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ICG1121-Tyrphostin AG 879
Tyrphostin AG 879,≥98%
【英文同義名】:AG879, AG 879, AG-879
訂購(gòu)信息:(*,常備現(xiàn)貨)
品 牌 | 產(chǎn)品名稱 | 產(chǎn)品貨號(hào) | 規(guī) 格 | 目錄價(jià)(元) |
Gene Operation | Tyrphostin AG 879 | ICG1121-0005MG | 5 mg | ¥1,699.00 |
ICG1121-0010MG | 10 mg | ¥2,320.00 | ||
ICG1121-0025MG | 25 mg | ¥5,104.00 |
產(chǎn)品描述
Tyrphostin AG 879是一種酪氨酸激酶抑制劑,抑制ErbB-2(IC50=1μM),TrkA磷酸化(IC50=10 μM),和VEGF受體FLK-1(IC50=1μM)[1]。還可以抑制RAS細(xì)胞中ETK活性(IC50=5 nM)和PAK1激酶活性,并抑制RAS誘導(dǎo)的惡性轉(zhuǎn)化[2]。另外,tyrphostin AG 879抑制schwannoma細(xì)胞中IL-6誘導(dǎo)的STAT3酪氨酸磷酸化并顯著抑制NGF和P92的活性[4]。Tyrphostin AG 879抑制人前列腺癌細(xì)胞LNCaP C-81中ErbB-2和MAPK活性,并導(dǎo)致前列腺分泌抗原(PSA)分泌的顯著下降[5]。Tyrphostin AG 879還可以顯著降低非神經(jīng)癌細(xì)胞的增殖并伴隨細(xì)胞凋亡的增長(zhǎng),在移植入平滑肌肉瘤和早幼粒細(xì)胞性白血病細(xì)胞的免疫抑制小鼠中tyrphostin AG 879可減小腫瘤大小[6]。
靶點(diǎn)
靶點(diǎn) | HER2-Neu | Trk | FLK-1 |
IC50(半數(shù)有效濃度) | 1.0 μM [1] | 10 μM [1] | 1 μM [1] |
化學(xué)特性
Cas No.: 148741-30-4 | 分子量: 316.46 |
分子式: C18H24N2OS | 純度: ≥98% |
同義名: AG879, AG 879, AG-879 | |
化學(xué)名: (2E)-3-[3, 5-Bis (1, 1-diMethylethyl)-4-hydroxyphenyl]-2-cyano-2-propenethioaMide | |
外觀: 黃色粉末 | |
溶解: 溶于DMSO (up to 100 mM) | |
保存:3年 -20℃粉狀 |
儲(chǔ)存液配制
儲(chǔ)存液 (1 ml DMSO體系) | 1 mM | 5 mM | 10 mM | 25 mM | 50 mM | 100 mM |
質(zhì)量(mg) | 0.3165 | 1.5823 | 3.1646 | 7.9115 | 15.8230 | 31.6460 |
結(jié)構(gòu)式
使用濃度(僅作參考)
Tyrphostin AG 87的具體使用濃度請(qǐng)參考相關(guān)文獻(xiàn),并根據(jù)自身實(shí)驗(yàn)條件(如實(shí)驗(yàn)?zāi)康模?xì)胞種類,培養(yǎng)特性等)進(jìn)行摸索和優(yōu)化。
參考文獻(xiàn)
[1] Yeh S, et al. From HER2/Neu signal cascade to androgen receptor and its coactivators: a novel pathway by induction of androgen target genes through MAP kinase in prostate cancer cells. Proc Natl Acad Sci U S A. 1999 May 11; 96(10):5458-63.
[2] Zhou Y, Brattain MG. Synergy of epidermal growth factor receptor kinase inhibitor AG1478 and ErbB2 kinase inhibitor AG879 in human colon carcinoma cells is associated with induction of apoptosis. Cancer Res. 2005 Jul 1; 65(13):5848-56.
[3] He H, et al. The Tyr-kinase inhibitor AG879, that blocks the ETK-PAK1 interaction, suppresses the RAS-induced PAK1 activation and malignant transformation. Cancer Biol Ther. 2004 Jan;3(1):96-101.
[4] Lee HK, et al. Tyrphostin ErbB2 Inhibitors AG825 and AG879 Have Non-specific Suppressive Effects on gp130/ STAT3 Signaling. Korean J Physiol Pharmacol. 2008 Oct;12(5):281-6.
[5] Lee MS, et al. ErbB-2 signaling is involved in regulating PSA secretion in androgen-independent human prostate cancer LNCaP C-81 cells. Oncogene. 2003 Feb 6;22(5):781-96.
[6] Rende M, et al. Role of nerve growth factor and its receptors in non-nervous cancer growth: efficacy of a tyrosine kinase inhibitor (AG879) and neutralizing antibodies antityrosine kinase receptor A and antinerve growth factor: an in-vitro and in-vivo study. Anticancer Drugs. 2006 Sep;17(8):929-41.