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Bortezomib is a potent, reversible and selective 20S proteasome inhibitor with a Ki of 0.6 nM. It is an antineoplastic agent that is used in treatment of refractory multiple myeloma and certain lymphomas. Synonyms: PS-341; PS 341; PS341; LDP 341; LDP-341; LDP341; MLN341; MLN-341; MLN 341; B-[(1R)-3-Methyl-1-[[(2S)-1-oxo-3-phenyl-2-[(2-pyrazinylcarbonyl)amino]propyl]amino]butyl]boronic Acid; Velcade; ((R)-3-Methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxamido)propanamido)butyl)boronic acid; N-[(1R)-1-(Dihydroxyboryl)-3-methylbutyl]-Nα-(2-pyrazinylcarbonyl)-L-phenylalaninamide. Grade: >98%. CAS No. 179324-69-7. Molecular formula: C19H25BN4O4. Mole weight: 384.24.
Bortezomib
Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome ( K i =0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Anti-cancer activity [1] [2]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: PS-341; LDP-341; NSC 681239. CAS No. 179324-69-7. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg; 200 mg. Product ID: HY-10227.
Bortezomib-d15
Bortezomib, sold under the brand name Velcade among others, is an anti-cancer medication used to treat multiple myeloma and mantle cell lymphoma. Bortezomib is a dipeptide boronic acid derivative that reversibly inhibits the 20S proteasome with Ki of 0.6 nM. It binds the β5-subunit of the 20S proteasome and selectively inhibits chymotryptic activity. Bortezomib blocks the degradation of tumor-suppressing and proapoptotic proteins to induce cell cycle arrest and apoptosis in cancer cell lines. New studies show that bortezomib may potentially help recover from vincristine treatment in treating acute lymphoblastic leukemia, when replacing vincristine in the process. Synonyms: LDP-341-d5; MG-341-d5; PS-341-d5. Grade: ≥99% atom D. Molecular formula: C57H54D15B3N12O9. Mole weight: 1113.76.
Bortezomib-[d5]
Bortezomib-[d5] is the labelled analogue of Bortezomib. Bortezomib is a proteasome inhibitor with an antineoplastic activity used to treat relapsed multiple myeloma and mantle cell lymphoma. Synonyms: Bortezomib-d5; B-[(1R)-3-Methyl-1-[[(2S)-1-oxo-3-phenyl-2-[(2-pyrazinylcarbonyl)amino]propyl]amino]butyl]boronic Acid-d5; [(1R)-3-Methyl-1-[[(2S)-1-oxo-3-phenyl-2-[(pyrazinylcarbonyl)amino]propyl]amino]butyl]boronic Acid-d5; Velcade-d5; Radiciol-d5; NSC 681239-d5; DPBA-d5; PS 341-d5; Radiciol-d5; Velcade-d5. Grade: >95%. CAS No. 1133706-15-6. Molecular formula: C19H20D5BN4O4. Mole weight: 389.28.
Bortezomib is the first proteasome inhibitor to be approved b the US FDA for multiple myeloma, a blood cancer. A reversible inhibitor of the 26S proteasome-a barrel-shaped multiprotein particle found in the nucleus and cytosol of all eukaryotic cells. Group: Biochemicals. Alternative Names: Velcade-deuterated, [ (1R) -3-Methyl-1- [ [ (2S) -1-oxo-3-phenyl-2- [ (pyrazinylcarbonyl) amino] propyl] amino] butyl] -boronic Acid-deuterated. Grades: Highly Purified. Pack Sizes: 1mg. US Biological Life Sciences.
Bortezomib is the active ingredient in the drug sold under the trade name Velcade®. This drug has been approved in at least one country to treat multiple myeloma. It is a potent (Ki, 0.6nM), specific and reversible proteasome inhibitor. There is not any significant inhibitory activity against other enzymes or receptors. In a study with the National Cancer Institute's panel of 60 human cell lines, Bortezomib showed a mean IC50 of 7nM as tested by SRB analysis. Group: Biochemicals. Grades: Highly Purified. CAS No. 179324-69-7. Pack Sizes: 5mg, 10mg, 25mg, 50mg, 100mg. US Biological Life Sciences.
