-(3-oxo-1H-isoindol-2-yl)-N-(1,3-thiazol-2-yl)acetamide; 2-(5-fluoro-2-hydroxyphenyl)-2-(1-oxo-2,3-dihydro-1H-isoindol-2-yl)-N-(1,3-thiazol-2-yl)acetamide; EAI045; EAI 045; EAI-045. CAS No. 1942114-09-1. Molecular formula: C19H14FN3O3S. Mole weight: 383.397.
EGF816
EGF816, also called as Nazartinib, a covalent mutant-selective EGFR inhibitor and potently inhibits the T790M resistance mutation while sparing wild-type EGFR. in vivo: demonstrated strong tumor regressions in several EGFR activating and resistant tumor m. Synonyms: EGF816; EGF-816; EGF 816; NVS-816; NVS 816; NVS816; Nazartinib; N- [7-chloro -1- [ (3R) -1- [ (E) -4- (di methyl amino) but-2-enoyl ] azepan-3-yl ] benzimidazol-2-yl ] -2- methyl pyridine-4-carboxamide EGF816UNII-KE7K32EME8KE7K32EME8EGF-8161508250-71-2GTPL9204SCHEMBL16767232SCHEMBL16767 240EGF 816compound 47 [PMID: 27433829]. CAS No. 1508250-71-2. Molecular formula: C26H31ClN6O2. Mole weight: 495.02.
EGF816 mesylate
EGF816 mesylate is the mesylate salt of EGF816 which is a covalent mutant-selective EGFR inhibitor and potently inhibits the T790M. Synonyms: N-[7-chloro-1-[(3R)-1-[(E)-4-(dimethylamino)but-2-enoyl]azepan-3-yl]benzimidazol-2-yl]-2-methylpyridine-4-carboxamide;methanesulfonic acid. CAS No. 1508250-72-3. Molecular formula: C27H35ClN6O5S. Mole weight: 591.12.
EGFR-IN-2
EGFR-IN-2 is a a noncovalent, irreversible, mutant-selective second generation EGFR inhibitor. It showed excellent cellular activity against both the single and double mutants of EGFR, demonstrating target engagement in vivo and ADME-PK properties that are suitable for further evaluation. CAS No. 1643497-70-4. Molecular formula: C26H33N9O3S. Mole weight: 551.66.
EGFR mutant-IN-2
EGFR mutant-IN-2 (Compound D51) is an EGFR mutant inhibitor. EGFR mutant-IN-2 inhibits the EGFR L858R/T790M/C797S mutant with an IC 50 value of 14 nM. EGFR mutant-IN-2 inhibits the EGFR del19/T790M/C797S mutant with an IC 50 value of 62 nM. EGFR mutant-IN-2 has favorable PK parameters, safety properties, in vivo stability, and antitumor activity [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 2770009-06-6. Pack Sizes: 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-155005.
EGFR T790M/L858R-IN-8
EGFR T790M/L858R-IN-8 (compound 9) is a potent inhibitor of EGFR , targeting mutant EGFR T790M/L858R with IC 50 of 56.8 μM. The anti-proliferative effect of EGFR T790M/L858R-IN-8 on cancer cell lines A549, A431, and NHI-H1975 is not significant [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 333419-97-9. Pack Sizes: 5 mg; 10 mg. Product ID: HY-164056.
EMI1
EMI1 is an EGFR ex19del/T790M/C797S and EGFR L858R/T790M/C797S inhibitor. EMI1 can be used for the research of mutant EGFR-associated, drug-resistant non-small-cell lung cancer (NSCLC) [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 35773-42-3. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-138072.
Firmonertinib
Firmonertinib (Alflutinib; Furmonertinib) is an orally active, mutant-selective, and highly brain penetrant EGFR inhibitor. Firmonertinib inhibits EGFR active mutations as well as the T790M acquired resistant mutation. Firmonertinib has the potential for the research of cancer diseases, especially advanced non-small cell lung cancer (NSCLC) with EGFR ex20ins mutation [1]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: Alflutinib; Furmonertinib; AST2818. CAS No. 1869057-83-9. Pack Sizes: 5 mg; 10 mg; 25 mg; 50 mg. Product ID: HY-112870.
