| Identification | Back Directory | [Name]
MT-DADMe-ImmA | [CAS]
653592-04-2 | [Synonyms]
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)- | [Molecular Formula]
C13H19N5OS | [MOL File]
653592-04-2.mol | [Molecular Weight]
293.39 |
| Chemical Properties | Back Directory | [Melting point ]
108-110 °C | [Boiling point ]
566.1±50.0 °C(Predicted) | [density ]
1.412±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 10 mg/ml; DMSO: 10 mg/ml; PBS (pH 7.2): 1 mg/ml | [form ]
A crystalline solid | [pka]
14.13±0.40(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
MT-DADMe-ImmA is an inhibitor of 5''-methylthioadenosine phosphorylase (MTAP; Ki = 1.7 nM). It increases levels of MTA , a product of polyamine metabolism, in FaDu human squamous cell carcinoma cells when used at a concentration of 1 μM. MT-DADMe-ImmA (5, 9, and 21 mg/kg per day for 28 days) reduces tumor growth in a FaDu mouse xenograft model. | [Uses]
MT-DADMe-ImmA is an inhibitor of human 5'-methylthioadenosine phosphorylase (MTAP) with a Ki of 90 pM. | [in vivo]
The t1/2 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[2]. | [storage]
Store at -20°C | [References]
[1] Evans GB, et al. Second generation transition state analogue inhibitors of human 5'-methylthioadenosine phosphorylase. J Med Chem. 2005 Jul 14;48(14):4679-89. DOI:10.1021/jm050269z
[2] Basu I, et al. A transition state analogue of 5'-methylthioadenosine phosphorylase induces apoptosis in head and neck cancers. J Biol Chem. 2007 Jul 20;282(29):21477-86. DOI:10.1074/jbc.M702287200 |
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| Company Name: |
Twochem Co.Ltd.
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| Tel: |
021-58111628 15800915896 |
| Website: |
cn.twochem.com |
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