| Identification | Back Directory | [Name]
PQR530 | [CAS]
1927857-61-1 | [Synonyms]
PQR530
CPD1536
PQR530;PQR 530;PQR-530
(S)-4-(Difluoromethyl)-5-(4-(3-methylmorpholino)-6-morpholino-1,3,5-triazin-2-yl)pyridin-2-amine
4-(difluoromethyl)-5-[4-[(3S)-3-methylmorpholin-4-yl]-6-morpholin-4-yl-1,3,5-triazin-2-yl]pyridin-2-amine
2-Pyridinamine, 4-(difluoromethyl)-5-[4-[(3S)-3-methyl-4-morpholinyl]-6-(4-morpholinyl)-1,3,5-triazin-2-yl]- | [Molecular Formula]
C18H23F2N7O2 | [MOL File]
1927857-61-1.mol | [Molecular Weight]
407.42 |
| Chemical Properties | Back Directory | [Boiling point ]
660.7±65.0 °C(Predicted) | [density ]
1.338±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 30 mg/ml; DMF:PBS (pH 7.2) (1:3): 0.33 mg/ml; DMSO: 10 mg/ml | [form ]
A crystalline solid | [pka]
5.05±0.10(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
PQR530 is a potent, ATP-competitive, orally bioavailable and brain-penetrant dual pan-PI3K/mTORC1/2 inhibitor, with a subnanomolar Kd toward PI3Kα and mTOR (0.84 and 0.33 nM, respectively). Antitumor activity[1][2]. | [IC 50]
mTOR: 0.33 nM (Kd); PI3Kα: 0.84 nM (Kd); PI3Kβ: 6.1 nM (Kd); PI3Kγ: 10 nM (Kd); PI3Kδ: 11 nM (Kd); PI3KC2β: 100 nM (Kd) | [storage]
Store at -20°C | [References]
[1] Denise Rageot, et al. Abstract 140: Discovery and biological evaluation of PQR530, a highly potent dual pan-PI3K/mTORC1/2 inhibitor. Cancer Res 2017;77(13 Suppl).
[2] Rageot D, et al. (S)-4-(Difluoromethyl)-5-(4-(3-methylmorpholino)-6-morpholino-1,3,5-triazin-2-yl)pyridin-2-amine (PQR530), a Potent, Orally Bioavailable, and Brain-Penetrable Dual Inhibitor of Class I PI3K and mTOR Kinase. J Med Chem. 2019;62(13):6241-62 DOI:10.1021/acs.jmedchem.9b00525 |
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| Company Name: |
Twochem Co.Ltd.
|
| Tel: |
021-58111628 15800915896 |
| Website: |
cn.twochem.com |
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