AZD9496

Igoa vaila'au:

(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 Code:

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 Key:

DFBDRVGWBHBJNR-BBNFHIFMSA-N

upu autu:

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

Solubility:Solu i le DMSO

Teuina:0 - 4°C mo taimi pupuu (aso i vaiaso), po'o le -20°C mo taimi uumi (masina)

Fa'amatalaga:

AZD 9496 o se estrogen receptor downregulator malosi ma filifilia (SERD) faʻatasi ai ma le tau IC50 o le 0.138 nM mo le faʻaogaina o le estrogen receptor α (ERα). E filifilia mo le ERα faʻatusatusa i isi faʻamaʻi faʻamaʻi faaniukilia faʻatasi ma IC50 tau o 0.0008, 0.54, 9.2, ma le 30 μM mo le ERα, faʻataʻitaʻiga o le progesterone (PR), glucocorticoid receptor (GR), ma le androgen receptor (AR), i le faasologa. AZD 9496 faʻaitiitia le gaioiga ERα (IC50 = 0.282 nM), fuaina e ala i le faʻatusatusaina o galuega PR i lalo, ma faʻaitiitia ai le faʻateleina o sela o le kanesa o le susu MCF-7 (IC50 = 0.0398 nM). E taofia ai foʻi le tuputupu aʻe o le xenograft MCF-7 i isumu i se fua faʻalagolago. O le AZD 9496 e mafai ona tu'u tautala ma fa'aputu o lo'o iai o lo'o su'esu'eina ile su'esu'ega ile falema'i mo togafitiga ole kanesa ole susu ole ER.

Sini: SERD