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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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A127419-5mg | 5mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $81.90 | |
A127419-25mg | 25mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $369.90 | |
A127419-100mg | 100mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $576.90 |
BH3 mimetic Bcl-xL, Bcl-2 and Bcl-w inhibitor
Synonyms | ABT-737 | 852808-04-9 | ABT 737 | ABT737 | UNII-Z5NFR173NV | 4-[4-[(4'-Chloro[1,1'-biphenyl]-2-yl)methyl]-1-piperazinyl]-N-[[4-[[(1R)-3-(dimethylamino)-1-[(phenylthio)methyl]propyl]amino]-3-nitrophenyl]sulfonyl]benzamide | Z5NFR173NV | (R)-4-(4-((4'-chloro-[1,1'-biphen |
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Specifications & Purity | Moligand™, ≥97% |
Biochemical and Physiological Mechanisms | ABT-737 is a pan-Bcl-2 inhibitor that has a wide range of single-agent activity against acute lymphoblastic leukemia (ALL) cell lines and xenografts. Increased expression of the Bcl-2 family of proteins in cancers has been associated with chemotherapy res |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | ANTAGONIST |
Mechanism of action | Antagonist of BCL2 apoptosis regulator;Antagonist of Bcl-2-like 1;Antagonist of Bcl-2-like 2 |
Note | Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details. |
Product Description | ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM in cell-free assays, respectively; no inhibition observed against Mcl-1, Bcl-B or Bfl-1. |
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IUPAC Name | 4-[4-[[2-(4-chlorophenyl)phenyl]methyl]piperazin-1-yl]-N-[4-[[(2R)-4-(dimethylamino)-1-phenylsulfanylbutan-2-yl]amino]-3-nitrophenyl]sulfonylbenzamide |
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INCHI | InChI=1S/C42H45ClN6O5S2/c1-46(2)23-22-35(30-55-37-9-4-3-5-10-37)44-40-21-20-38(28-41(40)49(51)52)56(53,54)45-42(50)32-14-18-36(19-15-32)48-26-24-47(25-27-48)29-33-8-6-7-11-39(33)31-12-16-34(43)17-13-31/h3-21,28,35,44H,22-27,29-30H2,1-2H3,(H,45,50)/t35-/m1/s1 |
InChi Key | HPLNQCPCUACXLM-PGUFJCEWSA-N |
Canonical SMILES | CN(C)CCC(CSC1=CC=CC=C1)NC2=C(C=C(C=C2)S(=O)(=O)NC(=O)C3=CC=C(C=C3)N4CCN(CC4)CC5=CC=CC=C5C6=CC=C(C=C6)Cl)[N+](=O)[O-] |
Isomeric SMILES | CN(C)CC[C@H](CSC1=CC=CC=C1)NC2=C(C=C(C=C2)S(=O)(=O)NC(=O)C3=CC=C(C=C3)N4CCN(CC4)CC5=CC=CC=C5C6=CC=C(C=C6)Cl)[N+](=O)[O-] |
PubChem CID | 11228183 |
Molecular Weight | 813.43 |
CAS Registry No. | 852808-04-9 |
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PubChem CID | 11228183 |
ChEMBL Ligand | CHEMBL376408 |
RCSB PDB Ligand | N3C |
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Solubility | DMSO ≥160mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL |
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Refractive Index | 1.7 |
Melt Point(°C) | 148-151°C |
1. Amundson SA, Myers TG, Scudiero D, Kitada S, Reed JC, Fornace Jr AJ. (2000) An informatics approach identifying markers of chemosensitivity in human cancer cell lines.. Cancer Res, 60 (21): (6101-10). [PMID:11085534] |
2. Green DR, Evan GI. (2002) A matter of life and death.. Cancer Cell, 1 (1): (19-30). [PMID:12086884] |
3. Witham J, Valenti MR, De-Haven-Brandon AK, Vidot S, Eccles SA, Kaye SB, Richardson A. (2007) The Bcl-2/Bcl-XL family inhibitor ABT-737 sensitizes ovarian cancer cells to carboplatin.. Clin Cancer Res, 13 (23): (7191-8). [PMID:18056200] |
4. Bruncko M, Oost TK, Belli BA, Ding H, Joseph MK, Kunzer A, Martineau D, McClellan WJ, Mitten M, Ng SC et al.. (2007) Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL.. J Med Chem, 50 (4): (641-62). [PMID:17256834] |
5. Jain HV, Meyer-Hermann M. (2011) The molecular basis of synergism between carboplatin and ABT-737 therapy targeting ovarian carcinomas.. Cancer Res, 71 (3): (705-15). [PMID:21169413] |
6. Tian BP, Xia LX, Bao ZQ, Zhang H, Xu ZW, Mao YY, Cao C, Che LQ, Liu JK, Li W et al.. (2017) Bcl-2 inhibitors reduce steroid-insensitive airway inflammation.. J Allergy Clin Immunol, 140 (2): (418-430). [PMID:28043871] |
7. Lheureux S, N'Diaye M, Blanc-Fournier C, Dugué AE, Clarisse B, Dutoit S, Giffard F, Abeilard E, Briand M, Labiche A et al.. (2015) Identification of predictive factors of response to the BH3-mimetic molecule ABT-737: an ex vivo experiment in human serous ovarian carcinoma.. Int J Cancer, 136 (5): (E340-50). [PMID:25066666] |