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Bortezomib Impurity 10
Bortezomib Impurity 10 is an impurity of bortezomib, a drug used in the biomedical industry for therapy purposes. Bortezomib is a potent anticancer drug mainly used in the therapy of multiple myeloma. Synonyms: 2-PyrazinecarboxaMide, N,N',N''-[2,4,6-boroxintriyltris[[(1R)-3-Methylbutylidene]iMino[(1S)-2-oxo-1-(phenylMethyl)-2,1-ethanediyl]]]tris-. Grade: > 95%. CAS No. 390800-88-1. Molecular formula: C57H69B3N12O9. Mole weight: 1098.69.
Bortezomib Impurity 12
Bortezomib Impurity 12 is an impurity of Bortezomib. Synonyms: (R)-Hydroperoxy Des(boric Acid) Bortezomib; N-((S)-1-(((R)-1-Hydroperoxy-3-methylbutyl)amino)-1-oxo-3-phenylpropan-2-yl)pyrazine-2-carboxamide; 2-PyrazinecarboxaMide, N-[(1S)-2-[[(1R)-1-hydroperoxy-3-Methylbutyl]aMino]-2-oxo-1-(phenylMethyl)ethyl]-. Grade: > 95%. CAS No. 886979-78-8. Molecular formula: C19H24N4O4. Mole weight: 372.43.
Bortezomib Impurity 13
Bortezomib Impurity 13 is an impurity of Bortezomib, a pharmaceutical agent primarily indicated in the therapy of multiple myeloma and mantle cell lymphoma. Synonyms: 2-PyrazinecarboxaMide, N-[(1S)-2-[[(1S)-1-hydroperoxy-3-Methylbutyl]aMino]-2-oxo-1-(phenylMethyl)ethyl]-; N-((S)-1-(((S)-1-hydroperoxy-3-Methylbutyl)aMino)-1-oxo-3-phenylpropan-2-yl)pyrazine-2-carboxaMide. Grade: > 95%. CAS No. 886979-81-3. Molecular formula: C19H24N4O4. Mole weight: 372.43.
Bortezomib Impurity 16
Bortezomib Impurity 16. Uses: For analytical and research use. Group: Impurity standards. Alternative Names: ((S)-3-methyl-1-((R)-3-phenyl-2-(pyrazine-2-carboxamido)propanamido)butyl)boronic acid. CAS No. 1132709-16-0. Molecular formula: C19H25BN4O4. Mole weight: 384.24. Catalog: APB1132709160.
Bortezomib Impurity 24
Bortezomib Impurity 24. Uses: For analytical and research use. Group: Impurity standards. CAS No. 1255646-95-7. Molecular formula: C17H18N2O3. Mole weight: 298.34. Catalog: APB1255646957.
Bortezomib Impurity 4
Bortezomib Impurity 4 is an impurity of Bortezomib. Synonyms: N(1-(3-Methylbutanamido) N(1-Des(boric Acid)) Bortezomib; (S)-N-(1-(3-Methylbutanamido)-1-oxo-3-phenylpropan-2-yl)pyrazine-2-carboxamide. Grade: > 95%. CAS No. 862894-96-0. Molecular formula: C19H22N4O3. Mole weight: 354.41.
Bortezomib Impurity 7
An impurity of Bortezomib. Bortezomib is a proteasome inhibitor primarily used in the treatment of multiple myeloma (MM) and mantle cell lymphoma (MCL). Synonyms: (R)-(3-Methyl-1-(pyrazine-2-carboxamido)butyl)boronic acid; Bortezomib Related Compound A. Grade: ≥95%. Molecular formula: C10H16BN3O3. Mole weight: 237.07.
Bortezomib Impurity 9
Bortezomib Impurity 9 is an impurity of Bortezomib and a tripeptide boronic acid proteasome inhibitor used as an antitumor agent. Synonyms: N-(2-Pyrazinylcarbonyl)-L-phenylalanyl-N-[(1R)-1-borono-3-methylbutyl]-L-phenylalaninamide ; ((R)-3-Methyl-1-((S)-3-phenyl-2-((S)-3-phenyl-2-(pyrazine-2-carboxamido)propanamido)propanamido)butyl)boronic Acid. Grade: > 95%. CAS No. 1194235-41-0. Molecular formula: C28H34BN5O5. Mole weight: 531.42.
Bortezomib Impurity B
Bortezomib Impurity B is used for the synthesis of Bortezomib. Synonyms: N-(2-pyrazinylcarbonyl)-L-phenylalanine; 3-Phenyl-2-[(pyrazine-2-carbonyl)amino]propionic Acid; (S)-3-Phenyl-2-(pyrazine-2-carbonylamino)propanoic Acid. Grade: 98% by HNMR. CAS No. 114457-94-2. Molecular formula: C14H13N3O3. Mole weight: 271.28.
