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产品价格:电议      采购度:1621      原产地:美洲
发布时间:2021/8/3 16:18:01 所属地区:上海 上海市
简要描述:
MBQ-167 是 Ras 相关的 C3 型肉毒素底物 (Rac) 和细胞分裂周期蛋白 (Cdc42) 的双抑制剂,其对 Rac 1/2/3 的 IC50 值为 103 nM, 对 Cdc42 的 IC50 值为 78 nM。
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CAS No. : 2097938-73-1
MCE 站:MBQ-167
产品活性:MBQ-167 是 Ras 相关的 C3 型肉毒素底物 (Rac) 和细胞分裂周期蛋白 (Cdc42) 的双抑制剂,其对 Rac 1/2/3 的 IC50 值为 103 nM, 对 Cdc42 的 IC50 值为 78 nM。
研究领域:GPCR/G Protein | Cell Cycle/DNA Damage
In Vitro: MBQ-167 (≥100 nM) induces a loss of polarity in metastatic breast cancer cells. Treatment with 500 nM MBQ-167 for 24 h results in ~95% cell rounding and detachment from the substratum in metastatic MDA-MB-231 cells. Moreover, MBQ-167 induces this phenotype in multiple mesenchymal cancer cell types including GFP-HER2-BM, MDA-MB-468, and Hs578t human breast cancer cells, as well as Mia-PaCa-2 pancreatic cancer cells, SKOV3 ovarian cancer cells, AGS and NCI-N87 gastric cancer cells, and SH-SY5Y neuroblastoma cells. Following treatment with 250 nM MBQ-167 for 24 h, the attached population of MDA-MB-231 cells demonstrate a ~25% decrease in Rac activation while the detached cells are more responsive with a ~75% decrease. At earlier times (6h), treatment with 250 or 500 nM MBQ-167, induce a inhibition in Rac activity in the attached cell population, while the detached population demonstrate a ~40-50% inhibition.
In Vivo: MBQ-167-treated mice demonstrate a statistically significant reduction in tumor growth. At sacrifice, 1.0 mg/kg BW of MBQ-167 results in a ~80% reduction in tumor growth, and the 10 mg/kg BW MBQ-167 treatment results in ~95% reduction in tumor growth. Since EHop-016 only exerts ~40% reduction of tumor growth at 10 mg/kg BW, MBQ-167 is 10X more effective than EHop-016. MBQ-167 treated mice demonstrate similar doubling times for both treatments (10 and 11 days).
相关产品:Bioactive Compound Library Plus | Cell Cycle/DNA Damage Compound Library | GPCR/G Protein Compound Library | Kinase Inhibitor Library | Anti-Cancer Compound Library | Anti-Aging Compound Library | Ferroptosis Compound Library | Glutamine Metabolism Compound Library | Anti-Breast Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | Anti-Blood Cancer Compound Library | BI-2852 | Ro-3306 | Seliciclib | Flavopiridol | NSC 23766 trihydrochloride | NVP-2 | Ketoconazole | ML141 | Rhosin hydrochloride | SNS-032 | EHT 1864 | AZD-5438 | CASIN | Kenpaullone | Lonafarnib | EHop-016 | GSK 3 Inhibitor IX | AUZ 454 | XL413 hydrochloride | Salirasib | CGP60474 | Wogonin | CID-1067700 | LC-2 | CVT-313 | GGTI298 | NG 52 | BMS-265246 | (R)-CR8 trihydrochloride
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更新时间:2024/1/2 10:17:44
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