AZD9496

Magaca Kiimikada:

(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

Koodhka dhoola cadeynta:

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

Koodhka 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

Furaha InChi:

DFBDRVGWBHBJNR-BBNFHIFMSA-N

Ereyga muhiimka ah:

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

Xalka:Ku milmay DMSO

Kaydinta:0 - 4°C muddo gaaban (maalmo ilaa toddobaadyo), ama -20°C muddo dheer (bilo)

Sharaxaad:

AZD 9496 waa mid awood leh oo la xushay estrogen receptor downregulator (SERD) oo leh qiimaha IC50 ee 0.138 nM ee hoos u dhigista estrogen receptor α (ERa). Waxay u doorataa ERα marka la barbardhigo kuwa kale ee hormoonnada nukliyeerka ah ee leh IC50 ee 0.0008, 0.54, 9.2, iyo 30 μM ee ERα, progesterone receptor (PR), glucocorticoid receptor (GR), iyo androgen receptor (AR), siday u kala horreeyaan. AZD 9496 waxay hoos u dhigtaa dhaqdhaqaaqa ERα (IC50 = 0.282 nM), oo lagu qiyaaso qiyaasta waxqabadka PR ee hoose, waxayna yaraynaysaa kororka unugyada kansarka naasaha ee MCF-7 (IC50 = 0.0398 nM). Waxa kale oo ay xakameysaa korriinka MCF-7 xenograft ee jiirarka iyadoo loo eegayo qiyaasta qiyaasta. AZD 9496 waa afka laga heli karo oo qaabab ay ku jirto ayaa lagu baarayaa tijaabooyinka kiliinikada ee daaweynta kansarka naasaha ee togan ee ER.

Ujeedka: SERD