A-1331852

SKU: orb1226296

Description

A-1331852 is a potent and selective BCL-XL inhibitor (Ki<10 pM); shows much weaker affinity for BCL-2 (Ki=6 nM), BCL-W (Ki=4 nM), and MCL-1 (Ki=142 nM); selectively disrupts BCL-XL–BIM complexes and induces the hallmarks of apoptosis in BCL-XL–dependent Molt-4 cells (Molt-4 viability IC50=6 nM); demonstrates antitumor efficacy in the Molt-4 xenograft model; orally active.(In Vitro):A-1331852 selectively disrupts BCL-XL–BIM complexes and induces the hallmarks of apoptosis in BCL-XL–dependent Molt-4 cells with IC50s in the low nanomolar range but does not affect MEF cells lacking BAK or BAX. In CellTiter-Glo cell viability assay, A-1331852 inhibits NCI-H847, NCI-H1417, SET-2, HEL, OCI-M2 with EC50 values of 3, 7, 80, 120 and 100 nM.(In Vivo):A-1331852 demonstrates antitumor efficacy in the Molt-4 xenograft model, inducing tumor regressions as a single agent. Additionally, A-1331852 combines with venetoclax to recapitulate the efficacy of navitoclax in the NCI-H1963.FP5 xenograft model of SCLC. A-1331852 significantly inhibits tumor growth in seven subcutaneous xenograft models of solid tumors, including breast cancer, NSCLC, and ovarian cancer.

Key Properties

• CAS Number: 1430844-80-6
• MW: 658.8117
• Purity: >98% (HPLC)
• Formula: C₃₈H₃₈N₆O₃S
• SMILES: CC1=C(C=NN1CC23CC4CC(C2)CC(C4)C3)C5=C(N=C(C=C5)N6CCC7=CC=CC(=C7C6)C(=O)NC8=NC9=CC=CC=C9S8)C(=O)O
• Target: Bcl-2
• Solubility: DMSO: ≥ 12 mg/mL

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

A1331852 | A 1331852

Quick Database Links

Gene Symbol

Bcl-2