PQR530
Iinkcukacha zeMveliso
Iithegi zeMveliso
| Ubungakanani bePakethi | Ubukho | Ixabiso (USD) |
| 100mg | Ikhona evenkileni | 500 |
| 500mg | Ikhona evenkileni | 800 |
| 1g | Ikhona evenkileni | 1200 |
| Iisayizi ezininzi | Fumana iiQuotes | Fumana iiQuotes |
Igama leMchiza:
(S) -4-(difluoromethyl)-5-(4-(3-methylmorpholino)-6-morpholino-1,3,5-triazin-2-yl)pyridin-2-amine
Ikhowudi yoncumo:
NC1=NC=C(C2=NC(N3[C@@H](C)COCC3)=NC(N4CCOCC4)=N2)C(C(F)F)=C1
Ikhowudi ye-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
Isitshixo se-InChi:
SYKBZXMKAPICSO-NSHDSACASA-N
Igama elingundoqo:
PQR530, PQR-530, PQR 530, 1927857-61-1
Ukunyibilika:Inyibilika kwi-DMSO
Ugcino:0 - 4°C ixesha elifutshane (iintsuku ukuya kwiiveki), okanye -20°C ixesha elide (iinyanga).
Inkcazo:
I-PQR530 yi-dual inhibitor enamandla kakhulu-PI3K/mTORC1/2. I-PQR530 inhibited protein kinase B (PKB, pSer473) kunye ne-ribosomal protein S6 (pS6, pSer235/236) i-phosphorylation ene-IC50 ixabiso le-0.07 µM. I-PQR530 ibonise ukukhetha okugqwesileyo kwiphaneli ebanzi ye-kinases, kunye nokukhetha okugqwesileyo xa kuthelekiswa ne-enzymes ze-receptor ezinganxulumananga kunye nemijelo ye-ion. Ngaphezu koko, i-PQR530 ibonise amandla kwiphaneli ye-44 imigca yeseli yomhlaza (NTRC Oncolines TM) ukukhusela ukukhula kweseli yomhlaza (ixabiso elithetha nge-GI50 ye-426 nM). Ukusetyenziswa komlomo kwe-PQR530 kwiimpuku kubangele i-PK ye-dose-proportional kwaye yabonisa i-bioavailability yomlomo efanelekileyo kunye nokungena kwengqondo okugqwesileyo.
Ithagethi: PI3K/mTOR
