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。

MYCi975 is an orally active inhibitor of MYC.

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].

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.

2289691-01-4

C25H16Cl2F6N2O2

561.3

NUCC-0200975

DMSO:247 mg/mL (440.05mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years