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蘋果酸鹽原料藥 小分子抑制劑 研究用藥效強 現貨供應順豐發貨僅供科研 產品名稱:蘋果酸鹽 產品別名:Cabozantinib malate (XL184) CAS.NO:1140909-48-3 分子式:C28H24FN3O5.C4H6O5 分子量:635.59 純度級別:實驗試劑LR 產品性狀:固態粉末 穩定性:3年 -20℃粉狀 6個月-80℃溶于溶劑 有效成分含量:99% 用途:科研 產品描述:Cabozantinib malate (XL184)是Cabozantinib的蘋果酸鹽,是有效的VEGFR2抑制劑,IC50為0.035 nM,也抑制c-Met, Ret, Kit, Flt-1/3/4, Tie2和AXL,無細胞試驗中IC50分別為1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM和7 nM。 靶點:VEGFR2/KDR [1] c-Met [1] Kit [1] VEGFR3/FLT4 [1] Axl [1] 體外研究:Cabozantinib has weak inhibitory activity against RON and PDGFRβ with IC50 of 124 nM and 234 nM, respectivey, and has low activity against FGFR1 with IC50 of 5.294 μM. [1] Cabozantinib at low concentration (0.1-0.5 μM) is sufficient to induce marked inhibition of constitutive and inducible Met phosphorylation and its resultant downstream signaling in MPNST cells, and inhibit HGF-induced MPNST cell migration and invasion. Cabozantinib also induces marked inhibition of Met and VEGFR2 phosphorylation in cytokine-stimulated human umbilical vein endothelial cells (HUVECs). Although Cabozantinib has no significant effect on MPNST cell growth at 0.1 μM, Cabozantinib at 5-10 μM significantly inhibits the MPNST cell growth. [2] 體內研究:Cabozantinib treatment at 30 mg/kg in RIP-Tag2 mice with spontaneous pancreatic islet tumors disrupts 83% of the tumor vasculature, reduces pericytes and empty basement membrane sleeves, causes widespread intratumoral hypoxia and extensive tumor cell apoptosis, and slows regrowth of the tumor vasculature after drug withdrawal, more significantly compared with XL999 that blocks VEGFR but not c-Met, leading to only 43% reduction in vascularity, suggesting that concurrent inhibition of VEGFR and other functionally relevant receptor tyrosine kinases (RTK) amplifies angiogenesis inhibition. Cabozantinib also decreases invasiveness of primary tumors and reduces metastasis. [1] Cabozantinib at 30 mg/kg/day significantly abrogates human MPNST xenografts growth and metastasis in SCID mice. [2] Administration of Cabozantinib induces dose-dependent inhibition of tumor growth in breast, lung, and glioma tumor models, in association with decreased tumor and endothelial cell proliferation as well as increased apoptosis. A single oral dose of Cabozantinib is sufficient to induce sustained tumor growth inhibition in MDA-MB-231 tumor-bearing mice and C6 tumor-bearing rats at 100 mg/kg and 10 mg/kg, respectively. [3]
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