Firmonertinib mesylate
Firmonertinib (Alflutinib; Furmonertinib) mesylate is is an orally active, mutant-selective, and highly brain penetrant EGFR inhibitor. Firmonertinib mesylate inhibits EGFR active mutations as well as the T790M acquired resistant mutation. Firmonertinib mesylate has the potential for the research of cancer diseases, especially advanced non-small cell lung cancer (NSCLC) with EGFR ex20ins mutation [1]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: Alflutinib mesylate; Furmonertinib mesylate; AST2818 mesylate. CAS No. 2130958-55-1. Pack Sizes: 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-112870A.
Flumatinib
Flumatinib is a multi-kinase inhibitor of c-Abl, PDGFRβ and c-Kit with IC50 values of 1.2 nM, 307.6 nM and 2662 nM respectively. It can predominantly inhibit the autophosphorylation of Bcr-Abl in K562 cell in vitro. It can inhibit the phosphorylation of c-Kit in Mo7e cell and the phosphorylation of PDGFR in Swiss3T3 cell in higher concentration. It has no or little effect on other tyrosine kinase including EGFR?KDR?c-Src andHER2. It can reduce the expression of C-MYC, HIF-1 α and VEGF in U266 cell line in a time- and dose-dependent manners. It effectively overcame the drug resistance of certain KIT mutants with activation loop mutations. It was developed by Jiangsu Hansoh Pharmaceutical Co., Ltd. and is currently in Phase III clinical trials in China for the treatment of chronic myelogenous leukemia (CML). Uses: Flumatinib is used for the treatment of chronic myelogenous leukemia (cml). Synonyms: 4-[(4-methylpiperazin-1-yl)methyl]-N-(6-methyl-5-{[4-(pyridin-3-yl)pyrimidin-2-yl]amino}pyridin-3-yl)-3-(trifluoromethyl)benzamide; HH-GV678; HHGV678; HH GV678; 4-[(4-Methyl-1-piperazinyl)methyl]-N-(6-methyl-5-{[4-(3-pyridinyl)-2-pyrimidinyl]amino}-3-pyridinyl)-3-(trifluoromethyl)benzamide. Grades: >98%. CAS No. 895519-90-1. Molecular formula: C29H29F3N8O. Mole weight: 562.59.
Icotinib
Icotinib (BPI-2009) is a potent and specific EGFR inhibitor with an IC 50 of 5 nM; also inhibits mutant EGFR L858R , EGFR L858R/T790M , EGFR T790M and EGFR L861Q. Icotinib 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: BPI-2009. CAS No. 610798-31-7. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg. Product ID: HY-15164A.
Icotinib Hydrochloride
Icotinib Hydrochloride (BPI-2009) is a potent and specific EGFR inhibitor with an IC 50 of 5 nM; also inhibits mutant EGFR L858R , EGFR L858R/T790M , EGFR T790M and EGFR L861Q. Icotinib (Hydrochloride) 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: BPI-2009H. CAS No. 1204313-51-8. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg. Product ID: HY-15164.
IK-930
IK930, a novel TEAD inhibitor, sensitizes KRAS and EGFR mutant tumors to oncogene targeted therapy. CAS No. 2563892-44-2. Molecular formula: C19H19F3N4O2S. Mole weight: 424.44.
Iruplinalkib
Iruplinalkib (WX-0593) is an orally active and selective ALK/ROS1 inhibitor. Iruplinalkib can effectively inhibit tyrosine autophosphorylation of ALK and mutant ALK , EGFR , with the IC 50 between 5.38 and 16.74 nM. Iruplinalkib is also a suppressive agent of the transporter MATE1 , MATE2K , P-gp and BCRP. Iruplinalkib can be used in the study of non-small cell lung cancer [1] [2]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: WX-0593. CAS No. 1854943-32-0. Pack Sizes: 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-145574.
Lazertinib
Lazertinib, also known as YH-25448 and GNS-1480, is a potent, highly mutant-selective, blood-brain barrier permeable, orally available and irreversible 3rd generation EGFR tyrosine kinase inhibitor, and can be used in the research of non-small cell lung cancer. Lazertinib is expected to beneficial for the NSCLC patients with brain metastasis due to good blood brain barrier (BBB) penetration property as well as for the treatment of primary lung lesion and extracranial lesions. Uses: Protein kinase inhibitors. Synonyms: 2-Propenamide, N-(5-((4-(4-((dimethylamino)methyl)-3-phenyl-1H-pyrazol-1-yl)-2-pyrimidinyl)amino)-4-methoxy-2-(4-morpholinyl)phenyl)-; N-(5-((4-(4-((Dimethylamino)methyl)-3-phenyl-1H-pyrazol-1-yl)pyrimidin-2-yl)amino)-4-methoxy-2-morpholinophenyl)acrylamide; Lazertinib; YH-25448; YH 25448; YH25448; GNS-1480; GNS 1480; GNS1480. CAS No. 1903008-80-9. Molecular formula: C30H34N8O3. Mole weight: 554.64.