Bortezomib Impurity F
Bortezomib Impurity F is used for the synthesis of Bortezomib. Synonyms: 3-Phenyl-2-[(pyrazine-2-carbonyl)-amino]-propionic Acid Methyl Ester; N-Pyrazinylcarbonyl-L-phenylalanine Methyl Ester; N-(2-Pyrazinylcarbonyl)-L-phenylalanine Methyl Ester. Grade: > 95%. CAS No. 73058-37-4. Molecular formula: C15H15N3O3. Mole weight: 285.31.
Bortezomib Impurity G
Bortezomib Impurity G is an impurity of the acclaimed drug Bortezomib, a drug tailored towards the affliction of multiple myeloma. Synonyms: (S)-Hydroxy Des(boric Acid) Bortezomib; N-[(1S)-2-[[(1S)-1-hydroxy-3-methylbutyl]amino]-2-oxo-1-(phenylmethyl)ethyl]-2-Pyrazinecarboxamide. Grade: > 95%. CAS No. 289472-81-7. Molecular formula: C19H24N4O3. Mole weight: 356.43.
Bortezomib Impurity G
Bortezomib Impurity G. Uses: For analytical and research use. Group: Impurity standards. Alternative Names: ((S)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxamido)propanamido)butyl)boronic acid. CAS No. 1132709-14-8. Molecular formula: C19H25BN4O4. Mole weight: 384.24. Catalog: APB1132709148.
Bortezomib Impurity H
Bortezomib Impurity H is an impurity of Bortezomib, a therapeutic agent for treating multiple myeloma and mantle cell lymphoma. Synonyms: (S)-N-(1-(isopentylaMino)-1-oxo-3-phenylpropan-2-yl)pyrazine-2-carboxaMide. Grade: > 95%. CAS No. 1446194-56-4. Molecular formula: C19H24N4O2. Mole weight: 340.43.
Bortezomib Impurity H
Bortezomib Impurity H. Uses: For analytical and research use. Group: Impurity standards. Alternative Names: ((R)-3-methyl-1-((R)-3-phenyl-2-(pyrazine-2-carboxamido)propanamido)butyl)boronic acid. CAS No. 1132709-15-9. Molecular formula: C19H25BN4O4. Mole weight: 384.24. Catalog: APB1132709159.
Bortezomib Impurity (R,R-Isomer)
Bortezomib Impurity (R,R-Isomer) is a diastereomer of Bortezomib. Synonyms: (1R,2R)-Bortezomib; B-[(1R)-3-Methyl-1-[[(2R)-1-oxo-3-phenyl-2-[(2-pyrazinylcarbonyl)amino]propyl]amino]butyl]boronic Acid; [(1R)-3-Methyl-1-[[(2R)-1-oxo-3-phenyl-2-[(pyrazinylcarbonyl)amino]propyl]amino]butyl]boronic Acid. Grade: 98% by HPLC. CAS No. 1132709-15-9. Molecular formula: C19H25BN4O4. Mole weight: 384.25.
Bortezomib Impurity (R,S-Isomer)
Bortezomib Impurity (R,S-Isomer) is a diastereomer of Bortezomib. Synonyms: (1S,2R)-Bortezomib; B-[(1S)-3-Methyl-1-[[(2R)-1-oxo-3-phenyl-2-[(2-pyrazinylcarbonyl)amino]propyl]amino]butyl]boronic Acid; N-(2-Pyrazinecarbonyl)-D-phenylalanine-D-leucine boronic anhydride. Grade: > 95%. CAS No. 1132709-16-0. Molecular formula: C19H25BN4O4. Mole weight: 384.25.
Bortezomib Liposome (PEGylated)
Bortezomib (BTZ) is a proteasome inhibitor used to treat various malignancies, including lung cancer, prostate cancer, colorectal cancer, breast cancer, etc. This product is a pre-formulated liposome encapsulating Bortezomib. It is only for research purposes. Group: Drug-loaded liposome. Categories: Niosomes, ethosomes, and transfersomes.
