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CBL0137盐酸 /CBL0137 HCl

货号:A232907 同义名: CBL-C137 hydrochloride;Curaxin-137 hydrochloride

CBL0137 HCl是一种代谢稳定的 curaxin,激活 p53(EC50 值为 0.37 µM),并抑制 NF-κB(EC50 值为 0.47 µM)。

CBL0137 HCl 化学结构 CAS号:1197397-89-9
CBL0137 HCl 化学结构
CAS号:1197397-89-9
CBL0137 HCl 3D分子结构
CAS号:1197397-89-9
CBL0137 HCl 化学结构 CAS号:1197397-89-9
CBL0137 HCl 3D分子结构 CAS号:1197397-89-9
规格 价格 库存 数量
50μL*10mM(DMSO) ¥129随货¥99 咨询
100μL*10mM(DMSO) ¥189随货¥139 咨询
250μL*10mM(DMSO) ¥369随货¥259 咨询
500μL*10mM(DMSO) ¥569随货¥399 咨询
10mM*1mL(DMSO) ¥862 咨询
2mg ¥441 咨询
5mg ¥878 咨询
10mg ¥1197 咨询
25mg ¥2155 咨询
50mg ¥3232 咨询
100mg ¥4788 咨询
1g ¥7585 咨询
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CBL0137 HCl 纯度/质量文件 产品仅供科研

货号:A232907 标准纯度:
批次查询: 批次纯度:

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产品名称 p53 其他靶点 纯度
Pifithrin-μ 99%+
Pifithrin-α HBr 98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。
产品名称 NF-κB 其他靶点 纯度
PDTC ammonium 98%
QNZ ++++

NF-κB, IC50: 11 nM

99%+
Sodium 4-Aminosalicylate Dihydrate 98%
Sodium Salicylate 95%
Parthenolide p53 97% HPLC
JSH-23 +

NF-κB, IC50: 7.1 μM

98%
Phenethyl caffeate 98%
Andrographolide 98+%
Curcumin HDAC,Nrf2 98%
SC75741 +++

NF-κB, EC50: 200 nM

99%+
CBL0137 HCl ++

NF-κB, EC50: 0.47 μM

p53 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

CBL0137 HCl 生物活性

靶点
  • NF-κB

    NF-κB, EC50:0.47 μM

描述 Administering CBL0137 hydrochloride eliminates viable cells at dosages surpassing 2.5 μM. This compound notably diminishes the number of colonies formed, impacting not just MiaPaCa-2 cells but also those resistant to gemcitabine, such as PANC-1 cells. In human pancreatic cancer cell treatments, CBL0137 hydrochloride leads to a concentration-dependent decrease in the protein and mRNA levels of RRM1 and RRM2[1].
体内研究

Observations from the CBL0137 hydrochloride solo treatment group and the group receiving a combination of CBL0137 hydrochloride and gemcitabine reveal extensive necrotic areas, a high number of apoptotic bodies, and a significant reduction in tumor cells. Lower doses of CBL0137 hydrochloride, between 50 to 60 mg/kg, enhance the anticancer efficacy of gemcitabine similarly to the maximum tolerated dose (MTD) of 90 mg/kg, underscoring no meaningful difference among the combination treatments. The mechanism of CBL0137 hydrochloride's action involves the inhibition of FACT by depleting the active FACT pool necessary for transcription elongation[1].

Furthermore, CBL0137 hydrochloride, when orally administered at a safe dosage of 30 mg/kg daily, following a 5 days on/2 days off regimen, effectively curtails tumor growth in xenograft models derived from colon (DLD-1), renal cell carcinoma (Caki-1), melanoma (Mel-7) cell lines, and surgical samples from pancreatic ductal adenocarcinoma patients[2].

体外研究

Administering CBL0137 hydrochloride eliminates viable cells at dosages surpassing 2.5 μM. This compound notably diminishes the number of colonies formed, impacting not just MiaPaCa-2 cells but also those resistant to gemcitabine, such as PANC-1 cells. In human pancreatic cancer cell treatments, CBL0137 hydrochloride leads to a concentration-dependent decrease in the protein and mRNA levels of RRM1 and RRM2[1].

CBL0137 HCl 动物研究

Dose Mice: 25 mg/kg[1] (p.o.); 90 mg/kg[1] (i.p.); 50 mg/kg (i.v.)
Administration p.o., i.p., i.v.

CBL0137 HCl 参考文献

[1]Burkhart C, et al. Curaxin CBL0137 eradicates drug resistant cancer stem cells and potentiates efficacy of gemcitabine in preclinical models of pancreatic cancer. Oncotarget. 2014 Nov 30;5(22):11038-53.

[2]Gasparian AV, et al. Curaxins: anticancer compounds that simultaneously suppress NF-κB and activate p53 by targeting FACT. Sci Transl Med. 2011 Aug 10;3(95):95ra74.

CBL0137 HCl 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.68mL

0.54mL

0.27mL

13.41mL

2.68mL

1.34mL

26.82mL

5.36mL

2.68mL

CBL0137 HCl 技术信息

CAS号1197397-89-9
分子式C21H25ClN2O2
分子量 372.888
别名 CBL-C137 hydrochloride;Curaxin-137 hydrochloride;Curaxin 137;CBLC137;CBL0137 (hydrochloride);Curaxin 137 HCl;CBLC137 HCl;CBL0137 hydrochloride
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Inert atmosphere,2-8°C

溶解方案

DMSO: 35 mg/mL(93.86 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 10 mg/mL(26.82 mM),配合低频超声助溶

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案一
方案二
动物实验配方
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