A-1331852

Research use only, not for human use.

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).

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.

——

——

A1331852 | A 1331852

Angiogenesis

Bcl-2

Bcl-2|Bcl-w|Bcl-xL|Mcl-1

Inflammation/Immunology

——

1430844-80-6

658.8117

C38H38N6O3S

>98% (HPLC)

DMSO: ≥ 12 mg/mL

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

2-Pyridinecarboxylic acid, 6-[8-[(2-benzothiazolylamino)carbonyl]-3,4-dihydro-2(1H)-isoquinolinyl]-3-[5-methyl-1-(tricyclo[3.3.1.13,7]dec-1-ylmethyl)-1H-pyrazol-4-yl]-

(-20℃)

With Ice Pack

≥ 2 years