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653592-04-2

中文名稱 653592-04-2
英文名稱 MT-DADMe-ImmA
CAS 653592-04-2
分子式 C13H19N5OS
分子量 293.39
MOL 文件 653592-04-2.mol
653592-04-2 結(jié)構(gòu)式 653592-04-2 結(jié)構(gòu)式

基本信息

中文別名
(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
英文別名
MTDIA
MT-DADMe-ImmA HCl
Methylthio-DADMe-Immucillin A
METHYLTHIO-DADME-IMMUCILLIN A
MTDIA
MTDIA
MTDIA HCL
METHYLTHIO-DADME-IMMUCILLIN A
MT-DADME-IMMA
MT-DADME-IMMA HCL
3-Pyrrolidinol, 1-[(4-amino-5H-pyrrolo[3,2-d]pyrimidin-7-yl)methyl]-4-[(methylthio)methyl]-, (3R,4S)-

物理化學(xué)性質(zhì)

熔點(diǎn)108-110 °C
沸點(diǎn)566.1±50.0 °C(Predicted)
密度1.412±0.06 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度DMF: 10 mg/ml; DMSO: 10 mg/ml; PBS (pH 7.2): 1 mg/ml
酸度系數(shù)(pKa)14.13±0.40(Predicted)
形態(tài)結(jié)晶固體
顏色White to off-white

常見問題列表

生物活性
MT-DADMe-ImmA是人5'-甲硫基腺苷磷酸化酶的抑制劑 (MTAP)，Ki值為90 pM。
靶點(diǎn)

Ki: 90 pM (MTAP)

體外研究

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.

體內(nèi)研究

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.

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