Lazertinib
Lazertinib (YH25448) is a potent, highly mutant-selective, blood-brain barrier permeable, orally available and irreversible third-generation EGFR tyrosine kinase inhibitor, and can be used in the research of non-small cell lung cancer [1]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: YH25448; GNS-1480. CAS No. 1903008-80-9. Pack Sizes: 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-109061.
Mobocertinib
Mobocertinib is an effective and orally active inhibitor of EGFR and HER2 oncogenic mutants. Anti-tumor activity. Synonyms: TAK-788; TAK788; AP32788. Grades: 98%. CAS No. 1847461-43-1. Molecular formula: C32H39N7O4. Mole weight: 585.7.
MTX-211
MTX-211 is a dual inhibitor of EGFR and PI3K, which plays important roles in the progression of KRAS mutant colorectal cancer. MTX-211 has the potential for the treatment of KRAS mutant colorectal cancer. Synonyms: MTX-211; MTX 211; MTX211; CS-7929; CS 7929; CS7929; HY-107364; HY 107364; HY107364; N-(2-chloro-5-(4-((3-chloro-4-fluorophenyl)amino)quinazolin-6-yl)pyridin-3-yl)methanesulfonamide. Grades: ≥98%. CAS No. 1952236-05-3. Molecular formula: C20H14Cl2FN5O2S. Mole weight: 478.323.
Naquotinib
Naquotinib is an irreversible, third-generation, mutant-selective, epidermal growth factor receptor (EGFR) inhibitor, with potential antineoplastic activity with IC50 of 8-33 nM toward EGFR mutants. Synonyms: ASP 8273; ASP8273; ASP-8273; (R)-5-((1-acryloylpyrrolidin-3-yl)oxy)-6-ethyl-3-((4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)amino)pyrazine-2-carboxamide. Grades: ≥98%. CAS No. 1448232-80-1. Molecular formula: C30H42N8O3. Mole weight: 562.719.
Naquotinib mesylate
Naquotinib is irreversible, third-generation, epidermal growth factor receptor (EGFR) inhibitor with IC50 value of 70 nM for NCI-H1650 cell growth. It can covalently bind to and inhibit the activity of mutant forms of EGFR, including the T790M EGFR mutant. So Naquotinib can prevent EGFR-mediated signaling. This may induce cell death and inhibit tumor growth in EGFR-overexpressing tumor cells. In Dec 2015, Phase-III clinical trials in Non-small cell lung cancer (First-line therapy, Late-stage disease) in Hungary was on-going. In Aug 2016, Phase-I clinical trials in Solid tumours in USA was on-going. Uses: Solid tumours;non-small cell lung cancer. Synonyms: ASP8273 mesilate; ASP 8273 mesilate; ASP-8273 mesilate; 6-Ethyl-3-((4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)amino)-5-(((3R)-1-(1-oxoprop-2-en-1-yl)pyrrolidin-3-yl)oxy)pyrazine-2-carboxamide monomethanesulfonate;448232-80-1 (free base). Grades: 98%. CAS No. 1448237-05-5. Molecular formula: C31H46N8O6S. Mole weight: 658.82.
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.
Osimertinib
Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC 50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer [1]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: AZD-9291; Mereletinib. CAS No. 1421373-65-0. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg; 200 mg; 500 mg; 1 g. Product ID: HY-15772.
Osimertinib mesylate
Osimertinib mesylate (AZD9291 mesylate) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC 50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer [1]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: AZD-9291 mesylate; Mereletinib mesylate. CAS No. 1421373-66-1. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg; 200 mg; 500 mg; 1 g. Product ID: HY-15772A.
Osimertinib (Standard)
Osimertinib (Standard) is the analytical standard of Osimertinib. This product is intended for research and analytical applications. Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC 50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 1421373-65-0. Pack Sizes: 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-15772R.