Bortezomib Pinanediol Ester
Bortezomib-pinanediol is a prodrug of Bortezomib and a proteasome inhibitor. Synonyms: N-((S)-1-(((R)-3-methyl-1-((3aS,4S,6S,7aR)-3a,5,5-trimethylhexahydro-4,6-methanobenzo[d][1,3,2]dioxaborol-2-yl)butyl)amino)-1-oxo-3-phenylpropan-2-yl)pyrazine-2-carboxamide; (1R)-(1S,2S,3R,5S)-Pinanediol-N-(N-pyrazinylphenylalaninoyl)-1-amino-3-methyl-butane-1-boronate; Bortezomib Pinanediol Impurity. Grade: 97+%. CAS No. 205393-22-2. Molecular formula: C29H39BN4O4. Mole weight: 518.46.
Bortezomib USP Impurity G
Bortezomib USP Impurity G is an isomer of Bortezomib. It has been demonstrated to inhibit serine proteases shown to lower cellular Aβ concentrations, associated with Alzheimer's or hypertension. Synonyms: (1S,2S)-Bortezomib; ((S)-3-Methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxamido)propanamido)butyl)boronic acid. Grade: 95%. CAS No. 1132709-14-8. Molecular formula: C19H25BN4O4. Mole weight: 384.243.
Bortezomib USP Related Compoud B
Bortezomib USP Related Compoud B is an impurity of the acclaimed drug Bortezomib, which is a drug tailored towards the affliction of multiple myeloma. Synonyms: Bortezomib Amide Impurity; N-[(1S)-2-Amino-2-oxo-1-(phenylmethyl)ethyl]-2-pyrazinecarboxamide; N-[(1S)-2-amino-2-oxo-1-(phenylmethyl)ethyl]pyrazinecarboxamide; (S)-N-(1-AMino-1-oxo-3-phenylpropan-2-yl)pyrazine-2-carboxamide. Grade: 98% by HPLC. CAS No. 289472-80-6. Molecular formula: C14H14N4O2. Mole weight: 270.29.
(1S)-3-Hydroxy Bortezomib is a metabolite of Bortezomib (B675700), the first proteasome inhibitor to be approved by the US FDA for multiple myeloma, a blood cancer. Bortezomib is a reversible inhibitor of the 26S proteasome-a barrel-shaped multiprotein particle found in the nucleus and cytosol of all eukaryotic cells. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 500ug, 5mg. Molecular Formula: C19H25BN4O5, Molecular Weight: 400.24. US Biological Life Sciences.
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(1S)-3-Hydroxy Bortezomib-d8
(1S)-3-Hydroxy Bortezomib-d8 is labelled (1S)-3-Hydroxy Bortezomib (H818155) which is a metabolite of Bortezomib (B675700), the first proteasome inhibitor to be approved by the US FDA for multiple myeloma, a blood cancer. Bortezomib is a reversible inhibitor of the 26S proteasome-a barrel-shaped multiprotein particle found in the nucleus and cytosol of all eukaryotic cells. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 1mg, 10mg. Molecular Formula: C19H17D8BN4O5, Molecular Weight: 408.29. US Biological Life Sciences.
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2-[(2-Pyrazinylcarbonyl)-Bortezomib
2-[(2-Pyrazinylcarbonyl)-Bortezomib is a derivative of Bortezomib (B675700) which is the first proteasome inhibitor to be approved by the US FDA for multiple myeloma, a blood cancer. Bortezomib is a reversible inhibitor of the 26S proteasome-a barrel-shaped multiprotein particle found in the nucleus and cytosol of all eukaryotic cells. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 1mg, 5mg. Molecular Formula: C24H27BN6O5, Molecular Weight: 490.32. US Biological Life Sciences.
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Desisobutyl-n-pentyl Bortezomib
Desisobutyl-n-pentyl Bortezomib is an impurity of Bortezomib (B675700), a dipeptidyl boronate proteasome inhibitor. Group: Biochemicals. Alternative Names: ( (R) -1- ( (S) -3-Phenyl-2- (pyrazine-2-carboxamido) propanamido) hexyl) boronic Acid. Grades: Highly Purified. Pack Sizes: 10mg. US Biological Life Sciences.
N(1-(3-Methylbutanamido) N(1-Des(boric Acid)) Bortezomib is an impurity of Bortezomib (B675700), the first proteasome inhibitor to be approved by the US FDA for multiple myeloma, a blood cancer. Group: Biochemicals. Grades: Highly Purified. CAS No. 862894-96-0. Pack Sizes: 10mg, 100mg. Molecular Formula: C19H22N4O3, Molecular Weight: 354.4. US Biological Life Sciences.
