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- ICG1054-Cediranib 產(chǎn)品型號(hào)
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ICG1054-Cediranib (AZD217)
Cediranib (AZD217),>99%
【英文同義名】:Recentin, 288383-20-0, AZD2171, AZD 2171, AZD-2171, Kinome_3318, Cediranib (USAN/INN), UNII-NQU9IPY4K9
【中文同義名】:西地尼布
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 | Cediranib (AZD217) | ICG1054-0005MG | 5 mg | ¥829.00 |
ICG1054-0010MG | 10 mg | ¥1,339.00 | ||
ICG1054-0050MG | 50 mg | ¥4,189.00 | ||
ICG1054-0100MG | 100 mg | ¥7,529.00 |
產(chǎn)品描述
Cediranib是高效的VEGFR2(KDR)小分子抑制劑,其IC50小于1 nM, Cediranib同時(shí)也能抑制Flt-1和Flt-3,其特異性比其他PDGFR相關(guān)成員高出36倍(PDGFR-a)到1000倍(Flt-3)。Cediranib抑制KDR時(shí)其特異性是EGFR的1600倍以上,MEK的10000倍以上。Cediranib在體內(nèi)可以*阻斷VEGF誘導(dǎo)的血管生成[1]。Cediranib能夠通過(guò)降低腫瘤血管通透性,血管周細(xì)胞覆蓋正常化,減薄基底膜及控制水腫使成膠質(zhì)細(xì)胞瘤小鼠存活期增加[2]。Cediranib與radiation聯(lián)用能顯著延遲Calu-6肺移植瘤的生長(zhǎng)[3]。Cediranib是Recentin商品藥劑的活性成分。
靶點(diǎn)
靶點(diǎn) | VEGFR2 | Flt-1 | Flt-4 |
IC50(半數(shù)有效濃度) | <1 nM | 5 nM | 3 nM[1] |
化學(xué)特性
Cas No.: 288383-20-0 | M. Wt.: 450.505 |
Formula: C25H27FN4O3 | Purity: >99% |
Synonym: Recentin, 288383-20-0, AZD2171, AZD 2171, AZD-2171, Kinome_3318, Cediranib (USAN/INN), | |
Chemical Name: 4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-6-methoxy-7-(3-pyrrolidin-1-ylpropoxy)quinazoline | |
Appearance: white solid powder | |
Solubility: Soluble in DMSO (up to 50 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 |
質(zhì)量(mg) | 0.4505 | 2.2525 | 4.5051 | 11.2625 | 22.5253 |
結(jié)構(gòu)式
使用濃度(僅作參考)
Cediranib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?,?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] Wedge, S. R. et al. AZD2171: a highly potent, orally bioavailable, vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor for the treatment of cancer. Cancer research 65, 4389-4400(2005).
[2] Kamoun, W. S. et al. Edema control by cediranib, a vascular endothelial growth factor receptor-targeted kinase inhibitor, prolongs survival despite persistent brain tumor growth in mice. Journal of clinical oncology : official journal of the American Society of Clinical Oncology 27, 2542-2552(2009).
[3] Williams, K. J. et al. Inhibition of vascular endothelial growth factor signalling using cediranib (RECENTIN; AZD2171) enhances radiation response and causes substantial physiological changes in lung tumour xenografts. The British journal of radiology 81 Spec , S21-27(2008).