CX-6258 hydrochloride hydrate是一种强效的、激酶选择性的pan-Pim 激酶抑制剂，对 Pim-1, Pim-2 和 Pim-3 作用的IC50值分别为 5 nM、25 nM 和 16 nM。

CX-6258 hydrochloride hydrate is a potent and kinase selective pan-Pim kinases inhibitor, with IC 50 s of 5 nM, 25 nM and 16 nM for Pim-1, Pim-2 and Pim-3, respectively [1].

CX-6258 causes dose dependent inhibition of the phosphorylation of two pro-survival proteins, Bad and 4E-BP1, at the Pim kinase specific sites S112 and S65 and T37/46, respectively [1]. CX-6258 treatment (12 mM, 3 h) treatment diminishes steady-state levels of ectopic NKX3.1 in PC3 cells [2]. CX-6258 treatment results in a significant reduction in NKX3.1 half-life [2]. Western Blot Analysis [1] Cell Line: MV-4-11 human AML cells. Concentration: 0.1 μM, 1 μM, 10 μM. Incubation Time: 2 hours. Result: Caused dose dependent inhibition of the phosphorylation of two pro-survival proteins, Bad and 4E-BP1, at the Pim kinase specific sites S112 and S65 and T37/46, respectively.

CX-6258 (50-100 mg/kg; p.o; daily; over a period of 21 days) exhibits robust in vivo efficacy in two Pim kinases driven tumor models [1]. Animal Model: Nude mice, MV-4-11 xenograft models [1] Dosage: 50 mg/kg, 100 mg/kg. Administration: Oral administration; once daily; over a period of 21 days. Result: Exhibited dose dependent efficacy, with a 50 mg/kg dose producing 45% tumor growth inhibition (TGI) and a 100 mg/kg dose producing 75% TGI.

1353858-99-7

C26H27Cl2N3O4

516.42

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years