AZD9496

Dzina la Chemical:

(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

SMILES Kodi:

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 kodi:

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

Mawu ofunika:

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

Kusungunuka:Zosungunuka mu DMSO

Posungira:0 - 4 ° C kwa nthawi yochepa (masiku mpaka masabata), kapena -20 ° C kwa nthawi yaitali (miyezi)

Kufotokozera:

AZD 9496 ndi yamphamvu komanso yosankha estrogen receptor downregulator (SERD) yokhala ndi mtengo wa IC50 wa 0.138 nM kwa estrogen receptor α (ERα) kutsika. Imasankha ERα poyerekeza ndi ma receptor ena a nyukiliya okhala ndi IC50 milingo ya 0.0008, 0.54, 9.2, ndi 30 μM ya ERα, progesterone receptor (PR), glucocorticoid receptor (GR), ndi androgen receptor (AR), motsatira. AZD 9496 imachepetsa ntchito ya ERα (IC50 = 0.282 nM), yoyezedwa ndi kuchuluka kwa zochitika zapansi pa PR, komanso imachepetsa kuchuluka kwa maselo a khansa ya m'mawere ya MCF-7 (IC50 = 0.0398 nM). Zimalepheretsanso kukula kwa MCF-7 xenograft mu mbewa m'njira yodalira mlingo. AZD 9496 ndi yopezeka pakamwa ndipo mapangidwe ake akufufuzidwa m'mayesero azachipatala ochizira khansa ya m'mawere ya ER.

Cholinga: SERD