AZD9496

Lebitso la lik'hemik'hale:

(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 Khouto:

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

Khoutu ea 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

Keyword:

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

Sollubility:E qhibiliha ka DMSO

Polokelo:0 - 4 ° C bakeng sa nako e khutšoanyane (matsatsi ho isa libeke), kapa -20 ° C bakeng sa nako e telele (likhoeli)

Tlhaloso:

AZD 9496 ke e matla le e khethang ea estrogen receptor downregulator (SERD) e nang le boleng ba IC50 ba 0.138 nM bakeng sa ho fokotseha ha estrogen receptor α (ERα). E khetha ERα ha e bapisoa le li-receptor tse ling tsa nyutlelie tse nang le litekanyetso tsa IC50 tsa 0.0008, 0.54, 9.2, le 30 μM bakeng sa ERα, progesterone receptor (PR), glucocorticoid receptor (GR), le androgen receptor (AR), ka ho latellana. AZD 9496 e fokotsa ts'ebetso ea ERα (IC50 = 0.282 nM), e lekantsoeng ka quantification ea ts'ebetso ea PR e tlase, 'me e fokotsa ho ata ha lisele tsa kankere ea matsoele tsa MCF-7 (IC50 = 0.0398 nM). E boetse e thibela kholo ea MCF-7 xenograft ho litoeba ka mokhoa o itšetlehileng ka lethal dose. AZD 9496 e fumaneha ka molomo 'me metsoako e nang le eona e ntse e etsoa lipatlisiso litekong tsa bongaka bakeng sa phekolo ea mofetše oa matsoele oa ER.

Sepheo: SERD