Mutant IDH1-IN-6

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Mutant IDH1-IN-6 

Mutant IDH1-IN-6 是一种有效的选择性的具有口服活性的突变型 IDH 抑制剂,对 IDH1 R132HIDH1 R132CIDH2 R140QIDH2 R172K 突变酶的 IC50 分别为 6.27 nM,3.71 nM,36.9 nM 和 11.5 nM。Mutant IDH1-IN-6 抑制 IDH 野生型酶的活性较低。

Mutant IDH1-IN-6

Mutant IDH1-IN-6 Chemical Structure

CAS No. : 2230263-60-0

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生物活性

Mutant IDH1-IN-6 is a potent, selective and orally active mutant isocitrate dehydrogenase (IDH) inhibitor with IC50s of 6.27 nM, 3.71 nM, 36.9 nM and 11.5 nM for IDH1 R132H, IDH1 R132C, IDH2 R140Q and IDH2 R172K mutant enzymes, respectively. Mutant IDH1-IN-6 is less active at inhibiting the IDH wild-type enzymes[1].

IC50 & Target

IC50: 6.27 nM (IDH1 R132H), 3.71 nM (IDH1 R132C), 36.9 nM (IDH2 R140Q), 11.5 nM (IDH2 R172K), 105 nM (IDH1 wild-type) and 884 nM (IDH2 wild-type)[1]

体外研究
(In Vitro)

Mutant IDH1-IN-6 (example 2) inhibits production of 2-hydroxyglutarate in HT1080 cells with an IC50 of 1.28 nM, indicating the inhibition of mutant IDHl R132C in cells. aKG, a metabolite generated by wild-type IDHl is not affected by Mutant IDH1-IN-6, indicating Mutant IDH1-IN-6 is selective for mutant IDHl over wild type IDHl in cells[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Mutant IDH1-IN-6 (Example 2; 0-32 mg/kg; oral gavage; twice daily; for 3 days) treatment inhibitis of 2-hydroxyglutarate in a dose-dependent manner in IDHl mutant xenograft mice[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Athymic nude mice (20-22 g) injected with TB08 cells[1]
Dosage: 1 mg/kg, 2 mg/kg, 4 mg/kg, 8 mg/kg, 16 mg/kg, 32 mg/kg
Administration: Oral gavage; twice daily; for 3 days
Result: Inhibitied of 2-hydroxyglutarate in IDHl mutant xenograft mice.

分子量

504.62

Formula

C28H36N6O3

CAS 号

2230263-60-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Renato Alejandro BAUER, et al. 7-phenylethylamino-4h-pyrimido[4,5-d][1,3]oxazin-2-one compounds as mutant idh1 and idh2 inhibitors. WO2018111707A1.

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