| Chemical Properties | Back Directory | [density ]
1.545±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 62.5 mg/mL (143.18 mM; Need ultrasonic) | [form ]
Solid | [pka]
1.18±0.10(Predicted) | [color ]
Light yellow to green yellow |
| Hazard Information | Back Directory | [Uses]
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]. | [Biological Activity]
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 | [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. |
|
|