MYCi975
产品说明书
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同义名 : | NUCC-0200975 |
| CAS号 : | 2289691-01-4 | |
| 货号 : | A1251865 | |
| 分子式 : | C25H16Cl2F6N2O2 | |
| 纯度 : | 99%+ | |
| 分子量 : | 561.3 | |
| MDL号 : | MFCD32263413 | |
| 存储条件： |
Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - |
| 生物活性 | |||
|---|---|---|---|
| 描述 | MYC proteins, including MYC, MYCL, and MYCN, play critical roles in tumorigenesis and therapeutic resistance. MYCi975 is an inhibitor of MYC that binds to intracellular MYC with a KD of 2.5 μM. Treatment of PC3 cells with MYCi975 (8 μM) enhanced MYC degradation and phosphorylation on T58. MYCi975 (6 μM) directly increased GSK3β-mediated MYC pT58 in the in vitro kinase assay. In prostate cancer cells and PC12 cells, MYCi975 inhibited cell viability in an MYC-dependent manner and selectively suppressed E-box luciferase activity. MYCi975 (6 μM; 24 h) affected the expression of 3,647 genes, most (69%) of which were MYC responsive. In vivo, MYCi975 significantly inhibited tumor growth and increased survival in the MycCaP allograft model with animals tolerating a 100 mg/kg/day i.p. dosing for 14 days. It increased pT58 and PD-L1 levels and enhanced tumor infiltration of CD3+ T cells, B220+ B Cells, and NKp46+ NK cells. Moreover, treatment of Lewis lung carcinoma (LLC1)-bearing mice with MYCi975 (100 mg/kg/day) inhibited tumor growth with no changes in body weight[2]. | ||
| 作用机制 | MYCi975 binds to amino acids 353–439 of the MYC protein[2]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
1.78mL 0.36mL 0.18mL |
8.91mL 1.78mL 0.89mL |
17.82mL 3.56mL 1.78mL |
| 参考文献 |
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