Cabozantinib (XL184,BMS-907351) 是一种新型 MET 和 VEGFR2 抑制剂，可同时抑制转移、血管生成和肿瘤生长[1]。其对 VEGFR2 和 c-Met 的 IC50 值分别为 0.035 nM 和 1.3 nM[2]。

Cabozantinib(XL184) 处理 MDA-MB-231 和 HCC70 细胞的 MAME 培养物（表达 HGF 的成纤维细胞）具有细胞毒性并显着减少多细胞侵袭性生长，即使在含有表达 HGF 的成纤维细胞的培养物中也是如此[3]。 Cabozantinib 诱导的细胞应激导致 DU-145 细胞系发生 ICD（一种特殊类型的细胞凋亡）[4]。据报道，卡博替尼可通过阻断膀胱癌细胞中的 HGF-MET 信号通路来抑制 MMP-1 的表达[5]。卡博替尼处理后ESCC细胞MMP-1显着降低，这是卡博替尼处理后ESCC细胞迁移活性降低的原因[6]。

卡博替尼抑制肿瘤生长在啮齿动物的人类肿瘤模型中呈剂量依赖性[1]。体内药效学研究表明，单次口服卡博替尼[7]后，TT 异种移植肿瘤中的 RET 得到显着抑制。使用 CRC（结直肠癌）外植体模型，卡博替尼在体内表现出优异的抗肿瘤作用[8]。

产品性质：

Cas No.:849217-68-1

别名:卡博替尼; XL184; BMS-907351

化学名: 1-N-[4-(6,7-dimethoxyquinolin-4-yl)oxyphenyl]-1-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide

Canonical SMILES COC1=CC2=C(C=CN=C2C=C1OC)OC3=CC=C(C=C3)NC(=O)C4(CC4)C(=O)NC5=CC=C(C=C5)F

分子式:C28H24FN3O5

分子量:501.51

溶解度:≥ 25.1mg/mL in DMSO

储存条件:4°C, protect from light

注意事项：

为了您的安全和健康，请穿实验服并戴一次性手套操作。

References:

[1]. Yakes F Michael,Chen Jason, et al. Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth.[J]. Molecular cancer therapeutics,2011,10(12).

[2]. Weon-Kyoo You, Barbara Sennino, et al. VEGF and c-Met Blockade Amplify Angiogenesis Inhibition in Pancreatic Islet Cancer[J]. Microenvironment and Immunology,2011.

[3]. Sameni Mansoureh,Tovar Elizabeth A, et al. Cabozantinib (XL184) Inhibits Growth and Invasion of Preclinical TNBC Models.[J]. Clinical cancer research : an official journal of the American Association for Cancer Research,2016,22(4).

[4] Scirocchi Fabio,Napoletano Chiara,et al. Immunogenic Cell Death and Immunomodulatory Effects of Cabozantinib[J]. Frontiers in Oncology,2021,11.

[5] Shintani T, Kusuhara Y, et al. The involvement of hepatocyte growth factor-MET-matrix metalloproteinase 1 signaling in bladder cancer invasiveness and proliferation. Effect of the MET inhibitor, cabozantinib (XL184), on bladder cancer cells. Urology. (2017) 101:169.e7-13. doi: 10.1016/j.urology.2016.12.006.

[6] Pei-Wen Yang, Yu-Cheng Liu, et al. Cabozantinib (XL184) and R428 (BGB324) Inhibit the Growth of Esophageal Squamous Cell Carcinoma (ESCC)[J]. Frontiers in Oncology, 2019.

[7] Bentzien Frauke,Zuzow Marcus, et al. In vitro and in vivo activity of cabozantinib (XL184), an inhibitor of RET, MET, and VEGFR2, in a model of medullary thyroid cancer.[J]. Thyroid : official journal of the American Thyroid Association,2013,23(12).

[8] Scott Aaron J,Arcaroli John J,et al. Cabozantinib Exhibits Potent Antitumor Activity in Colorectal Cancer Patient-Derived Tumor Xenograft Models via Autophagy and Signaling Mechanisms.[J]. Molecular cancer therapeutics,2018,17(10).