AZD9496

Izina ryimiti:

(E) -3- (3,5-difluoro-4 - (((1R, 3R) -2- pyrido [3,4-b] indol-1-yl) fenyl) acide acrylic

Kode ya SMILES:

O = C (O) / C = C / C1 = CC (F) = C ([C @ H] 2N (CC (C) (F) C) [C @ H] (C) CC3 = C2NC4 = C3C = CC = C4) C (F) = C1

InChi Code:

InChI = 1S / C25H25F3N2O2 / c1-14-10-17-16-6-4-5-7-20 (16) 29-23 (17) 24 (30 (14) 13-25 (2,3) 28) 22-18 (26) 11 -15 (12-19 (22) 27) 8-9-21 (31) 32 / h4-9,11-12,14,24,29H, 10,13H2,1-3H3, (H, 31,32) / b9-8 + / t14-, 24- / m1 / s1

InChi Urufunguzo:

DFBDRVGWBHBJNR-BBNFHIFMSA-N

Ijambo ryibanze:

AZD9496, AZD-9496, AZD 9496, 1639042-08-2

Gukemura:Gukemura muri DMSO

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

Ibisobanuro:

AZD 9496 ni igenzura rikomeye kandi ryatoranijwe rya resitora ya estrogene (SERD) ifite IC50 ifite agaciro ka 0.138 nM kuri resitora ya estrogene α (ERα). Ihitamo ERα ugereranije nizindi misemburo ya hormone yakira ifite agaciro ka IC50 ifite 0.0008, 0.54, 9.2, na 30 μM kuri ERα, reseptor progesterone (PR), reseptor glucocorticoid (GR), na reseptor ya androgene (AR). AZD 9496 igabanya ibikorwa bya ERα (IC50 = 0.282 nM), bipimwa hakoreshejwe umubare wibikorwa bya PR byo hepfo, kandi bigabanya ikwirakwizwa rya selile kanseri y'ibere MCF-7 (IC50 = 0.0398 nM). Irabuza kandi gukura kwa MCF-7 xenograft mu mbeba muburyo butandukanye. AZD 9496 irashobora kuboneka mu kanwa kandi ibisobanuro birimo birimo gukorwaho iperereza mu mavuriro yo kuvura kanseri y'ibere ya ER.

Intego: SERD