MRTX-1257
产品说明书
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同义名 : | - |
| CAS号 : | 2206736-04-9 | |
| 货号 : | A1003571 | |
| 分子式 : | C33H39N7O2 | |
| 纯度 : | 98% | |
| 分子量 : | 565.71 | |
| MDL号 : | MFCD31813777 | |
| 存储条件： |
Pure form Sealed in dry, store in freezer, under -20°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
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| 描述 | The Rat sarcoma (RAS) oncogene family, encoding 21 kD monomeric GTPases that function to transduce extracellular signals to intracellular signal transduction cascades, is comprised of three members (KRAS, HRAS, and NRAS) that play an important role in human cancer. KRAS is the most frequently mutated oncogene in cancer and KRAS mutation is commonly associated with poor prognosis and resistance to therapy [1]. MRTX1257 demonstrates the ability to irreversibly modify KRASG12C, trap it in its inactive GDP-bound state, and inhibit ERK1/2 (KRAS-dependent extracellular signal-regulated kinase) with an IC50 value of 1 nM. MRTX1257 also demonstrated dose-dependent irreversible modification of KRASG12C and inhibition of KRAS-dependent signal transduction in multiple KRASG12C mutant tumor models. Across a large panel of KRASG12C-mutant cell-derived and patient-derived xenografts (n = 23), MRTX1257 demonstrated near-complete KRAS target inhibition with broad spectrum anti-tumor activity including deep tumor regressions in approximately 80% of all models[1]. Further, MRTX-1257 shows sustained regression at 3, 10, 30, and 100 mg/kg dose groups[2]. | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
1.77mL 0.35mL 0.18mL |
8.84mL 1.77mL 0.88mL |
17.68mL 3.54mL 1.77mL |
| 参考文献 |
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