Isotope labelled N(1-(3-Methylbutanamido) N(1-Des(boric Acid)) Bortezomib is an impurity of Bortezomib (B675700), the first proteasome inhibitor to be approved by the US FDA for multiple myeloma, a blood cancer. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 1mg, 10mg. Molecular Formula: C19H13D9N4O3, Molecular Weight: 363.49. US Biological Life Sciences.
(R)-Hydroxy Des(boric Acid) Bortezomib. Uses: For analytical and research use. Group: Impurity standards. CAS No. 289472-78-2. Pack Sizes: 2.5MG. IUPAC Name: N-[(2S)-1-[[(1R)-1-hydroxy-3-methylbutyl]amino]-1-oxo-3-phenylpropan-2-yl]pyrazine-2-carboxamide. Molecular formula: C19H24N4O3. Mole weight: 356.42. Catalog: APS289472782. SMILES: CC(C)C[C@@H](O)NC(=O)[C@H](Cc1ccccc1)NC(=O)c2cnccn2. Format: Neat. Shipping: Room Temperature.
(R,R)-Hydroxy Des(boric Acid) Bortezomib
(R,R)-Hydroxy Des(boric Acid) Bortezomib. Group: Biochemicals. Alternative Names: N-((R)-1-(((R)-1-Hydroxy-3-methylbutyl)amino)-1-oxo-3-phenylpropan-2-yl)pyrazine-2-carboxamide. Grades: Highly Purified. Pack Sizes: 2.5mg. US Biological Life Sciences.
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(S)-Hydroxy Des(boric Acid) Bortezomib
(S)-Hydroxy Des(boric Acid) Bortezomib. Group: Biochemicals. Alternative Names: N-[(1S)-2-[[(1S)-1-hydroxy-3-methylbutyl]amino]-2-oxo-1-(phenylmethyl)ethyl]-2-Pyrazinecarboxamide; N-[(1S)-2-[[(1S)-1-hydroxy-3-methylbutyl]amino]-2-oxo-1-(phenylmethyl)ethyl]-pyrazinecarboxamide. Grades: Highly Purified. CAS No. 289472-81-7. Pack Sizes: 500ug. Molecular Formula: C19H24N4O3, Molecular Weight: 356.42. US Biological Life Sciences.
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(S)-Hydroxy-O-ethyl Des(boric Acid) Bortezomib
(S)-Hydroxy-O-ethyl Des(boric Acid) Bortezomib is an intermediate in the synthesis of (S)-Hydroperoxy Des(boric Acid) Bortezomib (H715405), which is an impurity of Bortezomib (B675700), the first proteasome inhibitor to be approved by the US FDA for multiple myeloma, a blood cancer. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 5mg, 10mg. Molecular Formula: C21H28N4O3. US Biological Life Sciences.
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(S,R)-Bortezomib Hydroxyisopentyl Amide Analog
(S,R)-Bortezomib Hydroxyisopentyl Amide Analog is an isomer of Bortezomib. It has been demonstrated to inhibit serine proteases shown to lower cellular Aβ concentrations, associated with Alzheimer's or hypertension. Synonyms: N-((S)-1-(((R)-1-Hydroxy-3-methylbutyl)amino)-1-oxo-3-phenylpropan-2-yl)pyrazine-2-carboxamide; (R)-Hydroxy Des(boric Acid) Bortezomib; Bortezomib Hydroxy Impurity (1R,2S)-Isomer. Grade: 98% by HPLC. CAS No. 289472-78-2. Molecular formula: C19H24N4O3. Mole weight: 356.43.
A cell-permeable flavone derivative that arrests the proliferation of acute myeloid leukemia cells (NB4, U937, HL-60, OCI AML3), in a dose and time-dependent manner (optimum at ~20uM and 96h) and blocks the colony formation in samples from acute myeloid leukemia patients, without affecting normal blood cells. Shown to reduce mitochondrial membrane potential and Bad phosphorylation (at Ser136), induce Bax and caspase 3, 8, and 9 activation in U937 cells. Does not affect the phosphorylation of Akt1, but significantly reduces the expression and phosphorylation of p70S6 kinase in U937 cells. Reported to inhibit the chymotrypsin-like activity of proteasome (IC50 = 2.0uM) and this effect is synergistic with bortezomib. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. US Biological Life Sciences.
