AZD9496

Inoa Kimia:

(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

Code 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

Ki InChi:

DFBDRVGWBHBJNR-BBNFHIFMSA-N

Hua'ōlelo:

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

Hiki ke hoʻoheheʻe:Hiki ke hoʻoheheʻe ʻia ma DMSO

Waihona:0 - 4°C no ka wā pōkole (nā lā i nā pule), a i ʻole -20°C no ka wā lōʻihi (mau mahina)

wehewehe:

ʻO AZD 9496 kahi mea hoʻohaʻahaʻa i ka estrogen receptor downregulator (SERD) me ka waiwai IC50 o 0.138 nM no ka estrogen receptor α (ERα) downregulation. He koho ia no ERα i hoʻohālikelike ʻia me nā mea hoʻokipa nuklea ʻē aʻe me nā waiwai IC50 o 0.0008, 0.54, 9.2, a me 30 μM no ERα, progesterone receptor (PR), glucocorticoid receptor (GR), a me androgen receptor (AR), kēlā me kēia. Hoʻemi ʻo AZD 9496 i ka hana ERα (IC50 = 0.282 nM), ana ʻia ma o ka helu ʻana o ka hana PR i lalo, a hoʻemi i ka hoʻonui ʻana o nā maʻi maʻi umauma MCF-7 (IC50 = 0.0398 nM). Kāohi ia i ka ulu ʻana o ka xenograft MCF-7 i nā ʻiole ma ke ʻano hilinaʻi. Hiki i ka AZD 9496 ke hoʻopaʻa ʻia i ka maʻi maʻi umauma ER maikaʻi.

Pahuhopu: SERD