TIAB SA 9496

Lub npe tshuaj:

(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 Code:

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

Lo lus tseem ceeb:

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

Solubility:Soluble hauv DMSO

Cia:0 - 4 ° C rau lub sijhawm luv (hnub mus rau lub lis piam), lossis -20 ° C rau lub sijhawm ntev (hli)

Nqe lus piav qhia:

AZD 9496 yog lub zog thiab xaiv cov tshuaj estrogen receptor downregulator (SERD) nrog IC50 tus nqi ntawm 0.138 nM rau estrogen receptor α (ERα) downregulation. Nws yog xaiv rau ERα piv rau lwm cov tshuaj hormones receptors nrog IC50 qhov tseem ceeb ntawm 0.0008, 0.54, 9.2, thiab 30 μM rau ERα, progesterone receptor (PR), glucocorticoid receptor (GR), thiab androgen receptor (AR), feem. AZD 9496 txo qis ERα kev ua haujlwm (IC50 = 0.282 nM), ntsuas los ntawm kev ua kom muaj nuj nqis ntawm cov dej ntws PR, thiab txo qis kev loj hlob ntawm MCF-7 cov qog nqaij hlav cancer mis (IC50 = 0.0398 nM). Nws kuj inhibits MCF-7 xenograft kev loj hlob hauv cov nas nyob rau hauv koob tshuaj. AZD 9496 yog qhov ncauj bioavailable thiab cov qauv uas muaj nws tab tom tshawb nrhiav hauv kev sim tshuaj kho mob ER zoo mob qog noj ntshav.

Hom phiaj: SERD