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ICG1088-SU11274
SU11274,>98%
【英文同義名】:Met Kinase Inhibitor, 658084-23-2, SU 11274, SU-11274, PKI-, PKI-, 658084-23-2
訂購(gòu)信息:(*,常備現(xiàn)貨)
品 牌 | 產(chǎn)品名稱(chēng) | 產(chǎn)品貨號(hào) | 規(guī) 格 | 目錄價(jià)(元) |
Gene Operation | ICG1088-0002MG | 2 mg | ¥589.00 | |
ICG1088-0005MG | 5 mg | ¥949.00 | ||
ICG1088-0025MG | 25 mg | ¥3,659.00 |
產(chǎn)品描述
是ATP競(jìng)爭(zhēng)性的Met小分子抑制劑,其IC50為10 nM。的選擇性是Flk-1的50倍以上 [1],是其它激酶如PDGFR,EGFR,CDK2,SRC和FGFR的500倍以上 [2]。劑量依賴(lài)的抑制BaF3.TPR-MET細(xì)胞的生長(zhǎng),也能誘導(dǎo)從TPR-MET-轉(zhuǎn)化的BaF3細(xì)胞凋亡和細(xì)胞周期的阻滯 [2]。也能抑制表達(dá)c-Met的 NSCLC細(xì)胞的活力并抑制HGF誘導(dǎo)的c-Met磷酸化及其下游信號(hào)傳導(dǎo) [3]。能抑制HCC細(xì)胞的生長(zhǎng)及DCP誘導(dǎo)的HCC細(xì)胞的生長(zhǎng)[4]。以時(shí)間和劑量依賴(lài)的方式顯著抑制結(jié)腸癌細(xì)胞的增殖和細(xì)胞存活 [5]。
靶點(diǎn)
靶點(diǎn) | Met |
IC50(半數(shù)有效濃度) | 10 nM [1] |
化學(xué)特性
Cas No.: 658084-23-2 | M. Wt.: 568.09 |
Formula: C28H30CIN5O4S | Purity: >98% |
Synonym: Met Kinase Inhibitor, SU 11274, SU-11274, PKI-, 658084-23-2 | |
Chemical Name: (Z)-N-(3-chlorophenyl)-3-((3,5-dimethyl-4-(1-methylpiperazine-4-carbonyl)-1H-pyrrol-2-yl)methylene) -N-methyl-2-oxoindoline-5-sulfonamide | |
Appearance: Yellow powder | |
Solubility: Soluble in DMSO (up to 100 mM) | |
Storage:Store powder at -20 ºC for the stability of three years |
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) | 0.5681 | 2.8405 | 5.6809 | 14.2023 | 28.4045 | 56.8090 |
結(jié)構(gòu)式
使用濃度(僅作參考)
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(lèi),培養(yǎng)特性等)進(jìn)行摸索和優(yōu)化。
參考文獻(xiàn)
[1] Wang, X. et al. Potent and selective inhibitors of the Met [hepatocyte growth factor/scatter factor (HGF/SF) receptor] tyrosine kinase block HGF/SF-induced tumor cell growth and invasion. Molecular cancer therapeutics 2, 1085-1092 (2003).
[2] Sattler, M. et al. A novel small molecule met inhibitor induces apoptosis in cells transformed by the oncogenic TPR-MET tyrosine kinase. Cancer research 63, 5462-5469 (2003).
[3] Ma, P. C. et al. Functional expression and mutations of c-Met and its therapeutic inhibition with and small interfering RNA in non-small cell lung cancer. Cancer research 65, 1479-1488 (2005).
[4] Inagaki, Y. et al. Effect of c-Met inhibitor on hepatocellular carcinoma cell growth. Bioscience trends 5, 52-56 (2011).
[5] Gao, S. H., Liu, C., Wei, J. & Feng, Y. Effect of c-Met inhibitor on human colon cancer cell growth. Chinese medical journal 126, 2705-2709 (2013).