OTX015 --- BET Inhibitor

Overview
Catalog #	bs-60193c-2-mg-solid
Product Name	OTX015 --- BET Inhibitor
Specifications
Storage Buffer	Powder
Storage Condition	Store in dry, dark place at -20C for 1 year.
Target
Product Information	Molecular Weight: 491.99 Formula: C25 H22 Cl N5 O2 S CAS Number: 202590-98-5 InChi Key: GNMUEVRJHCWKTO-FQEVSTJZSA-N InChi: InChI=1S/C25H22ClN5O2S/c1-13-14(2)34-25-22(13)23(16-4-6-17(26)7-5-16)28-20(24-30-29-15(3)31(24)25)12-21(33)27-18-8-10-19(32)11-9-18/h4-11,20,32H,12H2,1-3H3,(H,27,33)/t20-/m0/s1 Smiles: CC1=NN=C2[C@H](CC(=O)NC3C=CC(O)=CC=3)N=C(C3=C(SC(C)=C3C)N12)C1C=CC(Cl)=CC=1 Purity: 98.0 Solubility: DMSO up to 100 mM Appearance: Solid Power. Shelf Life: 1.0 years
Description	OTX015 is a novel, highly potent, selective and cell permeable inhibitor of the bromodomain and extra terminal (BET) family proteins BRD2, BRD3 and BRD4 with IC50 of 10-19 nM. It inhibits the growth of a variety of human cancer cell lines with IC50 ranging from 60 to 200 nM. OTX015 results in rapid down-regulation of c-MYC expression, and show the synergistic anti-proliferative effects in combination with ALK inhibitors in ALKpos ALCL cell lines. In vivo studies using OTX015 have demonstrated efficacy in a range of oncology models. OTX015 is currently in phase I clinical development for oncology indication.