1001600-56-1

Basic information

• Product Name: BV6
• Synonyms: BV6;N,N'-(hexane-1,6-diyl)bis(1-{(2S)-2-cyclohexyl-2-[(N-methyl-L-alanyl)amino]acetyl}-L-prolyl-beta-phenyl-L-phenylalaninamide):trifluoroacetic acid(1:x);4,4'-(1,6-Hexanediyl)bis[N-methyl-L-alanyl-(2S)-2-cyclohexylglycyl-L-prolyl-beta-phenyl-L-phenylalaninamide
• CAS NO: 1001600-56-1
• Molecular Formula: C₇₀H₉₆N₁₀O₈
• Molecular Weight: 1205.57344
• Product Categories: Inhibitors
• Mol File: 1001600-56-1.mol
• Article Data: 1

Chemical Properties

• Boiling Point: 1376.7±65.0 °C(Predicted)
• Appearance: /
• Density: 1.177±0.06 g/cm3(Predicted)
• Storage Temp.: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
• Solubility: ≥60.28 mg/mL in DMSO; insoluble in H2O; ≥12.6 mg/mL in EtOH with ultrasonic
• PKA: 12.89±0.20(Predicted)
• CAS DataBase Reference: BV6(CAS DataBase Reference)
• NIST Chemistry Reference: BV6(1001600-56-1)
• EPA Substance Registry System: BV6(1001600-56-1)

Safety Data

• Hazardous Substances Data: 1001600-56-1(Hazardous Substances Data)

Usage

Description

BV6 is a bivalent Smac mimetic and an antagonist of the inhibitor of apoptosis (IAP) proteins that binds to IAP1 and XIAP (Kds = 0.46 and 1.3 nM, respectively). It induces autoubiquitination and proteasomal degradation of IAP1 and XIAP in MDA-MB-231 cells when used at a concentration of 5 μM. BV6 (4 μM) induces NF-κB activation and TNF-dependent apoptosis in A2058 and MDA-MB-231 cells. It enhances radiosensitization and increases apoptosis in HCC193 and H460 non-small cell lung cancer (NSCLC) cell lines. BV6 (1 μM) induces cell death in a panel of 40 primary, patient-derived B cell precursor acute lymphoblastic leukemia (BCP-ALL) samples in a TNF-dependent manner. In vivo, BV6 (10 mg/kg) increases survival and the time to relapse in a high-risk BCP-ALL patient-derived xenograft (PDX) mouse model.

Uses

BV-6 is a SMAC mimetic and inhibitor of apoptosis (IAP) inhibitor. Apoptosis agent.

Relevant articles and documents

INHIBITORS OF IAP

The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds having the general formula U1 - M - U2 wherein M is a linking group covalently joining R2, R3, R4 or R5 of U1 to an R2, R3, R4 or R5 group of U2; U1 and U2 have the general formula (I) and G, X1, X2, R2, R3, R3', R4, R4' and R5, are as described herein.