MYCi975CAS号: 2289691-01-4分子式: C25H16Cl2F6N2O2分子量: 561.30描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)
产品描述 | |
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.
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纯度 |
98%
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储存/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.
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基本信息 | |
别名 |
NUCC-0200975
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外观 |
Off white powder
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可溶性/溶解性 |
DMSO :100 mg/mL (178.16 mM)
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生物活性 | |
靶点 |
MYC
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In vitro(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.
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In vivo(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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分子结构图