Cabozantinib S-malate (XL184 S-malate) is a potent multiplereceptor tyrosine kinasesinhibitor that inhibitsVEGFR2,c-Met,Kit,AxlandFlt3withIC₅₀s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.

Cabozantinib (0.1-0.5μM) inhibits the constitutive and inducible MET phosphorylation and its resultant downstream signaling in all MPNST cells. Cabozantinib (>0.1μM) elicits a significant MPNST cell growth inhibition; higher Cabozantinib doses are needed to inhibit NSC growth. Cabozantinib treatment blocks HGF-induced MPNST motility and invasion (a similar effect of found on NSC)^[2]. In cellular assays, cabozantinib inhibits phosphorylation of MET and VEGFR2, as well as KIT, FLT3, and AXL with IC₅₀values of 7.8, 1.9, 5.0, 7.5, and 42 μM, respectively. Cabozantinib also inhibits tubule formation in response to conditioned media derived from cultures of MDA-MB-231 (IC₅₀=5.1 nM), A431 (IC₅₀=4.1 nM), HT1080 (IC₅₀=7.7 nM), and B16F10 (IC₅₀=4.7 nM) cells^[3].

Cabozantinib (60 mg/kg, i.p.) decreases the tumor vascularity with reductions ranging from 67% at 3 mg/kg to 83% at 30 mg/kg for 7 days in animals. Tumors in RIP-Tag2 mice treated for 7 days beginning at age 10 weeks are 40% smaller after XL880 and 35% smaller after Cabozantinib, compared to corresponding values for vehicle^[1]. Cabozantinib (30 mg/kg) significantly decreases the microvessel density in mice^[2]. Cabozantinib (100 mg/kg, p.o.) inhibits in vivo stimulation of MET phosphorylation by HGF in liver hepatocytes and VEGF-stimulated phosphorylation of FLK1 with inhibition of both targets sustained through 8 hours postdose. Cabozantinib (100 mg/kg, p.o.) disrupts tumor vasculature and promotes tumor and endothelial cell death. Cabozantinib (1-60 mg/kg, p.o.) inhibits tumor growth and promotes tumor regression in vivo^[3].

635.59

Solid

C₃₂H₃₀FN₃O₁₀

1140909-48-3

卡博替尼苹果酸盐；苹果酸卡博替尼

Room temperature in continental US; may vary elsewhere.

DMSO : ≥ 23 mg/mL(36.19 mM)

H₂O :< 0.1 mg/mL(insoluble)

*"≥" means soluble, but saturation unknown.

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