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CAS No.: 1202916-90-2

CX-6258 Catalog No. CSN16136

Synonyms: Pim-Kinase Inhibitor X

CX-6258 is a selective and potent Pim inhibitor with IC50 values of 5nM, 25nM and 16nM for Pim-1, Pim-2 and Pim-3 (measured by SAR assay), respectively.

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生物活性

实验方案

技术信息

生物活性

描述Pim (provirus integration site for Moloney murine leukemia virus) family proteins are highly conserved serine/threonine kinases implicated in transcription, translation, cell cycle, survival, and drug resistance through the numerous targets. CX-6258 is a selective and potent Pim inhibitor with IC50 values of 5nM, 25nM and 16nM for Pim-1, Pim-2 and Pim-3 (measured by SAR assay), respectively. Treatment with CX-6258 at concentration ranging in 0.1-10μM for 2h caused dose-dependent reduction of phosphorylation level of BAD, a substrate of Pim-1, and 4E-BP1-S65 and 4E-BP1-T37/46 in MV-4-11 cells. CX-6258 showed antiproliferative activity against a panel of cell lines derived from human solid tumors and hematological malignancies with IC50 values ranging in 0.02-3.7μM, most potent to acute leukemia cell lines. In vivo study showed that oral administration of CX-6258 at dose of 50 or 100mg/kg, once daily for 21 days reduced tumor growth in MV-4-11 xenograft models without obvious weight loss observed^[1].
作用机制CX-6258 can bind to the ATP binding pocket of Pim-1 enzyme.^[1]
动物研究
剂量
Mice: 50 mg/kg, 100 mg/kg^[1] (p.o.)

给药途径
p.o.

动物药代数据
Animal Mice^[1]
F 23% (p.o.)
V_d 85 L/kg (i.v.)
T_1/2 27 h (i.v.)
CL_s 2.1 L/h/kg (i.v.)
AUC_0→24h 1016 ng·h/ml (p.o.)
参考文献

[1] Haddach M, Michaux J, et al. Discovery of CX-6258. A Potent, Selective, and Orally Efficacious pan-Pim Kinases Inhibitor. ACS Med Chem Lett. 2012;3(2):135-9.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1648 mL
- 10.8239 mL
- 21.6478 mL
- 5 mM
- 0.4330 mL
- 2.1648 mL
- 4.3296 mL
- 10 mM
- 0.2165 mL
- 1.0824 mL
- 2.1648 mL

技术信息

CAS号	1202916-90-2	储存条件	粉末液体 -20°C:3-6 月 -80°C:12月
分子式	C26H24ClN3O3	运输	蓝冰
分子量	461.94	别名	Pim-Kinase Inhibitor X

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