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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-. Grades: > 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]-. Grades: > 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. Grades: > 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 2 (SR-Isomer, Bortezomib Impurity E) is an impurity in the synthesis of Bortezomib. Grades: 98% by HPLC. CAS No. 289472-78-2. Molecular formula: C19H24N4O3. Mole weight: 356.43.
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. Grades: > 95%. CAS No. 862894-96-0. Molecular formula: C19H22N4O3. Mole weight: 354.41.
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. Grades: > 95%. CAS No. 1194235-41-0. Molecular formula: C28H34BN5O5. Mole weight: 531.42.
Bortezomib Impurity A
Bortezomib Impurity A is a metabolite of Bortezomib. Synonyms: 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; 2-PyrazinecarboxaMide, N-[(1S)-2-aMino-2-oxo-1-(phenylMethyl. Grades: 98% by HPLC. CAS No. 289472-80-6. Molecular formula: C14H14N4O2. Mole weight: 270.29.
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. Grades: 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. Grades: > 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. Grades: > 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. Grades: > 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. Grades: 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. Grades: > 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 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. Grades: 95%. CAS No. 1132709-14-8. Molecular formula: C19H25BN4O4. Mole weight: 384.243.
(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.
Worldwide
(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.
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-. Grades: ≥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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INCB16562
INCB16562 is a novel, selective, and orally bioavailable small-molecule inhibitor of JAK1 and JAK2 markedly selective over JAK3. Treatment of myeloma cells with INCB16562 potently inhibited interleukin-6 (IL-6)-induced phosphorylation of STAT3. INCB16562 abrogated the protective effects of recombinant cytokines or bone marrow stromal cells and sensitized myeloma cells to cell death by exposure to dexamethasone, melphalan, or bortezomib. Oral administration of INCB16562 antagonized the growth of myeloma xenografts in mice and enhanced the antitumor activity of relevant agents in combination studies. INCB16562 is a potent JAK1/2 inhibitor and that mitigation of JAK/STAT signaling by targeting JAK1 and JAK2 will be beneficial in the treatment of myeloma patients, particularly in combination with other agents. Synonyms: INCB-16562; INCB 16562; 2-(2,6-dichlorophenyl)-1,8-dihydroimidazo[4,5-d]dipyrido[2,3-b:4',3'-f]azepine. CAS No. 933768-63-9. Molecular formula: C19H11Cl2N5. Mole weight: 380.23.
Ixazomib
Ixazomib is a proteasome inhibitor and the biologically active form of MLN9708. Ixazomib exhibits an improved pharmacodynamic profile and antitumor activity compared with bortezomib in both OCI-Ly10 and PHTX22L models. Although both Ixazomib and bortezomib prolonged overall survival, reduced splenomegaly, and attenuated IgG2a levels in the iMyc(Cα)/Bcl-X(L) GEM model, only Ixazomib alleviated osteolytic bone disease in the DP54-Luc model. Synonyms: MLN2238; MLN-2238; MLN 2238; Ixazomib. Trade name: Ninlaro. (R)-(1-(2-(2,5-dichlorobenzamido)acetamido)-3-methylbutyl)boronic acid. Grades: > 95%. CAS No. 1072833-77-2. Molecular formula: C14H19BCl2N2O4. Mole weight: 361.026.
K-7174
K-7174 is a novel orally active, potent proteasome inhibitor. K-7174 exerts anti-myeloma activity in vitro and in vivo by down-regulating the expression of class I histone deacetylases. K-7174 kills bortezomib-resistant myeloma cells carrying a β5-subunit mutation in vivo and primary cells from a patient resistant to bortezomib. K-7174 is also a GATA-specific inhibitor, which may have potential application in treating anemia of chronic disease. Synonyms: K-7174; K 7174; K7174. Grades: 0.98. CAS No. 191089-59-5. Molecular formula: C33H48N2O6. Mole weight: 568.74.
K-7174 dihydrochloride
K-7174, one of proteasome inhibitory homopiperazine derivatives, exhibits a therapeutic effect, which is stronger when administered orally than intravenously, without obvious side effects in a murine myeloma model. Moreover, K-7174 kills bortezomib-resistant myeloma cells carrying a β5-subunit mutation in vivo and primary cells from a patient resistant to bortezomib. Synonyms: 1,4-bis((E)-5-(3,4,5-trimethoxyphenyl)pent-4-en-1-yl)-1,4-diazepane dihydrochloride; K7174; K 7174; K-7174; K-7174-2HCl; K-7174 dihydrochloride. Grades: >98%. CAS No. 191089-60-8. Molecular formula: C33H50Cl2N2O6. Mole weight: 641.67.
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 (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.
TAS-116
TAS-116 is a inhibitor of Hsp90. It induces significant cytotoxicity in MM cells even in the presence of BMSCs, associates with downregulation of phospho-Akt and phospho-ERK. In addition, neither exogenous IL-6 nor IGF-1 was able to protect against TAS-116. Importantly, TAS-116 did not induce cytotoxicity in BMSCs. TAS-116 enhanced bortezomib-induced cytotoxicity in MM.1S and RPMI-8226 cells, associated with decreased phospho-Akt, phospho-RelA (p65), phospho-IkBa, and phospho-IKKα/β; as well as increased CHOP and PARP cleavage. These results suggest that TAS-116 blocks bortezomib-induced canonical NF-κB pathway and augments bortezomib-induced endoplasmic reticulum (ER) stress. Synonyms: TAS116; TAS 116; TAS-116; 3-Ethyl-4-[3-(1-methylethyl)-4-[4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl]-1H-pyrazolo[3,4-b]pyridin-1-yl]benzamide. Grades: >98%. CAS No. 1260533-36-5. Molecular formula: C25H26N8O. Mole weight: 454.54.
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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