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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Isocitrate Dehydrogenase (IDH)-AGI-5198
AGI-5198

Chemical Structure : AGI-5198

CAS No.: 1355326-35-0

AGI-5198 (IDH-C35;AGI5198;AGI 5198;IDH C35)

货号: PC-45413Not For Human Use, Lab Use Only.

AGI-5198 (IDH-C35) is a potent, selective mutant IDH1 inhibitor with IC50 of 70 nM and 160 nM for R132H-IDH1 and R132C-IDH1, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

AGI-5198 (IDH-C35) is a potent, selective mutant IDH1 inhibitor with IC50 of 70 nM and 160 nM for R132H-IDH1 and R132C-IDH1, respectively.
AGI-5198 shows no inhibitory activity for wild type IDH1, IDH2, R140Q-IDH2, R172K-IDH2.
AGI-5198 induces demethylation of histone H3K9me3 and expression of genes associated with gliogenic differentiation, impairs the growth of IDH1-mutant glioma cells.
AGI-5198 decreases levels of D-2-HG in chondrosarcoma cell lines.

物理化学性质&存储条件

分子量 462.5591
分子式 C27H31FN4O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

DMSO: ≥ 34 mg/mL

Chemical Name/SMILES

1H-Imidazole-1-acetamide, N-[2-(cyclohexylamino)-1-(2-methylphenyl)-2-oxoethyl]-N-(3-fluorophenyl)-2-methyl-

参考文献

1. Rohle D, et al. Science. 2013 May 3;340(6132):626-30.

2. Suijker J, et al. Oncotarget. 2015 May 20;6(14):12505-19.

3. Molenaar RJ, et al. Cancer Res. 2015 Nov 15;75(22):4790-802.

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