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 免疫研究的敏感性。
| CAS No. | 2289691-01-4 |
| 生物活性 | 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. |
| 分子式 | C25H16Cl2F6N2O2 |
| 分子量 | 561.3 |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存条件 | Powder -20°C 3 years |
| 溶解性数据 | DMSO : ≥ 250 mg/mL (445.39 mM) |
| 体内研究 | 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. 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. |
| 体外研究 | 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. |
| 文献 | •Research Square Preprint. 2021 Jul. |
| 纯度及产品资料 | 98% |
邮箱：info@TianyaBio.com
电话：020-3107 8154
地址：广州市番禺区兴业大道东路1078号2-50
微信公众号
微信客服
