BM-1197

BM-1197 is a potent and selective inhibitor of dual Bcl-2/Bcl-xL, with IC50s of 3.5 nM and 5.2 nM for Bcl-2 and Bcl-xL, respectively. BM-1197 exhibits antitumor effects both in vitro and in vivo.

Product information

CAS Number: 1391107-89-3

Molecular Weight: 1131.78

Formula: C53H59ClF4N6O7S4

Chemical Name: N-[4-(4-{3-[2-(4-chlorophenyl)-4-methanesulfonyl-5-methyl-1-(propan-2-yl)-1H-pyrrol-3-yl]-5-fluorophenyl}piperazin-1-yl)phenyl]-4-{[(2R)-4-(4-hydroxypiperidin-1-yl)-1-(phenylsulfanyl)butan-2-yl]amino}-3-trifluoromethanesulfonylbenzene-1-sulfonamide

Smiles: CS(=O)(=O)C1C(=C(C2C=CC(Cl)=CC=2)N(C(C)C)C=1C)C1=CC(F)=CC(=C1)N1CCN(CC1)C1C=CC(=CC=1)NS(=O)(=O)C1=CC(=C(C=C1)N[C@@H](CSC1C=CC=CC=1)CCN1CCC(O)CC1)S(=O)(=O)C(F)(F)F

InChiKey: DMKVQMFONHHNMZ-HUESYALOSA-N

InChi: InChI=1S/C53H59ClF4N6O7S4/c1-35(2)64-36(3)52(73(4,66)67)50(51(64)37-10-12-39(54)13-11-37)38-30-40(55)32-44(31-38)63-28-26-62(27-29-63)43-16-14-41(15-17-43)60-75(70,71)47-18-19-48(49(33-47)74(68,69)53(56,57)58)59-42(34-72-46-8-6-5-7-9-46)20-23-61-24-21-45(65)22-25-61/h5-19,30-33,35,42,45,59-60,65H,20-29,34H2,1-4H3/t42-/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

How to use

In Vitro:

BM-1197 (2-2000 nM; 3 d) has marginal cytotoxicity against wild-type mouse embryonic fibroblast (MEF) cells but exerts potent growth-inhibitory activity in the MCL1−/− cells. BM-1197 shows potent growth-inhibitory activities in 7 small cell lung cancer (SCLC) cell lines with IC50s <100 nM, moderate activity in 3 SCLC cell lines with IC50s of ∼600 nM and weak activity in 2 SCLC cell lines with IC50s >2000 nM. BM-1197 (100 nM; 16 h) potently induces apoptosis in H146 cells. BM-1197 (100 nM; 2 h) disrupts the association between Bcl-xl and Puma or Bim in H146 cells. BM-1197 (100 nM; 0.5-2 h) induces Bax translocation, and it (3-30 nM; 2 h) induces cytochrome c release in H146 cells.

In Vivo:

BM-1197 (10 mg/kg; i.v. daily 5 days per week for 2 weeks) results in rapid and complete tumor regression in all 8 mice in H146 and H1963 tumor model. BM-1197 (15 mg/kg; i.v.) causes thrombocytopenia in mice but the effect is reversible even at highly efficacious doses. BM-1197 (10 mg/kg; i.v. qd) exerts a strong anti-tumor effect and is well tolerated in OCI-Ly8 xenograft models.

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