| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|
S81120-1mg买3赠1 |
99.70% | ￥280.00 |
8 | - | - | - |
|
S81120-2mg买3赠1 |
99.70% | ￥370.00 |
7 | - | - | - |
|
S81120-5mg买3赠1 |
99.70% | ￥590.00 |
8 | - | - | - |
|
S81120-10mg买3赠1 |
99.70% | ￥690.00 |
6 | - | - | - |
|
S81120-25mg买3赠1 |
99.70% | ￥780.00 |
5 | - | - | - |
|
S81120-50mg买3赠1 |
99.70% | ￥1400.00 |
5 | - | - | - |
|
S81120-100mg买3赠1 |
99.70% | ￥2400.00 |
5 | - | - | - |
|
| 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. | ||||||||||||||||||||
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| 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： |
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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