PQR530

Orukọ Kemikali:

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

KỌỌDỌ SMILES:

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

Koodu InChi:

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

Bọtini InChi:

SYKBZXMKAPICSO-NSHDSACASA-N

Koko-ọrọ:

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

Solubility:Tiotuka ni DMSO

Ibi ipamọ:0 - 4°C fun igba kukuru (ọjọ si awọn ọsẹ), tabi -20°C fun igba pipẹ (osu).

Apejuwe:

PQR530 jẹ oludena pan-PI3K/mTORC1/2 meji ti o lagbara pupọ. PQR530 ṣe idiwọ amuaradagba kinase B (PKB, pSer473) ati amuaradagba ribosomal S6 (pS6, pSer235/236) phosphorylation pẹlu awọn iye IC50 ti 0.07 µM. PQR530 ṣe afihan yiyan ti o dara julọ lori panẹli jakejado ti kinases, bakanna bi yiyan yiyan ti o dara julọ pẹlu awọn enzymu olugba ti ko ni ibatan ati awọn ikanni ion. Pẹlupẹlu, PQR530 ṣe afihan agbara ni nronu ti awọn laini sẹẹli alakan 44 (NTRC Oncolines TM) lati ṣe idiwọ idagbasoke sẹẹli alakan (itumọ iye fun GI50 ti 426 nM). Ohun elo ẹnu ti PQR530 si awọn eku yorisi ni iwọn-iwọn iwọn PK ati ṣafihan bioavailability ti ẹnu ti o dara ati ilaluja ọpọlọ to dara julọ.

Àfojúsùn: PI3K/mTOR