| 产品描述： | Ivosidenib (AG-120) is an orally active inhibitor of isocitrate dehydrogenase 1 mutant (mIDH1) enzyme, it exhibits profound d-2-hydroxyglutatrate (2-HG) lowering in vivo. Ivosidenib (AG-120) has the potential for AML therapy due to its acceptable safety profile and clinical activity |
| 靶点： |
12 nM (mouse IDH1R132H);Dehydrogenase;IsocitrateDehydrogenase(IDH) |
| 体外研究： |
Ivosidenib (AG-120) (0-13 μM; 48 hours) inhibits several IDH1-R132 mutants with potency similar IC50 values: IDH1-R132H (IC50=12 nM); IDH1-R132C (IC50=13 nM); IDH1-R132G (IC50=8 nM); IDH1-R132L (IC50=13 nM); IDH1-R132S (IC50=12 nM), respectively |
| 体内研究： |
AG-120 (gavage administration; 50 mg/kg and 150 mg/kg) declines tumor 2-HG concentration rapidly, with maximum inhibition (92.0% and 95.2% at the 50 mg/kg and 150 mg/kg doses, respectively) achieved at -12 h post dose. Animal Model: Female nude BALB/c mice inoculated with HT1080 cells Dosage: 50 mg/kg and 150 mg/kg Administration: Gavage administration; 50 mg/kg and 150 mg/kg Result: Showed robust tumor 2-HG reduction in mouse. |
| 参考文献： |
1. Popovici-Muller J, et al. Discovery of AG-120 (Ivosidenib): A First-in-Class Mutant IDH1 Inhibitor for the Treatment of IDH1Mutant Cancers. ACS Med Chem Lett. 2018 Jan 19;9(4):300-305. |
| 溶解性： |
soluble in DMSO |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.715 ml |
8.577 ml |
17.154 ml |
| 5 mM |
0.343 ml |
1.715 ml |
3.431 ml |
| 10 mM |
0.172 ml |
0.858 ml |
1.715 ml |
| 50 mM |
0.034 ml |
0.172 ml |
0.343 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京