ABT-199

SKU: orb1226663

Description

Venetoclax (ABT-199, GDC-0199) is a Bcl-2-selective inhibitor with Ki of 4800-fold more selective versus Bcl-xL and Bcl-w, and no activity to Mcl-1. Phase 3.(In Vitro):Venetoclax (ABT-199) potently kills FL5.12-BCL-2 cells (EC50=4 nM), Venetoclax (ABT-199) shows much weaker activity against FL5.12-BCL-XL cells (EC50=261 nM). ABT-199 also shows selectivity in cellular mammalian two-hybrid assays, where it disrupts BCL-2-BIM complexes (EC50=3 nM) but is much less effective against BCL-XL-BCL-XS (EC50=2.2 μM) or MCL-1-NOXA complexes.(In Vivo):After a single oral dose of 12.5 mg per kg body weight in xenografts derived from RS4;11 cells (ALL), Venetoclax (ABT-199) causes a maximal tumor growth inhibition (TGImax) of 47% (P<0.001) and tumor growth delay (TGD) of 26% (P<0.05).Treatment of established xenografted (a mouse xenograft model of the T-ALL cell line LOUCY) tumors with Venetoclax (ABT-199) 100 mg/kg for 4 days results in a significant reduction of leukemic burden.

Key Properties

• CAS Number: 1257044-40-8
• MW: 868.44
• Purity: >98% (HPLC)
• Formula: C₄₅H₅₀ClN₇O₇S
• SMILES: O=C(NS(=O)(C1=CC=C(NCC2CCOCC2)C([N+]([O-])=O)=C1)=O)C3=CC=C(N4CCN(CC5=C(C6=CC=C(Cl)C=C6)CC(C)(C)CC5)CC4)C=C3OC7=CN=C(NC=C8)C8=C7
• Target: Bcl-2
• Solubility: DMSO: 100 mg/mL warmed (115.14 mM)

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GDC-0199

Quick Database Links

Gene Symbol

Bcl-2