AZD9496

Orukọ Kemikali:

(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) akiriliki acid

KỌỌDỌ SMILES:

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

Bọtini InChi:

DFBDRVGWBHBJNR-BBNFHIFMSA-N

Koko-ọrọ:

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

Solubility:Tiotuka ni DMSO

Ibi ipamọ:0 - 4°C fun igba kukuru (ọjọ si awọn ọsẹ), tabi -20°C fun igba pipẹ (osu)

Apejuwe:

AZD 9496 jẹ agbara ati yiyan estrogen receptor downregulator (SERD) pẹlu iye IC50 kan ti 0.138 nM fun isọdọtun estrogen receptor α (ERa). O jẹ yiyan fun ERα akawe si awọn olugba homonu iparun miiran pẹlu awọn iye IC50 ti 0.0008, 0.54, 9.2, ati 30 μM fun ERα, progesterone receptor (PR), glucocorticoid receptor (GR), ati androgen receptor (AR), lẹsẹsẹ. AZD 9496 dinku iṣẹ-ṣiṣe ERα (IC50 = 0.282 nM), ti a ṣewọn nipasẹ titobi ti iṣẹ-ṣiṣe PR ti o wa ni isalẹ, ati pe o dinku ilọsiwaju ti MCF-7 awọn sẹẹli alakan igbaya (IC50 = 0.0398 nM). O tun ṣe idiwọ idagbasoke MCF-7 xenograft ninu awọn eku ni ọna ti o gbẹkẹle iwọn lilo. AZD 9496 wa ni ẹnu bioavailable ati awọn agbekalẹ ti o ni ninu rẹ wa labẹ iwadii ni awọn idanwo ile-iwosan fun itọju ER akàn igbaya rere.

afojusun: SERD