AZD9496

Nomen chemicum:

(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)acrylicum acidum

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

Keyword:

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

Solubilitas:Solutum in DMSO

Repono:0 - 4° C pro brevi termino (dies ad hebdomades), vel -20° C ad terminum longum (menses)

Descriptio:

AZD 9496 receptor downregulator (SERD) potent et selectivus est cum IC50 valore 0.138 nM pro estrogen receptor α (ERα) downregulation. Electivum est pro ERα comparatum cum aliis receptoribus nuclei hormonum cum IC50 valoribus 0.0008, 0.54, 9.2, et 30 µM pro ERα, progesterone receptore (PR), receptore glucocorticoideo (GR), et androgen receptore (AR), respective. AZD 9496 activitatem ERα decrescit (IC50 = 0,282 nM), per quantitatem amni PR activitatem mensuratur, et reducit multiplicationem cellularum MCF-7-cancri pectoris (IC50 = 0.0398 nM). Etiam MCF-7 xenografum incrementum murium in modum dosis dependens vetat. AZD 9496 viva voce bioavailable et formulae continentes eam sub investigatione in iudiciis clinicis ad curationem cancri pectoris ER positivi sunt.

Scopum: SERD