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- ICG1043 產(chǎn)品型號(hào)
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訪問(wèn)次數(shù):310更新時(shí)間:2023-03-15 09:40:47
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Vandetanib,≥99%
【英文同義名】:ZD-6474,ZD6474, AZD-6474, Caprelsa®.
【中文同義名】:凡德他尼
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 | Vandetanib | ICG1043-0025MG | 25 mg | ¥1,169.00 |
ICG1043-0050MG | 50 mg | ¥2,149.00 | ||
ICG1043-0100MG | 100 mg | ¥3,789.00 |
產(chǎn)品描述
凡德他尼 (vandetanib)是一種口服的VEGFR2抑制劑,IC50=40nM。同時(shí),也可以抑制VEGFR3和EGFR,IC50分別為110 nM和500nM[1]。是用于對(duì)甲狀腺的某些腫瘤的治療的抗癌藥物。它能夠抑制VEGFR依賴的腫瘤血管生成以及EGFR和RET依賴性腫瘤細(xì)胞的增殖和存活來(lái)作用于癌癥中的關(guān)鍵信號(hào)通路[2]。在移植瘤小鼠中,抑制腫瘤組織中VEGFR-2和EGFR的磷酸化,顯著降低了腫瘤的血管密度,增強(qiáng)腫瘤細(xì)胞凋亡,抑制腫瘤生長(zhǎng),提高存活率,減少了肝內(nèi)轉(zhuǎn)移數(shù)目,并且上調(diào)腫瘤組織中的VEGF,TGF-α和EGF[3]。目前正處于不可切除的局部晚期或轉(zhuǎn)移性遺傳的或分散的MTC病人的臨床三期研究[4]。
靶點(diǎn)
Targets | VEGFR2 |
IC50 | 40 nM[1] |
化學(xué)特性
Cas No.: 443913-73-3 | M. Wt.: 475.35 |
Formula: C22H24BrFN4O2 | Purity: ≥99% |
Synonym: ZD-6474,ZD6474, AZD-6474, Caprelsa®. | |
Chemical Name: N-(4-bromo-2-fluorophenyl)-6-methoxy-7-((1-methylpiperidin-4-yl)methoxy)quinazolin-4-amine | |
Appearance: | |
Solubility: Soluble in DMSO (3.6 mg/ml) | |
Storage:Store powder at -20 ºC for the stability of three years. |
結(jié)構(gòu)式
Reference
[1] Wedge SR, et al. ZD6474 inhibits vascular endothelial growth factor signaling, angiogenesis, and tumor growth following oral administration. Cancer Res. 62(16):4645-55(2002).
[2] Herbst RS, et al. (ZD6474): an orally available receptor tyrosine kinase inhibitor that selectively targets pathways critical for tumor growth and angiogenesis. Expert Opin Investig Drugs. 16(2):239-49(2007).
[3] Inoue K, et al. , an inhibitor of VEGF receptor-2 and EGF receptor, suppresses tumor development and improves prognosis of liver cancer in mice. Clin Cancer Res. 18(14):3924-33(2012).
[4] Ton GN, et al. : a novel targeted therapy for the treatment of metastatic or locally advanced medullary thyroid cancer. Am J Health Syst Pharm.70(10):849-55(2013).