货号:A984969 同义名: MTDIA;Methylthio-DADMe-Immucillin A
MT-DADMe-ImmA, a chemically stable analogue for the proposed transition state of human MTAP, is a novel MTAP inhibitor with potential for the treatment of human head and neck and prostate carcinoma.
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产品名称 | Phosphorylase ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
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Tipiracil hydrochloride | ✔ | 98% | |||||||||||||||||
CP-91149 |
+++
Glycogen phosphorylase (GP), IC50: 0.13 μM |
98+% | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | MT-DADMe-ImmA is an inhibitor of MTAP with a Ki value of 90 pM[1]. Treatment of cultured cells with MT-DADMe-ImmA and MTA inhibits MTAP, increases cellular MTA concentrations, reduces polyamines, and induces apoptosis in FaDu and Cal27 cells, but does not induce apoptosis in normal human fibroblast lines (CRL2522 and GM02037) or in MCF7 (a breast cancer cell line lacking the MTAP gene). Single use of MT-DADMe-ImmA does not induce apoptosis in any cell line, indicating that MTA acts as the active agent[2]. |
Animal study | The initial inhibition of MTAP by MT-DADMe-ImmA has a half-life (t1/2) of 50 minutes, with complete inhibition at 250 minutes. MTAP activity slowly recovers, and the oral bioavailability half-life of MT-DADMe-ImmA is 6.3 days. Oral or intraperitoneal injection of MT-DADMe-ImmA inhibits the time-dependent growth of FaDu tumors in immunodeficient mice[2]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.41mL 0.68mL 0.34mL |
17.04mL 3.41mL 1.70mL |
34.08mL 6.82mL 3.41mL |
CAS号 | 653592-04-2 |
分子式 | C13H19N5OS |
分子量 | 293.388 |
别名 | MTDIA;Methylthio-DADMe-Immucillin A |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Inert atmosphere,2-8°C |
溶解度 |
DMSO: 105 mg/mL(357.89 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |