Cabozantinib malate (XL184)MET andVEGF receptor2 inhibitor CAS# 1140909-48-3 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
Cas No. | 1140909-48-3 | SDF | Download SDF |
PubChem ID | 25102846 | Appearance | Powder |
Formula | C32H30FN3O10 | M.Wt | 635.59 |
Type of Compound | N/A | Storage | Desiccate at -20°C |
Synonyms | XL184; Cabozantinib | ||
Solubility | DMSO : ≥ 23 mg/mL (36.19 mM) H2O : < 0.1 mg/mL (insoluble) *"≥" means soluble, but saturation unknown. | ||
Chemical Name | 1-N-[4-(6,7-dimethoxyquinolin-4-yl)oxyphenyl]-1-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide;(2S)-2-hydroxybutanedioic acid | ||
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.C(C(C(=O)O)O)C(=O)O | ||
Standard InChIKey | HFCFMRYTXDINDK-WNQIDUERSA-N | ||
Standard InChI | InChI=1S/C28H24FN3O5.C4H6O5/c1-35-24-15-21-22(16-25(24)36-2)30-14-11-23(21)37-20-9-7-19(8-10-20)32-27(34)28(12-13-28)26(33)31-18-5-3-17(29)4-6-18;5-2(4(8)9)1-3(6)7/h3-11,14-16H,12-13H2,1-2H3,(H,31,33)(H,32,34);2,5H,1H2,(H,6,7)(H,8,9)/t;2-/m.0/s1 | ||
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. |
Description | Cabozantinib (S-malate) is a potent VEGFR2 inhibitor with IC50 of 0.035 nM, and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50s of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM, respectively.In Vitro:XL184 (0.1-0.5μM) inhibits the constitutive and inducible MET phosphorylation and its resultant downstream signaling in all MPNST cells. XL184 (> 0.1μM) elicits a significant MPNST cell growth inhibition; higher XL184 doses are needed to inhibit NSC growth. XL184 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 IC50 values 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].In Vivo: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 XL184, compared to corresponding values for vehicle[1]. XL184 (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]. References: |
Cabozantinib malate (XL184) Dilution Calculator
Cabozantinib malate (XL184) Molarity Calculator
1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
1 mM | 1.5733 mL | 7.8667 mL | 15.7334 mL | 31.4668 mL | 39.3335 mL |
5 mM | 0.3147 mL | 1.5733 mL | 3.1467 mL | 6.2934 mL | 7.8667 mL |
10 mM | 0.1573 mL | 0.7867 mL | 1.5733 mL | 3.1467 mL | 3.9334 mL |
50 mM | 0.0315 mL | 0.1573 mL | 0.3147 mL | 0.6293 mL | 0.7867 mL |
100 mM | 0.0157 mL | 0.0787 mL | 0.1573 mL | 0.3147 mL | 0.3933 mL |
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. |
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Cabozantinib malate is a potent inhibitor of MET andVEGF receptor2 with IC50 values of 1.3nM and 0.035nM [1].
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.
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