PQR-530

Modify Date: 2025-09-11 15:51:00

PQR-530 Structure
PQR-530 structure
Common Name PQR-530
CAS Number 1927857-61-1 Molecular Weight 407.42
Density 1.338±0.06 g/cm3 Boiling Point N/A
Molecular Formula C18H23F2N7O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of PQR-530


PQR-530 is a potent, oral and brain-penetrant dual pan-PI3K/mTORC1/2 inhibitor, exhibiting antitumor activity.

 Names

Name PQR530
Synonym More Synonyms

 PQR-530 Biological Activity

Description PQR-530 is a potent, oral and brain-penetrant dual pan-PI3K/mTORC1/2 inhibitor, exhibiting antitumor activity.
Related Catalog
Target

PI3K

mTORC1

mTORC2

In Vitro PQR-530 is a potent, oral and brain-penetrant dual pan-PI3K/mTORC1/2 inhibitor, exhibiting antitumor activity. PQR-530 inhibits all PI3K isoforms and mTOR complexes C1/2 potently and selectively. PQR-530 inhibits protein kinase B (PKB, pSer473) and ribosomal protein S6 (pS6, pSer235/236) phosphorylation with IC50 values of 0.07 µM in A2058 melanoma cells. PQR-530 shows inhibitory activity against the growth of 44 cancer cell lines with mean GI50 of 426 nM[1].
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).

 Chemical & Physical Properties

Density 1.338±0.06 g/cm3
Molecular Formula C18H23F2N7O2
Molecular Weight 407.42
InChIKey SYKBZXMKAPICSO-NSHDSACASA-N
SMILES CC1COCCN1c1nc(-c2cnc(N)cc2C(F)F)nc(N2CCOCC2)n1
Water Solubility Practically insoluble (0.057 g/L) (25 ºC)

 Synonyms

CPD1536
PQR-530
4-(Difluoromethyl)-5-[4-[(3S)-3-methyl-4-morpholinyl]-6-(4-morpholinyl)-1,3,5-triazin-2-yl]-2-pyridinamine
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