MYCi975,2289691-01-4

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抑制剂描述：

产品名称：MYCi975

产品别名：见爱必信官网

英文别名：MYCi975

靶点：

CAS：2289691-01-4

纯度：98%

外观：见爱必信官网

保存方法：Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

描述：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.

溶解性：DMSO ：100 mg/mL (178.16 mM)

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.

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.

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