| Bioactivity | TC-E 5008 is a potent mutant IDH1 inhibitor with Ki values of 190 nM and 120 nM for R132H and R132C IDH1 mutants, respectively. TC-E 5008 exhibits very weak activity against WT-IDH1 with a Ki value of 12.3 μM. TC-E 5008 has anti-proliferative activity on multiple ER positive breast cancer cell lines[1][2]. |
| Invitro | TC-E 5008 (化合物 2; 48 小时) 抑制具有 IDH1(R132C) 突变的 HT1080 纤维肉瘤细胞中 D2HG 的产生，EC50 值为 2.4 μM[1]。 TC-E 5008 (2-10 μM; 72 小时) 对多种 ER 阳性乳腺癌细胞系具有抗增殖活性[2]。 Cell Proliferation Assay[2] Cell Line: |
| Name | TC-E 5008 |
| CAS | 50405-58-8 |
| Formula | C13H13NO2 |
| Molar Mass | 215.25 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Baisong Zheng, et al. Crystallographic Investigation and Selective Inhibition of Mutant Isocitrate Dehydrogenase. ACS Med Chem Lett. 2013 Jun 13;4(6):542-546. [2]. Vasanth S. Murali, et al. Cancer drug discovery as a low rank tensor completion problem. bioRxiv, March 9, 2021. |