PQR530

Lub npe tshuaj:

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

SMILES Code:

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

InChi Code:

InChI = 1S/C18H23F2N7O2/c1-11-10-29-7-4-27(11)18-24-16(13-9-22-14(21)8-12(13)15(19)20) 23-17(25-18)26-2-5-28-6-3-26/h8-9,11,15H,2-7,10H2,1H3,(H2,21,22)/t11-/m0 /s1

InChi Key:

SYKBZXMKAPICSO-NSHDSACASA-N

Lo lus tseem ceeb:

PQR 530, PQR-530, PQR 530, 1927857-61-1

Solubility:Soluble hauv DMSO

Cia:0 - 4 ° C rau lub sijhawm luv (hnub mus rau lub lis piam), lossis -20 ° C rau lub sijhawm ntev (hli).

Nqe lus piav qhia:

PQR530 yog lub zog muaj zog dual yias-PI3K / mTORC1 / 2 inhibitor. PQR530 inhibited protein kinase B (PKB, pSer473) thiab ribosomal protein S6 (pS6, pSer235/236) phosphorylation nrog IC50 qhov tseem ceeb ntawm 0.07 µM. PQR530 tau pom kev xaiv zoo tshaj plaws ntawm ntau lub vaj huam sib luag ntawm kinases, nrog rau kev xaiv zoo heev tiv thaiv cov receptor enzymes tsis sib xws thiab ion channels. Ntxiv mus, PQR530 tau tso tawm qhov muaj zog hauv lub vaj huam sib luag ntawm 44 kab mob qog noj ntshav (NTRC OncolinesTM) los tiv thaiv kev mob qog noj ntshav (txhais tau tus nqi rau GI50 ntawm 426 nM). Kev siv qhov ncauj ntawm PQR530 rau cov nas ua rau muaj qhov sib npaug ntawm cov koob tshuaj PK thiab ua kom pom qhov zoo ntawm qhov ncauj bioavailability thiab kev nkag mus rau lub hlwb zoo heev.

Lub hom phiaj: PI3K / mTOR