BM-1074 is a potent and highly efficacious inhibitor of Bcl-2/Bcl-xL with Ki value of < 1nM . BM-1074 is a selective Bcl-2 and Bcl-xL inhibitor. It shows high binding affinity to both Bcl-2 and Bcl-xL. In H146 cell line, BM-1074 inhibits the cell growth with IC50 value of 1.3nM. It is found that 15 mg/kg dosed intravenously is the maximum tolerated dose (MTD) of BM-1074. BM-1074 at MTD induces cleavage of PARP and caspase-3 in H146 xenograft tumors in SCID mice, indicating a strong apoptosis induction in vivo. BM-1074 also shows rapid, complete and persistent antitumor efficacy in the H-146 xenograft model. Moreover, mice treated with BM-1074 shows no significant weight loss or other toxicity signs. In addition, BM-1074 inhibits cell growth in three other small-cell lung cancer cell lines, including H1963, H187 and H1417, with IC50 values of 1nM, 1.4nM and 2.3nM, respectively .

Product information

CAS Number: 1391108-10-3

Molecular Weight: 1013.68

Formula: C50H57ClN8O7S3

Chemical Name: (Z)-5-(4-chlorophenyl)-4-(3-{4-[4-(4-{[(2R)-4-(dimethylamino)-1-(phenylsulfanyl)butan-2-yl]amino}-3-nitrobenzenesulfonamido)phenyl]piperazin-1-yl}phenyl)-N-methanesulfonyl-2-methyl-1-(propan-2-yl)-1H-pyrrole-3-carboximidic acid

Smiles: CS(=O)(=O)/N=C(\O)/C1C(=C(C2C=CC(Cl)=CC=2)N(C(C)C)C=1C)C1=CC(=CC=C1)N1CCN(CC1)C1C=CC(=CC=1)NS(=O)(=O)C1=CC(=C(C=C1)N[C@@H](CSC1C=CC=CC=1)CCN(C)C)N(=O)=O

InChiKey: GISBATIMZJHKJK-RRHRGVEJSA-N

InChi: InChI=1S/C50H57ClN8O7S3/c1-34(2)58-35(3)47(50(60)54-68(6,63)64)48(49(58)36-15-17-38(51)18-16-36)37-11-10-12-42(31-37)57-29-27-56(28-30-57)41-21-19-39(20-22-41)53-69(65,66)44-23-24-45(46(32-44)59(61)62)52-40(25-26-55(4)5)33-67-43-13-8-7-9-14-43/h7-24,31-32,34,40,52-53H,25-30,33H2,1-6H3,(H,54,60)/t40-/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

Products are for research use only. Not for human use.