PF-06459988
PF-06459988 is a third-generation, irreversible epidermal growth factor receptor (EGFR) inhibitor. It can bind to and inhibit mutant forms of EGFR, including the secondary acquired resistance mutation T790M.PF-06459988 may have therapeutic benefits in tumors with T790M-mediated drug resistance. Preclinical trials in Non-small cell lung cancer in USA is on-going. Uses: Non-small cell lung cancer. Synonyms: PF-06459988; PF06459988; PF 06459988; PF-6459988; PF 6459988; PF6459988; 1-((3R,4R)-3-(((5-chloro-2-((1-methyl-1H-pyrazol-4-yl)amino)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy)methyl)-4-methoxypyrrolidin-1-yl)prop-2-en-1-one. Grades: 98%. CAS No. 1428774-45-1. Molecular formula: C19H22ClN7O3. Mole weight: 431.88.
Poziotinib
Poziotinib, also known as HM781-36B and NOV120101, is an orally bioavailable, quinazoline-based pan epidermal growth factor receptor (EGFR or HER) inhibitor with potential antineoplastic activity. HM781-36B irreversibly inhibits EGFR (HER1 or ErbB1), including EGFR mutants, HER2, and HER4, thereby inhibiting the proliferation of tumor cells that overexpress these receptors. EGFRs, cell surface receptor tyrosine kinases, are often upregulated in a variety of cancer cell types and play key roles in cellular proliferation and survival. Synonyms: HM781-36B; NOV120101; NOV-120101; NOV 120101; Poziotinib. CAS No. 1092364-38-9. Molecular formula: C23H21Cl2FN4O3. Mole weight: 491.344.
Poziotinib Hydrochloride
Poziotinib, also known as HM781-36B and NOV120101, is an orally bioavailable, quinazoline-based pan epidermal growth factor receptor (EGFR or HER) inhibitor with potential antineoplastic activity. HM781-36B irreversibly inhibits EGFR (HER1 or ErbB1), including EGFR mutants, HER2, and HER4, thereby inhibiting the proliferation of tumor cells that overexpress these receptors. EGFRs, cell surface receptor tyrosine kinases, are often upregulated in a variety of cancer cell types and play key roles in cellular proliferation and survival. Synonyms: Poziotinib HCl; NOV120101 hydrochloride; HM 781-36B hydrochloride. CAS No. 1429757-68-5. Molecular formula: C23H22Cl3FN4O3. Mole weight: 527.80.
Pruvonertinib
YK-029A is an orally active inhibitor of mutant EGFR , targeting to both the T790M mutations (EGFR T790M ) and exon 20 insertion of EGFR (EGFRex20ins). YK-029A exhibits significant antitumor activity, and results tumor regression in EGFRex20ins-driven PDX models [1]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: YK-029A. CAS No. 2064269-82-3. Pack Sizes: 10 mM * 1 mL; 1 mg; 5 mg; 10 mg; 25 mg. Product ID: HY-155537.
(Rac)-JBJ-04-125-02
(Rac)-JBJ-04-125-02 is the racemate of JBJ-04-125-02. JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 2140807-05-0. Pack Sizes: 10 mM * 1 mL; 1 mg; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-135805A.
Rociletinib
Rociletinib (CO-1686) is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the K i values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively. Uses: Scientific research. Group: Signaling pathways. Alternative Names: CO-1686; AVL-301; CNX-419. CAS No. 1374640-70-6. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-15729.
Rociletinib
Rociletinib is a third-generation irreversible kinase inhibitor of epidermal growth factor receptor (EGFR). Rociletinib was shown to inhibit the proliferation of non-small cell lung cancer (NSCLC) cells expressing mutant EGFR. It also exhibits anti-tumor activity in NSCLC EGFR mutant xenograft models. Synonyms: CO-1686; CO1686; CO 1686; AVL-301; AVL 301; AVL301; CNX-419; CNX 419; CNX419; N-[3-[[2-[4-(4-acetylpiperazin-1-yl)-2-methoxyanilino]-5-(trifluoromethyl)pyrimidin-4-yl]amino]phenyl]prop-2-enamide. CAS No. 1374640-70-6. Molecular formula: C27H28F3N7O3. Mole weight: 555.562.
Rociletinib hydrobromide
Rociletinib hydrobromide (CO-1686 hydrobromide) is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the K i values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively. Uses: Scientific research. Group: Signaling pathways. Alternative Names: CO-1686 hydrobromide; AVL-301 hydrobromide; CNX-419 hydrobromide. CAS No. 1446700-26-0. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-15729A.
