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CAS No.: 1353859-00-3

CX-6258 HCl Catalog No. CSN19180

Synonyms: CX-6258 Hydrochloride;CX-6258 HCl

CX-6258 HCl is a potent, orally efficacious pan-Pim kinase inhibitor with IC50 of 5 nM, 25 nM and 16 nM for Pim1, Pim2, and Pim3, respectively.

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400-920-2911

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Pim3

IC50:16nM Pim2

IC50:25nM Pim1

IC50:5nM
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 Hydrochloride is the hydrochloride form of CX-6258. 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^[1] (p.o.)

给药途径

p.o.

动物药代数据

Animal	Nude mice^[1]
Dose	50 mg/kg
Administration	i.v. p.o.
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→24 h}	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
- 2.0064 mL
- 10.0321 mL
- 20.0642 mL
- 5 mM
- 0.4013 mL
- 2.0064 mL
- 4.0128 mL
- 10 mM
- 0.2006 mL
- 1.0032 mL
- 2.0064 mL

技术信息

CAS号

1353859-00-3

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C26H25Cl2N3O3

运输

蓝冰

分子量

498.40

别名

CX-6258 Hydrochloride;CX-6258 HCl

溶解度

DMSO	55.0 mg/mL (110.4 mM) warming
Water	85.0 mg/mL (170.5 mM) warming
Ethanol	1.0 mg/mL (2.0 mM) warming

动物实验配方

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靶点	Description	IC50
Pim3		IC50:16nM
Pim2		IC50:25nM
Pim1		IC50:5nM

CX-6258 HCl Catalog No. CSN19180

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