Bcl-xL antagonist 2 是一种有效的，选择性的，并具有口服活性的 BCL-XL 拮抗剂。IC50 和 Ki 值分别为 0.091 μM和 65 nM。Bcl-xL antagonist 2 可以促进癌细胞凋亡 (apoptosis)。Bcl-xL antagonist 2 有针对研究慢性淋巴细胞白血病 (CLL) 和非霍奇金淋巴瘤 (NHL) 的潜力。
货号:ajcx35460
CAS:1235032-75-3
分子式:C21H16N4O3S2
分子量：436.51
溶解度:DMSO : 62.5 mg/mL (143.18 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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].

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

[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.