PQR-530( PQR530 )

Catalog No. M13022 CAS No. 1927857-61-1

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

PQR-530
Note

Research use only, not for human use.
Brief Description

PQR-530 (PQR530) is a potent, BBB penetrant, dual pan-PI3K/mTOR inhibitor.
Description

PQR-530 (PQR530) is a potent, BBB penetrant, dual pan-PI3K/mTOR inhibitor with Kd of 0.3/1/6/11/10 nM for mTOR/PIK3CA/PIK3CB/PIK3CD/PIK3CG, respectively; effectively cross the blood-brain barrier and increase seizure threshold in a mouse model of chronic epilepsy.
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.
In Vivo

——
Synonyms

PQR530
Pathway

PI3K/Akt/mTOR signaling
Target

PI3K
Recptor

PI3K
Research Area

Cancer
Indication

——

CAS Number

1927857-61-1
Formula Weight

407.42
Molecular Formula

C18H23F2N7O2
Purity

>98% (HPLC)
Solubility

In Vitro:?DMSO : 33.33 mg/mL (81.81 mM)
SMILES

NC1=NC=C(C2=NC(N3[C@@H](C)COCC3)=NC(N4CCOCC4)=N2)C(C(F)F)=C1
Chemical Name

(S)-4-(difluoromethyl)-5-(4-(3-methylmorpholino)-6-morpholino-1,3,5-triazin-2-yl)pyridin-2-amine

1. Brandt C, et al. Neuropharmacology. 2018 Aug 3;140:107-120.

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