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抑制剂/激活剂

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凋亡与自噬

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Cabozantinib 卡博替尼; XL184; BMS-907351

Cabozantinib是一种有效的多受体酪氨酸激酶抑制剂，抑制VEGFR2，c-Met，Kit，Axl 和 Flt3 的 IC50 分别为0.035，1.3，4.6，7 和 11.3 nM。

货号：
TK0548
规格：

1mg

2mg

5mg

10mg

50mg
价格：
￥0.00

产品参数

CAS No.	849217-68-1
生物活性	Cabozantinib is a potent multiple receptor tyrosine kinases (RTKs) inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.
分子式	C28H24FN3O5
分子量	501.51
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	4°C, protect from light
溶解性数据	DMSO : ≥ 30 mg/mL (59.82 mM) H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)
体内研究	Tumor vascularity decreases after Cabozantinib (XL184), with reductions ranging from 67% at 3 mg/kg to 83% at 30 mg/kg for 7 days. In mouse models, Cabozantinib dramatically alters tumor pathology, resulting in decreased tumor and endothelial cell proliferation coupled with increased apoptosis and dose-dependent inhibition of tumor growth in breast, lung, and glioma tumor models. Importantly, treatment with Cabozantinib does not increase lung tumor burden in an experimental model of metastasis, which has been observed with inhibitors of VEGF signaling that do not target MET. On a body weight dosage basis, Cabozantinib plasma exposures range from 6- to 10-fold higher in rats than in mice, which accounts for lower doses inducing tumor growth inhibition/regression in rats than in mice. Subchronic administration of Cabozantinib is well tolerated in mice and rats with no signs of toxicity, as determined by stable and/or increasing body weights during the treatment period.
体外研究	Cabozantinib is a potent inhibitor of MET and VEGFR2 with IC50 values of 1.3 and 0.035 nM, respectively. MET-activating kinase domain mutations Y1248H, D1246N, or K1262R are also inhibited by Cabozantinib (IC50=3.8, 11.8, and 14.6 nM, respectively). Cabozantinib displays strong inhibition of several kinases that have also been implicated in tumor pathobiology, including KIT, RET, AXL, TIE2, and FLT3 (IC50=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). In cellular assays, Cabozantinib inhibits phosphorylation of MET and VEGFR2, as well as KIT, FLT3, and AXL with IC50 values of 7.8, 1.9, 5.0, 7.5, and 42 μM, respectively. The effect of Cabozantinib on proliferation is evaluated in a number of human tumor cell lines. SNU-5 and Hs746T cells harboring amplified MET are the most sensitive to Cabozantinib (IC50=19 and 9.9 nM, respectively); however, SNU-1 and SNU-16 cells lacking MET amplification are more resistant (IC50=5,223 and 1,149 nM, respectively). MDA-MB-231 and U87MG cells exhibit comparable levels of sensitivity to Cabozantinib (IC50=6,421 and 1,851 nM, respectively), whereas H441, H69, and PC3 cell lines are the least sensitive to Cabozantinib with IC50 values of 21,700, 20,200, and 10,800 nM, respectively. In addition, BaF3 cells expressing human FLT3-ITD, an activating mutation in acute myelogenous leukemia, are sensitive to Cabozantinib (IC50=15 nM) when compared with wild-type BaF3 cells (IC50=9,641 nM).
文献	•Cancer Discov. 2021 Jan;11(1):126-141. •Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093. •Cancer Lett. 2019 Apr 10;447:105-114. •J Med Chem. 2016 Jan 14;59(1):358-73. •Antioxidants (Basel). 2021, 10(9), 1336. •Mol Cancer Ther. 2017 Nov;16(11):2387-2398. •J Neurosci. 2020 Dec 9;40(50):9602-9616. •Acta Pharmacol Sin. 2021 Jan;42(1):108-114. •Biomedicines. 2020 Nov 28;8(12):547. •Mol Cancer Res. 2019 Feb;17(2):499-507. •J Pharm Anal. 2021 Jun 19. •Mediat Inflamm. 2020 Oct 24;2020:1649453. •J Cell Biochem. 2020 Mar;121(3):2343-2353. •Sci Rep. 2019 Nov 12;9(1):16600. •Drug Des Devel Ther. 2018 Apr 30;12:1009-1017. •Spectrochim Acta A Mol Biomol Spectrosc. 2016 Apr 15;159:199-208. •Exp Cell Res. 2020 Aug 1;393(1):112054. •Am J Reprod Immunol. 2021 Mar;85(3):e13352. •PLoS One. 2017 Sep 25;12(9):e0185321. •Fundam Clin Pharmacol. 2021 Feb 1. •React Kinet Mech Cat. 07 January 2022. •Eur J Drug Metab Pharmacokinet. 2021 Jul 18;1-11. •Biomed Chromatogr. 2020 Aug;34(8):e4862. •Biochem Biophys Rep. 2020 Jan 17;21:100726. •Patent. US20170349880A1. •Harvard Medical School LINCS LIBRARY
纯度及产品资料	98%

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