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    AUY922 (NVP-AUY922)是熱休克蛋白90 (HSP90)的有效的新型合成間苯二酚基異惡唑酰胺抑制劑。[1]是一種小分子，分子式為C26H31N3O5，分子量為465.5。它對(duì)Hsp90有更高的親和力，并可在HSP 90N-末端結(jié)構(gòu)域的ATP結(jié)合位點(diǎn)找到。[2]熱休克蛋白90 (HSP90)是細(xì)胞生長(zhǎng)和存活的關(guān)鍵調(diào)節(jié)物的穩(wěn)定性所必需的分子伴侶。NVP-AUY922以大約2至40 nmol/L的GI50值有效地抑制胃癌細(xì)胞系的增殖，并顯著誘導(dǎo)生長(zhǎng)因子受體和其他客戶蛋白的降解。[3]

產(chǎn)品性質(zhì)：

Cas No.:747412-49-3

別名:VER-52296, AUY-922, AUY 922, Luminespib

化學(xué)名: (5Z)-N-ethyl-5-(4-hydroxy-6-oxo-3-propan-2-ylcyclohexa-2,4-dien-1-ylidene)-4-[4-(morpholin-4-ylmethyl)phenyl]-2H-1,2-oxazole-3-carboxamide

Canonical SMILES:CCNC(=O)C1=C(C(=C2C=C(C(=CC2=O)O)C(C)C)ON1)C3=CC=C(C=C3)CN4CCOCC4

分子式:C26H31N3O5

分子量:465.5

溶解度:≥ 23.3 mg/mL in DMSO, ≥ 100.6 mg/mL in EtOH with ultrasonic

儲(chǔ)存條件:Store at -20°C

注意事項(xiàng)：

為了您的安全和健康，請(qǐng)穿實(shí)驗(yàn)服并戴一次性手套操作。

References:

[1] Suzanne A. E, Andy M, Florence I. R, et al. NVP-AUY922: A Novel Heat Shock Protein 90 Inhibitor Active against Xenograft Tumor Growth, Angiogenesis, and Metastasis. Cancer Res. 2008, 68. 2850-2860.

[2] Tsuyoshi U, Kazunori T, Shinichi T, Midori A, Munenori T, et al. Strong anti-tumor effect of NVP-AUY922, a novel Hsp90 inhibitor, on non-small cell lung cancer. Lung Cancer. 2012, 76. 26-31.

[3] Kyung-Hun L, Ju-Hee L, Sae-Won H, Seock-Ah I, et al. Antitumor activity of NVP-AUY922, a novel heat shock protein 90 inhibitor, in human gastric cancer cells is mediated through proteasomal degradation of client proteins. Cancer Sci. 2011, 102. 1388–1395.