PQR530
- Product Name
- PQR530
- CAS No.
- 1927857-61-1
- Chemical Name
- PQR530
- Synonyms
- PQR530;CPD1536;PQR530, 10 mM in DMSO;PQR530;PQR 530;PQR-530;(S)-4-(Difluoromethyl)-5-(4-(3-methylmorpholino)-6-morpholino-1,3,5-triazin-2-yl)pyridin-2-amine;PQR 530,Inhibitor,PQR530,Phosphoinositide 3-kinase,PI3K,inhibit,Mammalian target of Rapamycin,mTOR;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]-
- CBNumber
- CB03362615
- Molecular Formula
- C18H23F2N7O2
- Formula Weight
- 407.42
- MOL File
- 1927857-61-1.mol
PQR530 Property
- 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
N-Bromosuccinimide Price
- Product number
- CS-0028216
- Product name
- PQR530
- Purity
- 99.93%
- Packaging
- 5mg
- Price
- $200
- Updated
- 2021/12/16
- Product number
- CS-0028216
- Product name
- PQR530
- Purity
- 99.93%
- Packaging
- 10mg
- Price
- $300
- Updated
- 2021/12/16
- Product number
- PRK0000451
- Product name
- (S)-4-(DIFLUOROMETHYL)-5-(4-(3-METHYLMORPHOLINO)-6-MORPHOLINO-1,3,5-TRIAZIN-2-YL)PYRIDIN-2-AMINE
- Purity
- 95.00%
- Packaging
- 5MG
- Price
- $450.27
- Updated
- 2021/12/16
- Product number
- CS-0028216
- Product name
- PQR530
- Purity
- 99.93%
- Packaging
- 25mg
- Price
- $550
- Updated
- 2021/12/16
- Product number
- CS-0028216
- Product name
- PQR530
- Purity
- 99.93%
- Packaging
- 50mg
- Price
- $850
- Updated
- 2021/12/16
PQR530 Chemical Properties,Usage,Production
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)
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