Sorafenib, p-Toluenesulfonate Salt
Sorafenib (Bay 43-9006) is a novel bi-aryl urea compound that inhibits cell proliferation by targeting the ERK pathway and angiogenesis by targeting the receptor tyrosine kinases VEGFR-2 and PDGFR-b and their associated signaling cascades. Although sorafenib was initially developed as a Raf kinase inhibitor (IC50=6nM), it has since been shown to have activity against many receptor tyrosine kinases involved in tumorigenesis and angiogenesis including FGFR-1, wt BRAF and V599E mutant BRAF, as well as members of the so-called "split kinase" family: VEGFR-2, VEGFR-3, PDGFR-b, c-KIT, and Flt3. However, sorafenib is not active against erbB1, erbB2, ERK-1, MEK-1, EGFR, HER-2, IGFR-1, c-MET, c-yes, PKB, PKA, cdk1/cyclinB, PKC, and pim-1. In cellular mechanistic assays, sorafenib decreased basal phosphorylation of the ERK pathway in melanoma, breast, colon, and pancreatic tumor cell lines. Group: Biochemicals. Grades: Highly Purified. CAS No. 475207-59-1. Pack Sizes: 1g, 5g, 10g. Molecular Formula: C21H16ClF3N4O3 C7H8O3S, Molecular Weight: 637.03. US Biological Life Sciences.
Worldwide
SPH5030
SPH5030 is a selective and irreversible HER2 inhibitor. SPH5030 inhibits HER2 WT and EGFR WT with IC 50 s of 3.51 and 8.13 nM, respectively. SPH5030 shows excellent activities against HER2 mutants. SPH5030 can be used for the research of cancer [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 2364326-23-6. Pack Sizes: 5 mg; 10 mg; 25 mg; 50 mg. Product ID: HY-143319.
STX-721
STX-721 is a mutant-selective inhibitor of EGFR and HER2 Exon 20 insertion (ex20ins) mutants [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 2765525-82-2. Pack Sizes: 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-157229.
Sunvozertinib
Sunvozertinib (DZD9008) is a potent ErbBs (EGFR, Her2, especially mutant forms) and BTK inhibitor. Sunvozertinib shows IC 50 s of 20.4, 20.4, 1.1, 7.5, and 80.4 nM for EGFR exon 20 NPH insertion, EGFR exon 20 ASV insertion, EGFR L858R and T790M mutations, and Her2 Exon20 YVMA, and EGFR WT A431, respectively (patent WO2019149164A1, example 52) [1]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: DZD9008. CAS No. 2370013-12-8. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-132842.
Tamnorzatinib
Tamnorzatinib (ONO-7475) is a potent, selective, and orally active Axl/Mer inhibitor with IC50 values of 0.7 nM and 1.0 nM, respectively. Tamnorzatinib sensitizes AXL-overexpressing EGFR-mutant NSCLC cells to the EGFR-TKIs, suppresses the emergence and maintenance of tolerant cells. Tamnorzatinib combines with Osimertinib (HY-15772) provides a bright promise for the study of EGFR-mutated non-small cell lung cancer (NSCLC). Uses: Scientific research. Group: Signaling pathways. Alternative Names: ONO-7475. CAS No. 1646839-59-9. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-114358.
Transtinib
This active molecular is an irreversible EGFR ( epidermal growth factor receptor ) tyrosine kinase inhibitor. Transtinib shows good anti-proliferative activity against the H1975 and A431 cell lines and IC50 values is 34 nM and 62 nM. In xenograft models, Transtinib decreases tumor size for a prolonged period of time. Transtinib may become a drug candidate for the inhibition of mutant EGFR to overcome the development of resistance. Uses: Anti-cancer. Synonyms: (S,E)-N-(4-((3-chloro-4-((3-fluorobenzyl)oxy)phenyl)amino)-7-ethoxyquinazolin-6-yl)-3-(pyrrolidin-2-yl)acrylamide. Grades: 98%. CAS No. 1246089-27-9. Molecular formula: C30H29ClFN5O3. Mole weight: 562.04.
WZ-8040
WZ8040 is a novel mutant-selective irreversible EGFRT790M inhibitor with potential anticancer activity. WZ8040 is about 30-fold more potent against EGFR T790M, and up to 100-fold less potent against wild-type EGFR, than other quinazoline-based EGFR inhibitors such as CL-387785 and HKI-272. WZ-8040 may be clinically more effective and better tolerated than quinazoline-based inhibitors. Synonyms: WZ8040; WZ 8040. Grades: 0.98. CAS No. 1214265-57-2. Molecular formula: C24H25ClN6OS. Mole weight: 481.015.
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