1927857-61-1

1927857-61-1 structure

Name: PQR-530
Chemical Name: PQR530
CAS Number: 1927857-61-1
Molecular Formula: C₁₈H₂₃F₂N₇O₂
Molecular Weight: 407.42
Catalog: Research Areas Cancer
Create Date: 2018-06-04 03:00:15
Modify Date: 2024-01-02 15:54:02
PQR-530 is a potent, oral and brain-penetrant dual pan-PI3K/mTORC1/2 inhibitor, exhibiting antitumor activity.

Name	PQR530
Synonyms	CPD1536 PQR-530 4-(Difluoromethyl)-5-[4-[(3S)-3-methyl-4-morpholinyl]-6-(4-morpholinyl)-1,3,5-triazin-2-yl]-2-pyridinamine

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