|1,1'-(9-(2-(异丙基氨基)乙基)-9H-咔唑-3,6-二基)二乙酮盐酸盐|CsnPharm

CAS No.: 1197397-89-9

CBL0137 HCl/CBL0137盐酸 Catalog No. CSN22315

Synonyms: Curaxin-137 hydrochloride;CBL-C137 hydrochloride;CBLC137

CBL0137 HCl is a metabolically stable curaxin that activates p53 with an EC50 value of 0.37 µM and inhibits NF-κB with an EC50 of 0.47 µM.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述CBL0137 hydrochloride is the hydrochloride form of CBL0137. CBL0137 is an NF-κB inhibitor and a P53 activator with EC50 value of 470nM and 370nM (measured by cell-based p53 and NF-kB reporter assays), respectively, and also showed indirect inhibition of FACT and heat shock response stress pathways mediated by HSF-1. Induced phosphorylation of Ser392 of p53 can be observed in HT1080 cells treated with 0.8μM CBL0137 for 8h. CBL0137 showed anticancer effect in mice as it inhibited oncogene-induced transformation and tumor growth in an interferon-dependent manner. Also it can destabilize nucleosomes via disruption of histone/DNA interactions and induce TRAIN.
动物研究
剂量
Mice: 25 mg/kg^[1] (p.o.); 90 mg/kg^[1] (i.p.); 50 mg/kg (i.v.)

给药途径
p.o., i.p., i.v.
参考文献

动物研究
剂量	Mice: 25 mg/kg^[1] (p.o.); 90 mg/kg^[1] (i.p.); 50 mg/kg (i.v.)
给药途径	p.o., i.p., i.v.

[1] Barone TA, Burkhart CA, et al. Anticancer drug candidate CBL0137, which inhibits histone chaperone FACT, is efficacious in preclinical orthotopic models of temozolomide-responsive and -resistant glioblastoma. Neuro Oncol. 2017 Feb 1;19(2):186-196.

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
- 2.6818 mL
- 13.4088 mL
- 26.8177 mL
- 5 mM
- 0.5364 mL
- 2.6818 mL
- 5.3635 mL
- 10 mM
- 0.2682 mL
- 1.3409 mL
- 2.6818 mL

技术信息

CAS号

1197397-89-9

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H25ClN2O2

运输

蓝冰

分子量

372.89

别名

Curaxin-137 hydrochloride;CBL-C137 hydrochloride;CBLC137;CBL0137 (hydrochloride);CBL-0137

溶解度

DMSO	25.0 mg/mL (67.0 mM)

动物实验配方

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