I-AZD9496

Igama Lekhemikhali:

(E)-3-(3,5-difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H- i-pyrido[3,4-b]indol-1-yl)phenyl)i-acrylic acid

Ikhodi ye-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

Ikhodi ye-InChi:

I-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

I-InChi Key:

DFBDRVGWBHBJNR-BBNFHIFMSA-N

Igama elingukhiye:

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

Ukunyibilika:I-Soluble ku-DMSO

Isitoreji:0 - 4°C isikhathi esifushane (izinsuku ukuya emavikini), noma -20°C isikhathi eside (izinyanga)

Incazelo:

I-AZD 9496 iyisilawuli esinamandla nesikhethayo se-estrogen receptor (SERD) enevelu ye-IC50 engu-0.138 nM yokwehlisa ukulawulwa kwe-estrogen receptor α (ERα). Iyakhetha i-ERα uma iqhathaniswa namanye ama-receptors e-nuclear hormone anamanani e-IC50 ka-0.0008, 0.54, 9.2, kanye ne-30 μM ye-ERα, i-progesterone receptor (PR), i-glucocorticoid receptor (GR), kanye ne-androgen receptor (AR), ngokulandelanayo. I-AZD 9496 yehlisa umsebenzi we-ERα (IC50 = 0.282 nM), ikalwa ngokulinganisa umsebenzi we-PR ongezansi, futhi yehlisa ukwanda kwamaseli omdlavuza webele we-MCF-7 (IC50 = 0.0398 nM). Iphinde ivimbele ukukhula kwe-MCF-7 xenograft kumagundane ngendlela encike kumthamo. I-AZD 9496 iyatholakala nge-bioavailable ngomlomo futhi amafomu aqukethe ayaphenywa ezivivinyweni zokwelashwa zokwelashwa komdlavuza webele we-ER.

Ithagethi: I-SERD