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Bcl-xL antagonist 2

Names

[ CAS No. ]:
1235032-75-3

[ Name ]:
Bcl-xL antagonist 2

Biological Activity

[Description]:

Bcl-xL antagonist 2 is a potent, selective, and orally active antagonist of BCL-XL with an IC50 and Ki of 0.091 μM and 65 nM, respectively. Bcl-xL antagonist 2 promotes the apoptosis of cancer cells. Bcl-xL antagonist 2 has the potential for the research of the chronic lymphocytic leukemia (CLL) and non-Hodgkin’s lymphoma (NHL)[1][2].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Bcl-2 Family
Research Areas >> Cancer

[Target]

0.091 μM (BCL-XL)[1]


[In Vivo]

Assessment of Pharmacokinetics (PK) profile of Bcl-xL antagonist 2 (compound 14) in rat[1]. iv (1 mg/kg) po (5 mg/kg) CLp (mL/min/kg) Vss (L/kg) t 1/2 (h) F % 0.47 0.16 6.0 16

[References]

[1]. Koehler MF, et al. Structure-Guided Rescaffolding of Selective Antagonists of BCL-XL. ACS Med Chem Lett. 2014;5(6):662-667.

[2]. Wang L, et al. Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-XL Inhibitor. ACS Med Chem Lett. 2020;11(10):1829-1836.

Chemical & Physical Properties

[ Molecular Formula ]:
C21H16N4O3S2

[ Molecular Weight ]:
436.51

Related Compounds