| 中文名称: | CBL0137 | ||||
|---|---|---|---|---|---|
| 英文名称: | CBL0137 | ||||
| 别名: | 1,1'-[9-[2-[(1-methylethyl)amino]ethyl]-9H-carbazole-3,6-diyl]bis-ethanone | ||||
| CAS No: | 1197996-80-7 | 分子式: | C21H24N2O2 | 分子量: | 336.40 |
| CAS No: | 1197996-80-7 | ||||
| 分子式: | C21H24N2O2 | ||||
| 分子量: | 336.40 | ||||
包装规格：
1mg 5mg 10mg 25mg 50mg 100mg in glass bottle
产品简介：
一种代谢稳定的Curxin,激活p53并抑制NF-κB,EC50：0.47μm。
溶解性：
溶于DMSO
体外研究：
Treatment with CBL-0137 leads to complete absence of living cells at concentrations above 2.5 μM. CBL-0137 causes a greater reduction in the number of colonies formed of not only MiaPaCa-2 cells when combined with gemcitabine, but also gemcitabine-resistant PANC-1 cells. Treatment of human pancreatic cancer cells with CBL-0137 results in a dose dependent reduction of protein and mRNA levels of RRM1 and RRM2. CBL-0137 is able to prevent gemcitabine induced expression of RRM1 and RRM2 on mRNA and protein levels.
体内研究：
The CBL-0137 monotherapy group and the CBL-0137-gemcitabine combination group samples show large necrotic fields, numerous apoptotic bodies and loss of tumor cells. Sub-optimal doses of 50 to 60 mg/kg CBL-0137 causes similar enhancement of gemcitabine antitumor activity as that produced by the maximum tolerated dose (MTD) of 90 mg/kg as indicated by the lack of statistically significant differences among the combination groups. CBL0137 hydrochloride inhibits FACT function through depletion of the pool of active FACT involved in transcription elongation. CBL-0137, given by oral gavage at a nontoxic dose of 30 mg/kg per day on a 5 days on/2 days off schedule, suppresses tumor growth in xenografts of colon (DLD-1), renal cell carcinoma (Caki-1), and melanoma (Mel-7) tumor cell lines and transplanted surgical samples from patients with pancreatic ductal adenocarcinoma.
保存条件：
-20℃
注意事项：
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2、以上信息仅做参考交流之用。
2、以上信息仅做参考交流之用。
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参考文献 & 客户发表文献
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质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
