1. Protein Tyrosine Kinase/RTK
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  3. Cabozantinib S-malate

Cabozantinib S-malate (Synonyms: XL184 (S-malate); BMS-907351 (S-malate))

Cat. No.: HY-12044 Purity: 99.93%
Handling Instructions

Cabozantinib S-malate (XL184 S-malate) is a potent multiple receptor tyrosine kinases 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.

For research use only. We do not sell to patients.

Cabozantinib S-malate Chemical Structure

Cabozantinib S-malate Chemical Structure

CAS No. : 1140909-48-3

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Customer Review

Based on 14 publication(s) in Google Scholar

Other Forms of Cabozantinib S-malate:

Top Publications Citing Use of Products

    Cabozantinib S-malate purchased from MCE. Usage Cited in: PLoS One. 2017 Sep 25;12(9):e0185321.

    Treatment with Cabozantinib results in complete inhibition of the c-MET phosphorylation stimulated by HGF at nanomolar concentrations.

    Cabozantinib S-malate purchased from MCE. Usage Cited in: J Med Chem. 2016 Jan 14;59(1):358-73.

    Autophosphorylation of RET and its downstream signaling are blocked by 6i. The effect of 6i on autophosphorylation of RET in (A) RET-WT Ba/F3, (B) RET-S891A Ba/F3, (C) RET-V804L Ba/F3 and (D) RET-V804M Ba/F3. (A-D) Ba/F3 cells, stably transformed with the indicated constructs, are treated for 1 h with gradually increasing concentrations of 7a, Cabozantinib and 6i (0-10 μM) and then lysed. Protein extracts are immunoblotted with antibodies specific for the Y905 and Y1062 phosphorylated forms of R

    Cabozantinib S-malate purchased from MCE. Usage Cited in: J Med Chem. 2016 Jan 14;59(1):358-73.

    Autophosphorylation of RET and its downstream signaling are blocked by 6i. The effect of 6i on autophosphorylation of RET in (A) RET-WT Ba/F3, (B) RET-S891A Ba/F3, (C) RET-V804L Ba/F3 and (D) RET-V804M Ba/F3. (A-D) Ba/F3 cells, stably transformed with the indicated constructs, are treated for 1 h with gradually increasing concentrations of 7a, Cabozantinib and 6i (0-10 μM) and then lysed. Protein extracts are immunoblotted with antibodies specific for the Y905 and Y1062 phosphorylated forms of R

    Cabozantinib S-malate purchased from MCE. Usage Cited in: Mol Cancer Ther. 2017 Nov;16(11):2387-2398.

    Representative Western blots and densitometry show that cabozantinib reduces phosphorylation of Erk1/2 after 6 hours and reduces cyclin D1 and increases p27 protein levels after 24 hours of treatment (n=3-4).

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    • Biological Activity

    • Protocol

    • Technical Information

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    • References

    Description

    Cabozantinib S-malate (XL184 S-malate) is a potent multiple receptor tyrosine kinases 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.

    IC50 & Target[1]

    VEGFR2

    0.035 nM (IC50)

    In Vitro

    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 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 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].

    Clinical Trial
    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 23 mg/mL (36.19 mM)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.5733 mL 7.8667 mL 15.7334 mL
    5 mM 0.3147 mL 1.5733 mL 3.1467 mL
    10 mM 0.1573 mL 0.7867 mL 1.5733 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Kinase Assay
    [3]

    The inhibition profile of cabozantinib against a broad panel of 270 human kinases is determined using luciferase-coupled chemiluminescence, 33P-phosphoryl transfer, or AlphaScreen technology. Recombinant human full-length, glutathione S-transferase tag, or histidine tag fusion proteins are used, and half maximal inhibitory concentration (IC50) values are determined by measuring phosphorylation of peptide substrate poly (Glu, Tyr) at ATP concentrations at or below the Km for each respective kinase. The mechanism of kinase inhibition is evaluated using the AlphaScreen Assay by determining the IC50 values over a range of ATP concentrations.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [3]

    Cells are seeded in triplicate overnight in media containing 10% FBS. The next day, cells are treated with serial dilutions of cabozantinib for 48 hours, followed by analysis of proliferation using Cell Proliferation ELISA, BrdUrd.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [3]

    H441 cells (3×106) are implanted intradermally into the hind flank and when tumors reach approximately 150 mg, tumor weight is calculated using the formula: (tumor volume=length (mm) × width2 (mm2)]/2, mice are randomized (n=5 per group) and orally administered a single 100 mg/kg dose of cabozantinib or vehicle. Tumors are collected at the indicated time points. Pooled tumor lysates are subjected to immunoprecipitation with anti-MET (SC161) and Western blotting with anti-phosphotyrosine MET (pY1230/34/35). After blot stripping, total MET is quantitated as a loading control. In a separate experiment, naive mice (n=5 per group) are administered a single 100 mg/kg dose of cabozantinib or vehicle, followed by intravenous administration of HGF (10 μg per mouse) 10 minutes before liver collection. Analysis of MET phosphorylation in liver lysates is as described above. In a separate experiment, naive mice (n=5 per group) are administered a single 100 mg/kg dose of cabozantinib or vehicle, followed by intravenous administration of VEGF (10 μg per mouse) 30 minutes before lung collection. Pooled lung lysates are subjected to immunoprecipitation with FLK1 (SC6251) and Western blotting with anti-phosphotyrosine (4G10). After blot stripping, total FLK1 is quantitated as a loading control.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    635.59

    Formula

    C₃₂H₃₀FN₃O₁₀

    CAS No.

    1140909-48-3

    SMILES

    O=C([[email protected]](CC(O)=O)O)O.O=C(NC1=CC=C(C=C1)OC2=CC=NC3=CC(OC)=C(C=C23)OC)C4(CC4)C(NC5=CC=C(C=C5)F)=O

    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 99.93%

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    Product Name:
    Cabozantinib S-malate
    Cat. No.:
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    Cabozantinib S-malate

    Cat. No.: HY-12044