Saukewa: AZD9496

Sunan Sinadari:

(E) -3- (3,5-difluoro-4- ((1R,3R)-2- (2-fluoro-2-methylpropyl) -3-methyl-2,3,4,9-tetrahydro-1H- pyrido[3,4-b]indol-1-yl) phenyl) acrylic acid

Lambar 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

Lambar InChi:

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 Key:

DFBDRVGWBHBJNR-BBNFHIFMSA-N

Mabuɗin kalma:

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

Solubility:Mai narkewa a cikin DMSO

Ajiya:0 - 4 ° C na gajeren lokaci (kwanaki zuwa makonni), ko -20 ° C na dogon lokaci (watanni)

Bayani:

AZD 9496 mai ƙarfi ne da zaɓaɓɓen mai karɓar isrogen receptor downregulator (SERD) tare da ƙimar IC50 na 0.138 nM don ragewar isrogen receptor α (ERa). Yana da zaɓi don ERα idan aka kwatanta da sauran masu karɓar hormone na nukiliya tare da ƙimar IC50 na 0.0008, 0.54, 9.2, da 30 μM don ERα, progesterone receptor (PR), glucocorticoid receptor (GR), da androgen receptor (AR), bi da bi. AZD 9496 yana rage ayyukan ERα (IC50 = 0.282 nM), wanda aka auna ta hanyar ƙididdige ayyukan PR na ƙasa, kuma yana rage yaduwar ƙwayar cutar ciwon nono MCF-7 (IC50 = 0.0398 nM). Hakanan yana hana MCF-7 xenograft girma a cikin mice a cikin hanyar dogaro da kashi. AZD 9496 yana samuwa a baki kuma ana gudanar da gwaje-gwajen da ke dauke da shi a cikin gwaje-gwajen asibiti don maganin cutar sankarar nono mai kyau na ER.

manufa: SERD