MYCi975是一种具有口服活性的MYC抑制剂,具有很强的抗肿瘤作用和良好的耐受性,增加肿瘤免疫细胞浸润,增强肿瘤对抗 PD1 免疫研究的敏感性。它破坏 MYC/MAX 相互作用,促进 MYC T58 磷酸化和 MYC 降解,并损害 MYC 驱动的基因表达。
产品描述
MYCi975 is an orally active inhibitor of MYC.
体外活性
MYCi975 inhibits P493-6, MV411,SK-N-B2 cells viability in an MYC-dependent manner(IC50s of 3.7, 3.9, 6.4 μM, respectively)[1].
体内活性
The initial lead, MYC inhibitor 361 (MYCi361), suppressed in vivo tumor growth in mice, increased tumor immune cell infiltration, upregulated PD-L1 on tumors, and sensitized tumors to anti-PD1 immunotherapy. However, 361 demonstrated a narrow therapeutic index. An improved analog, MYCi975 showed better tolerability.
Cas No.
2289691-01-4
分子式
C25H16Cl2F6N2O2
分子量
561.3
别名
NUCC-0200975
储存和溶解度
DMSO:247 mg/mL (440.05mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years