1927857-98-4

Name	2-Pyridinamine, 4-(difluoromethyl)-5-[4-[(3R,5S)-3,5-dimethyl-4-morpholinyl]-6-[(3R)-3-methyl-4-morpholinyl]-1,3,5-triazin-2-yl]-
CAS	1927857-98-4
Molecular Formula	C20H27F2N7O2
Molecular Weight	435.47
MOL File	1927857-98-4.mol

Synonyms

PQR626 2-Pyridinamine, 4-(difluoromethyl)-5-[4-[(3R,5S)-3,5-dimethyl-4-morpholinyl]-6-[(3R)-3-methyl-4-morpholinyl]-1,3,5-triazin-2-yl]-

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Chemical Properties

Boiling point	655.4±65.0 °C(Predicted)
density	1.264±0.06 g/cm3(Predicted)
form	Solid
pka	5.05±0.10(Predicted)
color	Light yellow to yellow

Hazard Information

Description

PQR626 is a Potent, Orally Available, and Brain-Penetrant mTOR Inhibitor for the Treatment of Neurological Disorders.

Uses

PQR626, a rapamycin derivative, is a potent, selective, orally active, and brain-penetrant mTOR inhibitor, with an IC50 and Ki of 5 nM and 3.6 nM, respectively. PQR626 can be can be used for the research of neurological disorders[1][2].

in vivo

PQR626 (10-50 mg/kg; twice a day; for 90 days) reduces the loss of Tsc1-induced mortality as compared to vehicle^[2].
PQR626 exhibits terminal elimination half-life (mice 3.0 h) due to high plasma clearance (1096 ng/mL) following oral dosing (10 mg/kg; p.o.; daily; for 4 days)^[2].

Animal Model:	BALB/c nude female mice, Tsc1^GFAP CKO mice model^[2]
Dosage:	10 mg/kg, 25 mg/kg, 50 mg/kg
Administration:	Oral administration, twice a day, for 90 days
Result:	Significantly reduced the loss of Tsc1-induced mortality.

Animal Model:	Female C57BL/6J Mice^[1]
Dosage:	10 mg/kg (Pharmacokinetic Analysis)
Administration:	Oral administration, daily, for 4 days
Result:	C_max (1096 ng/mL), T_1/2 (3.0 h).

References

[1] Denise RAGEOT, et al. Treatment of neurological disorders. WO2017198346A1.
[2] Chiara Borsari, et al. 4-(Difluoromethyl)-5-(4-((3 R,5 S)-3,5-dimethylmorpholino)-6-(( R)-3-methylmorpholino)-1,3,5-triazin-2-yl)pyridin-2-amine (PQR626), a Potent, Orally Available, and Brain-Penetrant mTOR Inhibitor for the Treatment of Neurological Disorders. J Med Chem. 2020 Nov 25;63(22):13595-13617. DOI:10.1021/acs.jmedchem.0c00620

Supplier

ShangHai Caerulum Pharma Discovery Co., Ltd.

Telephone18149758185 18149758185

Websitehttp://www.caerulumpharma.com

Shanghai YuanYe Biotechnology Co., Ltd.

Telephone 15026964105

Websitehttps://www.shyuanye.com

TargetMol Chemicals Inc.

Telephone4008200310 15002144251

Websitehttps://www.targetmol.cn/

Suzhou Meidi Senuo Pharmaceutical Technology Co., Ltd.

Telephone 13771642864

Websitehttps://www.chemicalbook.com/ShowSupplierProductsList1659441/0_EN.htm

RD International Technology Co., Limited

Telephone 18024082417

Websitehttps://www.ruidiresearch.com

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