Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Olutasidenib (FT-2102) 是一种可透过血脑屏障的、具有口服活性的、突变型异柠檬酸脱氢酶(IDH)1的选择性有效抑制剂,对IDH1- R132H 和 IDH1- R132C 的IC50分别为 21.2 nM 和 114 nM,可用于急性髓性白血病或骨髓增生异常综合征的研究。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 697 | 现货 | ||
5 mg | ¥ 1,730 | 现货 | ||
10 mg | ¥ 2,820 | 现货 | ||
25 mg | ¥ 4,680 | 现货 | ||
50 mg | ¥ 6,690 | 现货 | ||
100 mg | ¥ 8,930 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,870 | 现货 |
产品描述 | Olutasidenib (FT-2102) is under the study in the treatment of acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS). Olutasidenib is a highly effective, brain penetrant, and selective inhibitor of the mutant Isocitrate dehydrogenase 1 (IDH1) (IC50: 21.2 nM and 114 nM for IDH1- R132H and IDH1- R132C, respectively). |
靶点活性 | IDH1- R132C:114 nM (IC50), IDH1- R132H:21.2 nM (IC50) |
体外活性 | Olutasidenib is highly selective for IDH1 isoforms, showing no appreciable inhibition against wild-type IDH1 (> 20 μM) and IDH2 mutants (R172K and R140Q: both > 20 μM). Olutasidenib effectively suppresses 2-HG production by multiple IDH1-R132 mutants (R132H, R132C, R132G, R132L), displaying Olutasidenib (FT-2102) could be efficacious against most IDH1-R132 mutant-expressing tumors [2]. |
体内活性 | In HCT116-IDH1-R132H/+ xenograft bearing female BALB/c Nude mice, Olutasidenib (three oral doses (12.5, 25, and 50 mg/kg) in 12-hour intervals) shows effective anti-tumor activity [2]. |
别名 | FT-2102 |
分子量 | 354.79 |
分子式 | C18H15ClN4O2 |
CAS No. | 1887014-12-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 122 mg/mL (343.87mM), sonification is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.8186 mL | 14.0928 mL | 28.1857 mL | 70.4642 mL |
5 mM | 0.5637 mL | 2.8186 mL | 5.6371 mL | 14.0928 mL | |
10 mM | 0.2819 mL | 1.4093 mL | 2.8186 mL | 7.0464 mL | |
20 mM | 0.1409 mL | 0.7046 mL | 1.4093 mL | 3.5232 mL | |
50 mM | 0.0564 mL | 0.2819 mL | 0.5637 mL | 1.4093 mL | |
100 mM | 0.0282 mL | 0.1409 mL | 0.2819 mL | 0.7046 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Olutasidenib 1887014-12-1 Metabolism Isocitrate Dehydrogenase (IDH) Dehydrogenase mutant FT2102 FT 2102 inhibit 2-HG FT-2102 Inhibitor inhibitor