PQR530

Magaca Kiimikada:

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

Koodhka dhoola cadeynta:

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

Koodhka InChi:

InChi=1S/C18H23F2N7O2/c1-11-10-29-7-4-27(11)18-24-16(13-9-22-14(21)8-12(13)15(1) 9)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

Furaha InChi:

SYKBZXMKAPICSO-NSHDSACASA-N

Ereyga muhiimka ah:

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

Xalka:Ku milmay DMSO

Kaydinta:0 - 4°C muddo gaaban (maalmo ilaa toddobaadyo), ama -20°C muddo dheer (bilo).

Sharaxaad:

PQR530 waa pan-PI3K/mTORC1/2 inhibitor aad u xoog badan. PQR530 waxay joojisay borotiinka kinase B (PKB, pSer473) iyo borotiinka ribosomal S6 (pS6, pSer235/236) fosforyaalka leh IC50 qiyamka 0.07 µM. PQR530 waxay muujisay xulasho heer sare ah oo ka badan guddi ballaaran oo kinases ah, iyo sidoo kale xulasho aad u wanaagsan oo ka soo horjeeda enzymes soo dhaweynta aan la xiriirin iyo kanaalka ion. Waxaa intaa dheer, PQR530 waxay soo bandhigtay awoodda koox ka kooban 44 khadadka unugyada kansarka (NTRC OncolinesTM) si looga hortago koritaanka unugyada kansarka (qiimaha celceliska GI50 ee 426 nM). Codsiga afka ee PQR530 ee jiirarka waxay keentay qiyaas-qiyaasta PK waxayna muujisay bioavailability afka oo wanaagsan iyo dhexgalka maskaxda oo aad u wanaagsan.

Hadafka: PI3K/mTOR