AZD9496

Chemical Name:

(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

SMILES Kodhi:

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

InChi Code:

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

InChi Key:

DFBDRVGWBHBJNR-BBNFHIFMSA-N

Keyword:

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

Solubility:Soluble muDMSO

Kuchengeta:0 - 4 ° C kwenguva pfupi (mazuva kusvika mavhiki), kana -20 ° C kwenguva refu (mwedzi)

Tsanangudzo:

AZD 9496 ine simba uye inosarudza estrogen receptor downregulator (SERD) ine IC50 kukosha kwe0.138 nM yeestrogen receptor α (ERα) kuderedza. Inosarudza ERα kana ichienzaniswa nemamwe mahomoni enyukireya ane IC50 maitiro e0.0008, 0.54, 9.2, uye 30 μM yeERα, progesterone receptor (PR), glucocorticoid receptor (GR), uye androgen receptor (AR), maererano. AZD 9496 inoderedza ERα chiitiko (IC50 = 0.282 nM), inoyerwa kuburikidza nehuwandu hwekudzika kwePR chiitiko, uye inoderedza kuwanda kweMCF-7 cancer cancer maseru (IC50 = 0.0398 nM). Iyo inodzivisawo MCF-7 xenograft kukura mumakonzo nenzira inoenderana nedosi. AZD 9496 inowanikwa nemuromo uye magadzirirwo anayo ari kuferefetwa mumakiriniki ekuedzwa kwekurapa gomarara rezamu reER.

Chinangwa: SERD