AZD9496

Aha kemịkalụ:

(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

Koodu Ọchịchọ:

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

Koodu 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

Igodo InChi:

DFBDRVGWBHBJNR-BBNFHIFMSA-N

Okwu:

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

Solubility:Soluble na DMSO

Nchekwa:0 - 4 Celsius C maka obere oge (ụbọchị ruo izu), ma ọ bụ -20 Celsius maka ogologo oge (ọnwa)

Nkọwa:

AZD 9496 bụ onye na-emepụta estrogen receptor downregulator (SERD) na-ahọrọ nke nwere uru IC50 nke 0.138 nM maka nkwụsị nke estrogen receptor α (ERa). Ọ bụ nhọrọ maka ERα ma e jiri ya tụnyere ndị na-anabata hormone nuklia ndị ọzọ nwere ụkpụrụ IC50 nke 0.0008, 0.54, 9.2, na 30 μM maka ERα, progesterone receptor (PR), glucocorticoid receptor (GR), na androgen receptor (AR), n'otu n'otu. AZD 9496 na-ebelata ọrụ ERα (IC50 = 0.282 nM), nke a tụrụ site na ọnụọgụ nke ọrụ PR dị ala, ma na-ebelata mmụba nke mkpụrụ ndụ cancer ara MCF-7 (IC50 = 0.0398 nM). Ọ na-egbochikwa uto MCF-7 xenograft na ụmụ oke na usoro dabere na dose. A na-enyocha AZD 9496 n'ọnụ ọnụ yana usoro ndị nwere ya na-enyocha nyocha ụlọ ọgwụ maka ọgwụgwọ ọrịa kansa ara ER.

Ebumnuche: SERD