AZD9496

Ingoa matū:

(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)waikawa kiriaku

Waehere 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

Waehere 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

Kī InChi:

DFBDRVGWBHBJNR-BBNFHIFMSA-N

Kupumatua:

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

Wairewa:Wairewa i roto i te DMSO

Rokiroki:0 - 4°C mo te wa poto (ra ki nga wiki), -20°C ranei mo te wa roa (marama)

Whakaahuatanga:

Ko te AZD 9496 he kaha me te whiriwhiringa o te estrogen receptor downregulator (SERD) me te uara IC50 o 0.138 nM mo te whakahekenga o te estrogen receptor α (ERα). He mea whiriwhiri mo te ERα ka whakaritea ki etahi atu kaikawe homoni karihi me nga uara IC50 o 0.0008, 0.54, 9.2, me te 30 μM mo te ERα, te kaitautoko progesterone (PR), te kaiwhiwhi glucocorticoid (GR), me te kaitautoko androgen (AR), ia. Ko te AZD 9496 te whakaheke i te mahi ERα (IC50 = 0.282 nM), ka inehia ma te inenga o te mahi PR o raro, me te whakaheke i te tipu o te MCF-7 nga pukupuku pukupuku pukupuku (IC50 = 0.0398 nM). Ka aukati ano i te tipu o te xenograft MCF-7 i roto i nga kiore i runga i te tikanga inenga. Ko te AZD 9496 kei te waatea-a-waha me nga hanganga kei roto kei te tirotirohia i roto i nga whakamatautau haumanu mo te maimoatanga o te mate pukupuku u pai.

Whāinga: SERD