CX-6258

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的、选择性的、口服有效的 pan-Pim 抑制剂，对 Pim1/2/3 的 IC50 分别为 5/25/16 nM。

A potent, selective, and orally efficacious pan-Pim inhibitor with IC50 of 5/25/16 nM for Pim1/2/3, respectively; exhibits in vitro synergy with chemotherapeutics and robust in vivo efficacy in driven tumor models; also decreases steady state levels and half-life of NKX3.1 protein but not mRNA in prostate cancer cells.Blood Cancer Discontinued.

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.CX-6258 treatment (12 mM, 3 h) treatment diminishes steady-state levels of ectopic NKX3.1 in PC3 cells.CX-6258 treatment results in a significant reduction in NKX3.1 half-life. Western Blot Analysis 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. Animal Model:Nude mice, MV-4-11 xenograft modelsDosage: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.

CX6258 | CX 6258

JAK/STAT Signaling

Pim

Pim1| Pim2| Pim3

Cancer

Blood cancer

1202916-90-2

461.9401

C26H24ClN3O3

>98% (HPLC)

10 mM in DMSO

CN1CCCN(CC1)C(=O)C2=CC=CC(=C2)C3=CC=C(O3)/C=C/4\C5=C(C=CC(=C5)Cl)NC4=O

2H-Indol-2-one, 5-chloro-3-[[5-[3-[(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)carbonyl]phenyl]-2-furanyl]methylene]-1,3-dihydro-, (3E)-

(-20℃)

With Ice Pack

≥ 2 years