653592-04-2

653592-04-2

中文名称653592-04-2
中文同义词(3R,4S)-1-[(4-氨基-5H-吡咯并[3,2-D]嘧啶-7-基)甲基]-4-[(甲硫基]-3-吡咯烷醇;(3R,4S)-1-((4-氨基-5H-吡咯并[3,2-D]嘧啶-7-基)甲基)-4-((甲硫基)甲基)吡咯烷-3-醇;化合物MT-DADME-IMMA
英文名称MT-DADMe-ImmA
英文同义词MT-DADMe-ImmA HCl;MTDIA; MTDIA HCL; METHYLTHIO-DADME-IMMUCILLIN A; MT-DADME-IMMA; MT-DADME-IMMA HCL;Methylthio-DADMe-Immucillin A;METHYLTHIO-DADME-IMMUCILLIN A; MTDIA;MTDIA;3-Pyrrolidinol, 1-[(4-amino-5H-pyrrolo[3,2-d]pyrimidin-7-yl)methyl]-4-[(methylthio)methyl]-, (3R,4S)-;(3R,4S)-1-((4-Amino-5H-pyrrolo[3,2-d]pyrimidin-7-yl)methyl)-4-((methylthio)methyl)pyrrolidin-3-ol;MTDADMeImmA,inhibit,MT DADMe ImmA,Inhibitor
CAS号653592-04-2
分子式C13H19N5OS
分子量293.39
EINECS号
相关类别
Mol文件653592-04-2.mol
结构式653592-04-2 结构式

653592-04-2 性质

熔点108-110 °C
沸点566.1±50.0 °C(Predicted)
密度1.412±0.06 g/cm3(Predicted)
储存条件Store at -20°C
溶解度DMF:10mg/mL; DMSO:10mg/mL; PBS(pH 7.2):1 mg/mL
形态结晶固体
酸度系数(pKa)14.13±0.40(Predicted)
颜色白色至米白色

653592-04-2 用途与合成方法

MT-DADMe-ImmA是人5'-甲硫基腺苷磷酸化酶的抑制剂 (MTAP),Ki值为90 pM。

Ki: 90 pM (MTAP)

Treatment of cultured cells with MT-DADMe-ImmA and MTA inhibit MTAP, increase cellular MTA concentrations, decrease polyamines, and induce apoptosis in FaDu and Cal27, two head and neck squamous cell carcinoma cell lines. The same treatment does not induce apoptosis in normal human fibroblast cell lines (CRL2522 and GM02037) or in MCF7, a breast cancer cell line with an MTAP gene deletion. MT-DADMe-ImmA alone does not induce apoptosis in any cell line, implicating MTA as the active agent.

The t 1/2 for onset of inhibition is 50 min with complete inhibition by 250 min. MTAP activity slowly returns, giving a biological half-life for the action of oral MT-DADMe-ImmA of 6.3 days. The time-dependent growth of FaDu tumors in immunodeficient mice is suppressed by oral or intraperitoneal treatment with MT-DADMe-ImmA.

安全信息

MSDS信息

653592-04-2 上下游产品信息

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