S81120 |
Cobimetinib |
源叶(MedMol) | 98% |
- 提示:详情请下载说明书。
- 产品描述: Cobimetinib (GDC-0973, RG7420) is a potent, selective and oral MEK1 inhibitor with an IC50 of 4.2 nM for MEK1.
- 靶点: MEK1:4.2 nM (IC50);Apoptosis; MEK
- 体内研究:
In the NCI-H2122 KRASG12C mutant non-small cell lung carcinoma (NSCLC) xenograft model, treatment with up to 5 mg/kg Cobimetinib (GDC-0973) lead to moderate TGI and at 10 mg/kg approaches tumor stasis. GDC-0973 and GDC-0941 are administered to A2058 tumor-bearing mice daily (QD) or every third day (Q3D) either as single agents or in combination. The population rate constants associated with tumor growth inhibition for GDC-0973 and GDC-0941 are 0.00102 and 0000651 μM-1 h-1, respectively. Following single doses of GDC-0973 (1, 3, or 10 mg/kg, p.o.) estimated in vivo IC50 values of %pERK decrease based on tumor concentrations in xenograft mice are 0.78 (WM-266-4) and 0.52 μM (A375)
- 参考文献:
1. Hoeflich KP, et al. Intermittent administration of MEK inhibitor GDC-0973 plus PI3K inhibitor GDC-0941 triggers robust apoptosis and tumor growth inhibition. Cancer Res. 2012 Jan 1;72(1):210-9. 2. Choo EF, et al. PK-PD modeling of combination efficacy effect from administration of the MEK inhibitor GDC-0973 and PI3K inhibitor GDC-0941 in A2058 xenografts. Cancer Chemother Pharmacol. 2013 Jan;71(1):133-43. 3. Wong H, et al. Bridging the gap between preclinical and clinical studies using pharmacokinetic-pharmacodynamic modeling: an analysis of GDC-0973, a MEK inhibitor. Clin Cancer Res. 2012 Jun 1;18(11):3090-9. 4. Corazao-Rozas P, et al. Mitochondrial oxidative phosphorylation controls cancer cell's life and death decisions upon exposure to MAPK inhibitors. Oncotarget. 2016 Feb 29. doi: 10.18632/oncotarget.7790.
- 溶解性: DMSO : 50 mg/mL (94.11 mM; ultrasonic and warming and heat to 60°C) H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 1.882 ml 9.411 ml 18.821 ml 5 mM 0.376 ml 1.882 ml 3.764 ml 10 mM 0.188 ml 0.941 ml 1.882 ml 50 mM 0.038 ml 0.188 ml 0.376 ml
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)