I-PQR530

Igama Lekhemikhali:

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

Ikhodi ye-SMILES:

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

Ikhodi ye-InChi:

I-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

I-InChi Key:

I-SYKBZXMKAPICSO-NSHDSACASA-N

Igama elingukhiye:

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

Ukunyibilika:I-Soluble ku-DMSO

Isitoreji:0 - 4°C isikhathi esifushane (izinsuku ukuya emavikini), noma -20°C isikhathi eside (izinyanga).

Incazelo:

I-PQR530 iyi-dual inhibitor ekabili ye-pan-PI3K/mTORC1/2 enamandla kakhulu. I-PQR530 inhibited protein kinase B (PKB, pSer473) kanye ne-ribosomal protein S6 (pS6, pSer235/236) phosphorylation enamanani e-IC50 angu-0.07 µM. I-PQR530 ibonise ukukhetha okuhle kakhulu phezu kwephaneli elibanzi lama-kinases, kanye nokukhetha okuhle kakhulu ngokumelene nama-enzyme e-receptor angahlobene namashaneli e-ion. Ngaphezu kwalokho, i-PQR530 ibonise amandla kuphaneli yemigqa yamaseli omdlavuza we-44 (NTRC OncolinesTM) ukuvimbela ukukhula kwamangqamuzana omdlavuza (inani elisho ukuthi i-GI50 ye-426 nM). Ukusetshenziswa ngomlomo kwe-PQR530 kumagundane kubangele i-PK yokulinganisa umthamo futhi kwabonisa i-bioavailability yomlomo enhle kanye nokungena okuhle kakhulu kobuchopho.

Ithagethi: PI3K/mTOR