(3aS,4S,6S,7aR)-2-Butylhexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborole is an intermediate in the preparation of Bortezomib (B675700), a dipeptidyl boronate proteasome inhibitor. Group: Biochemicals. Alternative Names: [3aS-(3aα,4 β,6 β,7aα)]-2-Butylhexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborole. Grades: Highly Purified. CAS No. 85167-10-8. Pack Sizes: 1g. US Biological Life Sciences.
(3aS,4S,6S,7aR)-Hexahydro-3a,5,5-trimethyl-2-pentyl-4,6-methano-1,3,2-benzodioxaborole is an intermediate in the preparation of Bortezomib (B675700), a dipeptidyl boronate proteasome inhibitor. Group: Biochemicals. Grades: Highly Purified. CAS No. 476335-09-8. Pack Sizes: 1g. US Biological Life Sciences.
Bortezomib intermediate. A boronic acid dipeptide derivative as proteasome inhibitors. Group: Biochemicals. Grades: Highly Purified. CAS No. 179324-87-9. Pack Sizes: 25mg. US Biological Life Sciences.
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AZD5991
AZD5991 is a potent and selective Mcl-1 inhibitor with an IC50 of <3 nM in FRET assay for treatment of hematologic cancers. AZD5991 has high selectivity and affinity for Mcl-1 and is currently in clinical development. AZD5991 shows potent antitumor activity in vivo with complete tumor regression in several models of multiple myeloma and acute myeloid leukemia after a single tolerated dose as monotherapy or in combination with bortezomib or venetoclax. AZD5991 monotherapy caused apoptosis preferentially in hematological cell lines with 6/22 AML and 7/19 MM cell lines showing caspase EC50 values <100 nM. In solid tumor cell lines single agent activity was seen mostly in NSCLC and BrCa. Uses: Antineoplastic agents. Synonyms: AZD-5991; AZD 5991; AZD-5991 Racemate; 22H-9,4,8-(Metheniminomethyno)-14,20:26,23-dimetheno-10H,20H-pyrazolo[4,3-l][2,15,22,18,19]benzoxadithiadiazacyclohexacosine-32-carboxylic acid, 5-chloro-2,11,12,24,27,29-hexahydro-2,3,24,33-tetramethyl-. Grade: ≥98%. CAS No. 2143010-83-5. Molecular formula: C35H34ClN5O3S2. Mole weight: 672.26.
CCF-642
CCF-642 is a protein disulfide isomerase (PDI) inhibitor that exhibits 100-fold higher potency than PACMA 31 (by di-E-GSSG assay) via an alternative mode of action. CCF642 displayed potent efficacy in an aggressive syngeneic mouse model of multiple myeloma and prolonged the lifespan of C57BL/KaLwRij mice engrafted with 5TGM1-luc myeloma, an effect comparable to the first-line multiple myeloma therapeutic bortezomib. Synonyms: 3-(4-Methoxyphenyl)-5-[(5-nitro-2-thienyl)methylene]-2-thioxo-4-thiazolidinone; CCF-642; CCF 642; CCF642. CAS No. 346640-08-2. Molecular formula: C15H10N2O4S3. Mole weight: 378.44.
CEP-7055
CEP-18770 is An orally bioavailable synthetic P2 threonine boronic acid inhibitor of the chymotrypsin-like activity of the proteasome, with potential antineoplastic activity. Proteasome inhibitor CEP 18770 represses the proteasomal degradation of a variety of proteins, including inhibitory kappaBalpha (IkappaBalpha), resulting in the cytoplasmic sequestration of the transcription factor NF-kappaB; inhibition of NF-kappaB nuclear translocation and transcriptional up-regulation of a variety of cell growth-promoting factors; and apoptotic cell death in susceptible tumor cell populations. In vitro studies indicate that this agent exhibits a favorable cytotoxicity profile toward normal human epithelial cells, bone marrow progenitors, and bone marrow-derived stromal cells relative to the proteasome inhibitor bortezomib. The intracellular protein IkappaBalpha functions as a primary inhibitor of the proinflammatory transcription factor NF-kappaB. Synonyms: CEP 7055; CEP7055; 3-(9-isopropoxymethyl-5-oxo-6,7,12,13-tetrahydro-5H-indeno[2,1-a]pyrrolo[4,3-c]carbazol-12-yl)propyl 2-dimethylaminoacetate. CAS No. 402857-58-3. Molecular formula: C32H35N3O4. Mole weight: 525.65.
