PQR530

Izina ryimiti:

(S) -4- (difluoromethyl) -5- (4-

Kode ya SMILES:

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 Urufunguzo:

SYKBZXMKAPICSO-NSHDSACASA-N

Ijambo ryibanze:

PQR530, PQR-530, PQR 530, 1927857-61-1

Gukemura:Gukemura muri DMSO

Ububiko:0 - 4 ° C mugihe gito (iminsi kugeza ibyumweru), cyangwa -20 ° C mugihe kirekire (amezi).

Ibisobanuro:

PQR530 ninzitizi ikomeye cyane pan-PI3K / mTORC1 / 2 inhibitor. PQR530 yabujije protein kinase B (PKB, pSer473) na poroteyine ya ribosomal S6 (pS6, pSer235 / 236) fosifora hamwe na IC50 ifite agaciro ka 0.07 µM. PQR530 yerekanye uburyo bwiza bwo guhitamo hejuru yumurongo mugari wa kinase, kimwe no guhitamo neza hamwe na enzymes za reseptor zidafitanye isano hamwe numuyoboro wa ion. Byongeye kandi, PQR530 yerekanye imbaraga mumurongo wumurongo wa kanseri 44 (NTRC OncolinesTM) kugirango wirinde gukura kwa kanseri (bivuze agaciro ka GI50 ya 426 nM). Gukoresha umunwa PQR530 ku mbeba byavuyemo igipimo cya PK kandi kigaragaza neza bioavailable yo mu kanwa no kwinjira neza mu bwonko.

Intego: PI3K / mTOR