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)。
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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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。 |
靶点 |
|
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]. |
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. |
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 |
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 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
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动物实验配方 |