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化學性質(zhì):
規(guī)格 | 10mM (in 1mL DMSO) 5mg 25mg 100mg |
CAS | 1140909-48-3 |
別名 |
|
化學名 | 1-N-[4-(6,7-dimethoxyquinolin-4-yl)oxyphenyl]-1-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide;(2S)-2-hydroxybutanedioic acid |
分子式 | C32H30FN3O10 |
分子量 | 635.59 |
溶解度 | ≥ 31.8mg/mL in DMSO |
儲存條件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
產(chǎn)品描述:
Cabozantinib is a pan-tyrosine kinase inhibitor and is developed as an oral treatment of various cancers including MTC, GBM, NSCLC, pancreatic carcinoma, breast and colon cancer. The targets of cabozantinib are MET, VEGFR-2, RET, FLT3, KIT, AXL as well as TEK. In cellular assays, cabozantinib inhibits the phosphorylation of MET, VEGFR2, KIT, FLT3 and AXL with IC50 values of 7.8, 1.9, 5.0, 7.5 and 42μM, respectively [1, 2].
As a pan-tyrosine kinase inhibitor, cabozantinib can affect many biological processes. Cabozantinib inhibits the tubule formation of HMVEC cells with IC50 value of 6.7nM. In B16F10 cells, cabozantinib inhibits HGF-inducedmigration and invasion with IC50 values of 31nM and 9nM, respectively. Moreover, cabozantinib shows anti-proliferation efficacy in a variety of tumors such as SNU-5, Hs746T, MDA-MB-231 and U87MG. It is also reported that the combination of cabozantinib and gefitinib can cause potent inhibition of the gefitinib-resistant HCC827GR6 cell line [1, 2].
References:
[1] Yakes F M, Chen J, Tan J, et al. Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth. Molecular cancer therapeutics, 2011, 10(12): 2298-2308.
[2] Zhang Y, Guessous F, Kofman A, et al. XL-184, a MET, VEGFR-2 and RET kinase inhibitor for the treatment of thyroid cancer, glioblastoma multiforme and NSCLC. IDrugs, 2010, 13(2): 112.
特別提醒:
1. 本產(chǎn)品僅供科研使用。請勿用于醫(yī)藥、臨床診斷或治療,食品及化妝品等用途。請勿存放于普通住宅區(qū)。
2. 為了您的安全和健康,請穿好實驗服并佩戴一次性手套和口罩操作。
原創(chuàng)作者:上海莼試生物技術(shù)有限公司
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