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Background Information:
BCL-2 is overexpressed in several hematologic malignancies, acting as a key regulator of the intrinsic apoptotic pathway by neutralizing pro-apoptotic molecules and inhibiting apoptosis. ABT-199 is an orally bioavailable, second-generation BH3-mimetic that specifically and potently inhibits BCL-2 (Ki<0.10 nM), highly selective over BCL-xL (Ki=48 nM, a 500-fold selectivity). It is the first small molecule targeting BCL-xL with such selectivity and potency, and currently in clinical trials for cancer treatment.
Reference:
1. A. J. Souers, et al., ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets, Nature Medicine, 19(2), 202-8 (2013)
2. M. S. Davids, et al., ABT-199: Taking Dead Aim at BCL-2, Cancer Cell, Vol 23, Issue 2, 139-141, 11 February 2013.
APIM050004: ABT-199 (VENETOCLAX)
CAS No.: 1257044-40-8
Molecular Formula: C45H50ClN7O7S
Molecular Weight: 868.4 (refer to Certificate, batch-specific).
Purity: 99.9% by HPLC at 214 and 254 nm.
QC: HPLC-MS, 1HNMR, and Quantitative Elemental Analysis Report.
Solubility: DMSO.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.
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