A-1331852是具有口服活性的BCL-XL选择性抑制剂,Ki值小于10 pM。
Description | A-1331852 is an orally available BCL-XL selective inhibitor with a Ki of less than 10 pM. | ||||||||||||||||
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IC50 & Target[1] |
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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[1]. | ||||||||||||||||
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[1]. | ||||||||||||||||
Solvent & Solubility | In Vitro: DMSO : ≥ 50 mg/mL (75.89 mM) H2O : < 0.1 mg/mL (insoluble) * "≥" means soluble, but saturation unknown. Preparing Stock Solutions
* Please refer to the solubility information to select the appropriate solvent. In Vivo:
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References |
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