Olutasidenib

製品コードS8949 バッチS894901

印刷

化学情報

Chemical Structure Synonyms FT-2102 Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C18H15ClN4O2

 
分子量 354.79 CAS No. 1887014-12-1
Solubility (25°C)* 体外 DMSO 71 mg/mL (200.11 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Olutasidenib is a potent, orally bioavailable, brain penetrant and selective mutant IDH1 (mIDH1) inhibitor with IC50 of 21.1 nM, 114 nM for IDH1-R132H, IDH1-R132C, respectively.
in vitro

Profiling in various mIDH1 over-expressing U87 cells and HCT116 cells reveals that olutasidenib potently inhibits 2-HG production by multiple IDH1-R132 mutants (R132H, R132C, R132G, R132L), suggesting olutasidenib could be efficacious against most IDH1-R132 mutant-expressing tumors. Olutasidenib is highly selective for IDH1 isoforms, showing no appreciable inhibition against wild-type IDH1 and IDH2 mutants.[1].
in vivo

In IDH1-R132H/ xenograft models, the free concentration of Olutasidenib is comparable in plasma and xenograft tumors, and exposures are dose-dependent. In comparison to the vehicle treated group, Olutasidenib shows a time and dose-dependent inhibition of 2-HG levels in tumor. Calculations based upon the percentage of suppression of 2-HG concentration in tumor versus the free drug concentration in tumor give in vivo IC50 values of 26 nM and 36 nM in the HCT116-IDH1-R132H or HCT116-IDH1-R132C models, respectively. Olutasidenib has good cell permeability and low efflux ratio in the male CD-1 mouse, which indicate a low probability of p-glycoprotein driven efflux.[1].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 HCT116-IDH1-R132H/+, HCT116-IDH1-R132C/+, HT1080, U87MG cells
濃度
反応時間 24 h
実験の流れ

HCT116-IDH1-R132H/+ and HCT116-IDH1-R132C/+ cells are cultured in McCoy’s 5A media supplemented with 10% Fetal Bovine Serum (FBS). HT-1080 and IDH1 mutant expressing U87MG cells are cultured in Dulbecco’s Modified Eagle’s medium supplemented with 10% FBS. To determine the potency of Olutasidenib in inhibiting 2-HG production, cells are treated with Olutasidenib for 24 hours in a 37°C CO2 incubator. The cell pellets are extracted with 80% Methanol/20% dH2O, and the 2-HG level are measured by RapidFireTM Mass spectroscopy.
動物実験 動物モデル female BALB/c Nude mice, male CD-1 mouse
投薬量 5, 12.5, 25, 50, 100 mg/kg
投与方法 Oral gavage

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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