PQR-530

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

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.

Name	PQR530
Synonym	More Synonyms

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).

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)

Name: Intrinsic clearance in dog hepatocytes assessed per 10'6 cells
Source: ChEMBL
Target: N/A
External Id: CHEMBL4360978

Name: Intrinsic clearance in rat hepatocytes assessed per 10'6 cells
Source: ChEMBL
Target: N/A
External Id: CHEMBL4360977

Name: Intrinsic clearance in human hepatocytes assessed per 10'6 cells
Source: ChEMBL
Target: N/A
External Id: CHEMBL4360976

Name: Metabolic stability in human liver microsomes assessed as compound remaining after 30...
Source: ChEMBL
Target: N/A
External Id: CHEMBL4360975

Name: Metabolic stability in rat liver microsomes assessed as compound remaining after 30 m...
Source: ChEMBL
Target: N/A
External Id: CHEMBL4360974

Name: Metabolic stability in dog liver microsomes assessed as compound remaining after 30 m...
Source: ChEMBL
Target: N/A
External Id: CHEMBL4360973

Name: Metabolic stability in mouse liver microsomes assessed as compound remaining after 30...
Source: ChEMBL
Target: N/A
External Id: CHEMBL4360972

Name: Inhibition of Wortmannin covalent binding to N-terminal His-tagged recombinant human ...
Source: ChEMBL
Target: Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
External Id: CHEMBL4360971

Name: Terminal half-life in C57BL/6J mouse plasma at 50 mg/kg, po administered as single do...
Source: ChEMBL
Target: N/A
External Id: CHEMBL4360986

Name: Tmax in C57BL/6J mouse plasma at 50 mg/kg, po administered as single dose by LC-MS an...
Source: ChEMBL
Target: N/A
External Id: CHEMBL4360985

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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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Shanghai Nianxing Industrial Co., Ltd
China
Product Name: PQR530
Price: Check
Purity: 98.0%
Delivery: 10 Day
Contact: Yang
Email: sales@echemcloud.com

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Chemical & Physical Properties

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Synonyms

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.