Olutasidenib

製品コードS8949 バッチS894901

印刷

化学情報

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

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	3.550mg/ml (10.01mM)	Taking the 1 mL working solution as an example, add 50 μL of 71 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.590mg/ml (1.66mM)	Taking the 1 mL working solution as an example, add 50 μL of 11.8 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <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 this compound could be efficacious against most IDH1-R132 mutant-expressing tumors. It 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, this compound 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. This chemical 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 this compound 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

参考

https://pubmed.ncbi.nlm.nih.gov/31971798/

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。