货号:A232907 同义名: CBL-C137 hydrochloride;Curaxin-137 hydrochloride
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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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 | ✔ | Nrf2,HDAC | 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 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Inert atmosphere,2-8°C |
溶解度 |
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 |
动物实验配方 |