I-AZD9496

Igama leMchiza:

(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

Ikhowudi yoncumo:

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

Ikhowudi ye-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

Isitshixo se-InChi:

DFBDRVGWBHBJNR-BBNFHIFMSA-N

Igama elingundoqo:

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

Ukunyibilika:Inyibilika kwi-DMSO

Ugcino:0 - 4°C ixesha elifutshane (iintsuku ukuya kwiiveki), okanye -20°C ixesha elide (iinyanga)

Inkcazo:

I-AZD 9496 inamandla kwaye ikhethiweyo ye-estrogen receptor downregulator (SERD) enexabiso le-IC50 le-0.138 nM ye-estrogen receptor α (ERα) yokunciphisa ukulawulwa. Ikhetha i-ERα xa kuthelekiswa nezinye ii-receptors ze-hormone zenyukliya kunye ne-IC50 ixabiso le-0.0008, i-0.54, i-9.2, kunye ne-30 μM ye-ERα, i-progesterone receptor (PR), i-glucocorticoid receptor (GR), kunye ne-androgen receptor (AR), ngokulandelanayo. I-AZD 9496 inciphisa umsebenzi we-ERα (IC50 = 0.282 nM), ilinganiswe ngobungakanani bomsebenzi we-PR osezantsi, kunye nokunciphisa ukwanda kweeseli zomhlaza webele we-MCF-7 (IC50 = 0.0398 nM). Ikwanqanda ukukhula kwe-MCF-7 xenograft kwiimpuku ngendlela exhomekeke kwidosi. I-AZD 9496 iyafumaneka ngomlomo kwaye imixube eyiquletheyo iphantsi kophando kulingo lwezonyango lomhlaza webele we-ER.

Ithagethi: ISERD