ABT-199 --- BCL-2 inhibitor

Overview
Catalog #	bs-60075c-2-mg-solid
Product Name	ABT-199 --- BCL-2 inhibitor
Specifications
Storage Buffer	Powder
Storage Condition	Store in dry, dark place at -20C for 1 year.
Target
Product Information	Molecular Weight: 868.44 Formula: C45 H50 Cl N7 O7 S CAS Number: 1257044-40-8 InChi Key: LQBVNQSMGBZMKD-UHFFFAOYSA-N InChi: InChI=1S/C45H50ClN7O7S/c1-45(2)15-11-33(39(26-45)31-3-5-34(46)6-4-31)29-51-17-19-52(20-18-51)35-7-9-38(42(24-35)60-36-23-32-12-16-47-43(32)49-28-36)44(54)50-61(57,58)37-8-10-40(41(25-37)53(55)56)48-27-30-13-21-59-22-14-30/h3-10,12,16,23-25,28,30,48H,11,13-15,17-22,26-27,29H2,1-2H3,(H,47,49)(H,50,54) Smiles: CC1(C)CC(C2C=CC(Cl)=CC=2)=C(CN2CCN(CC2)C2=CC(OC3C=C4C=CNC4=NC=3)=C(C=C2)C(=O)NS(=O)(=O)C2=CC(=C(C=C2)NCC2CCOCC2)[N+]([O-])=O)CC1 Purity: 98.0 Solubility: DMSO up to 50 mM Appearance: Solid Power. Shelf Life: 1.0 years
Description	ABT-199 is a highly potent, selective, and orally bioavailable BCL-2 inhibitor. ABT-199 has picomolar affinity for BCL-2 (Ki < 0.010 nM) and > 1000 folds selectivity over BCL-XL (Ki = 48 nM) and BCL-W (Ki = 245 nM). Therefore, ABT-199 is a much improved lead compound over the original ABT-263 (navitoclax) to avoid thrombocytopenia caused by BCL-XL inhibition. ABT-199’s cell-killing effect is selective and mechanism dependent. It can potently kill BCL-2-overexpressing FL5.12 cells (EC50 ~ 4 nM) and RS4;11 BCL-2–dependent ALL cells (EC50 ~8 nM), but showed much weaker activity against BCL-XL-overexpressing FL5.12 cells (EC50 ~261 nM) and H146 ALL cells (EC50 ~4, 260 nM). ABT-199 inhibits the growth of BCL-2–dependent human hematological tumors in vivo and spares human platelets as a single agent or in combination with rituximab and bendamustine. A single dose of ABT-199 in three patients with refractory chronic lymphocytic leukemia resulted in tumor lysis within 24 h. These data indicates that selective pharmacological inhibition of BCL-2 shows promise for the treatment of BCL-2–dependent hematological cancers.