2230263-60-0

Name	2H-Pyrimido[4,5-d][1,3]oxazin-2-one, 7-[[(1S)-1-[4-[(1S)-2-cyclopropyl-1-[4-(1-oxo-2-propen-1-yl)-1-piperazinyl]ethyl]phenyl]ethyl]amino]-1-ethyl-1,4-dihydro-
CAS	2230263-60-0
Molecular Formula	C28H36N6O3
Molecular Weight	504.62
MOL File	2230263-60-0.mol

Synonyms

Mutant IDH1-IN-6 2H-Pyrimido[4,5-d][1,3]oxazin-2-one, 7-[[(1S)-1-[4-[(1S)-2-cyclopropyl-1-[4-(1-oxo-2-propen-1-yl)-1-piperazinyl]ethyl]phenyl]ethyl]amino]-1-ethyl-1,4-dihydro-

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Chemical Properties

Boiling point	704.2±70.0 °C(Predicted)
density	1.251±0.06 g/cm3(Predicted)
pka	6.73±0.10(Predicted)

Hazard Information

Uses

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].

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].

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.

IC 50

IDH1; IDH2

References

[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.

Spectrum Detail

2H-Pyrimido[4,5-d][1,3]oxazin-2-one, 7-[[(1S)-1-[4-[(1S)-2-cyclopropyl-1-[4-(1-oxo-2-propen-1-yl)-1-piperazinyl]ethyl]phenyl]ethyl]amino]-1-ethyl-1,4-dihydro-(2230263-60-0)¹HNMR

Supplier

WUHAN SUN-SHINE BIO-TECHNOLOGY Co., Ltd.

Telephone17702719238

Websitehttp://www.sun-shinechem.com/

Shandong Dayou Pharmaceutical Research and Development Co., Ltd.

Telephonedayouchem@126.com 15165037910

Website

TargetMol Chemicals Inc.

Telephone 15002134094

Websitehttps://www.targetmol.cn/

Shanghai Amole Biotechnology Co., Ltd.

Telephone13370042665 18916960931

Websitehttps://www.amole.com.cn/

Beijing RuiDaHengHui Science&Technology Development Co., LTD

Telephone010-64126590-807 13031133168

Websitehttps://www.henghuimall.com/articles/305.html

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