MYCi975 (NUCC-0200975) 是一种具有口服活性的 MYC 抑制剂，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 (NUCC-0200975) 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 免疫治疗的敏感性。
货号:ajcx15018
CAS:2289691-01-4
分子式:C25H16Cl2F6N2O2
分子量：561.3
溶解度:DMSO: ≥ 250 mg/mL (445.39 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

MYCi975 (NUCC-0200975) is an orally active MYC inhibitor, which disrupts MYC/MAX interaction, promotes MYC T58 phosphorylation and MYC degradation, and impairs MYC driven gene expression. MYCi975 (NUCC-0200975) exhibits potent anti-tumor efficacy with good tolerability, increases tumor immune cell infiltration, and sensitizes tumors to anti-PD1 immunotherapy[1].

MYCi975 (3 days) inhibits P493-6, MV411, and SK-N-B2 cells viability in an MYC-dependent manner with IC50s of 3.7, 3.9, 6.4 μM, respectively[1].

MYCi975 exhibits excellent pharmacokinetic profiles following p.o., i.p., or i.v. administration. The half-lives observed are 7 and 12 hours when dosed at 100 and 250 mg/kg p.o., respectively. The Cmax values attained are 41,533 ng/mL (74 μM) and 54,000 ng/mL (96 μM), respectively[1]. MYCi975 significantly inhibits tumor growth and increases survival in the MycCaP allograft model with animals tolerating a 100 mg/kg/day i.p. dosing for 14 days[1].

[1]. Han H, et al. Small-Molecule MYC Inhibitors Suppress Tumor Growth and Enhance Immunotherapy. Cancer Cell. 2019 Nov 11;36(5):483-497.e15.