Delanzomib
Delanzomib, also known as CEP-18770, is An orally bioavailable synthetic P2 threonine boronic acid inhibitor of the chymotrypsin-like activity of the proteasome, with potential antineoplastic activity. Proteasome inhibitor CEP 18770 represses the proteasomal degradation of a variety of proteins, including inhibitory kappaBalpha (IkappaBalpha), resulting in the cytoplasmic sequestration of the transcription factor NF-kappaB; inhibition of NF-kappaB nuclear translocation and transcriptional up-regulation of a variety of cell growth-promoting factors; and apoptotic cell death in susceptible tumor cell populations. In vitro studies indicate that this agent exhibits a favorable cytotoxicity profile toward normal human epithelial cells, bone marrow progenitors, and bone marrow-derived stromal cells relative to the proteasome inhibitor bortezomib. The intracellular protein IkappaBalpha functions as a primary inhibitor of the proinflammatory transcription factor NF-kappaB. Uses: Proteasome inhibitors. Synonyms: CEP18770; CEP 18770; CEP-18770; Delanzomib. CAS No. 847499-27-8. Molecular formula: C21H28BN3O5. Mole weight: 413.27.
Doramapimod
Doramapimod is a highly potent inhibitor of p38 mitogen-activated protein kinase (MAPK). Doramapimod is a potential agent for the treatment of inflammatory diseases. Doramapimod blocks baseline and bortezomib-triggered upregulation of p38 MAPK and Hsp27 phosphorylation leading to enhanced cytotoxicity and caspase activation. Group: Biochemicals. Alternative Names: N-[3-(1,1-Dimethylethyl)-1-(4-methylphenyl)-1H-pyrazol-5-yl]-N'-[4-[2-(4-morpholinyl)ethoxy]-1-naphthalenyl]urea; BIRB 796BS; Birb 796. Grades: Highly Purified. CAS No. 285983-48-4. Pack Sizes: 10mg. US Biological Life Sciences.
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N-Pyrazinylcarbonyl-L-phenylalanine methyl ester
Used for the synthesis of Bortezomib from L-phenylalanine via dipeptidyl boronic acid ester intermediates. Group: Biochemicals. Alternative Names: N-(2-Pyrazinylcarbonyl)-L-phenylalanine Methyl Ester; 3-Phenyl-2-[ (pyrazine-2-carbonyl) amino]propionic Acid Methyl Ester. Grades: Highly Purified. CAS No. 73058-37-4. Pack Sizes: 100mg, 250mg, 500mg, 1g. Molecular Formula: C??H??N?O?, Molecular Weight: 285.3. US Biological Life Sciences.
Worldwide
N-Pyrazinylcarbonyl-L-phenylalanine Methyl Ester
N-Pyrazinylcarbonyl-L-phenylalanine Methyl Ester. Uses: Designed for use in research and industrial production. Additional or Alternative Names: Bortezomib Impurity R. Appearance: White Powder. CAS No. 73058-37-4. Molecular formula: C15H15N3O3. Mole weight: 285.29. Purity: 0.95. Product ID: ACM73058374. Alfa Chemistry ISO 9001:2015 Certified. Categories: DTXSID90503277.
Suvecaltamide
Suvecaltamide (MK-8998) is a selective T-type calcium channel inhibitor with oral efficacy. Suvecaltamide exhibits no cytotoxicity in myeloma cell lines and does not affect the antitumor efficacy of Bortezomib (BTZ). Suvecaltamide reverses BTZ-induced peripheral neuropathy (CIPN) in mouse and rat models, and helps inhibit myeloma growth [1]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: MK-8998; CX-8998; JZP385. CAS No. 953778-58-0. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-101096.
Tipifarnib
A farnesyltransferase inhibitor. Sensitizes human multiple myeloma cell to proteasome inhibition by blocking degradation of bortezomib-induced aggresomes. Also shown to inhibit the growth of myeloid leukemia cell lines and primary leukemia cells by inducing apoptosis and cell-cycle blockage when combined with rapamycin(R124000). Group: Biochemicals. Alternative Names: 6-[(R)-Amino(4-chlorophenyl)(1-methyl-1H-imidazol-5-yl)methyl]-4-(3-chlorophenyl)-1-methyl-2(1H)-quinolinone; (R)-(+)-R 115777; Zarnestra. Grades: Highly Purified. CAS No. 192185-72-1. Pack Sizes: 2.5mg. US Biological Life Sciences.
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