| 产品描述: | Adagrasib (MRTX849) 是一种有效的,选择性的和共价的KRAS G12C抑制剂,具有良好的药物样特性,可选择性地修饰GDP结合的KRAS G12C中的突变半胱氨酸12并抑制KRAS依赖性信号传导 |
| 靶点: |
K-Ras(G12C);Ras |
| 体外研究: |
To evaluate the breadth of MRTX849 activity, its effect on cell viability is determined across a panel of 17 KRASG12C-mutant and three non-KRASG12C-mutant cancer cell lines using 2D (3-day, adherent cells) and 3D (12-day, spheroids) cell growth conditions. MRTX849 potently inhibits cell growth in the vast majority of KRASG12C-mutant cell lines with IC50 values ranging between 10 nM and 973 nM in the 2D format and between 0.2 nM and 1042 nM in the 3D format |
| 体内研究: |
Rapid tumor regression is observed at the earliest posttreatment tumor measurement and animals in the 30 mg/kg and 100 mg/kg cohorts exhibits evidence of a complete response at study Day 15. Dosing is stopped at study Day 16 and all 4 mice in the 100 mg/kg cohort and 2 out of 7 mice in the 30 mg/kg cohort remains tumor-free through study Day 70 |
| 细胞实验: |
Cell lines: MIA PaCa-2, H1373, H358, H2122, SW1573, H2030, KYSE-410 cells (G12C); H1299 (WT); A549 (G12S), HCT116 (G13D) cells Concentrations: -- Incubation Time: 24 h Method: All cell lines were maintained at 37 ℃ in a humidified incubator at 5% CO2 and were periodically checked for mycoplasma. CellTiter-Glo assay to evaluate cell viability performed on seven KRAS G12C-mutant cell lines and three non-KRAS G12C-mutant cell lines cells grown in 2D tissue culture conditions in a 3-day assay or 3D conditions using 96-well, ULA plates in a 12-day assay. |
| 动物实验: |
Animal Models: MIA PaCa-2 model Dosages: 3 mg/kg, 10 mg/kg, 30 mg/kg and 100 mg/kg Administration: Oral gavage |
| 参考文献: |
1. Jill Hallin,et al. The KRASG12C Inhibitor MRTX849 Provides Insight toward Therapeutic Susceptibility of KRAS-Mutant Cancers in Mouse Models and Patients. Cancer Discov.2020;10 (1): 54-71. |
| 溶解性: |
Soluble in DMSO、Ethanol |
| 保存条件: |
-20°C |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
1.655 ml |
8.277 ml |
16.553 ml |
| 5 mM |
0.331 ml |
1.655 ml |
3.311 ml |
| 10 mM |
0.166 ml |
0.828 ml |
1.655 ml |
| 50 mM |
0.033 ml |
0.166 ml |
0.331 ml |
|
| 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。 |