2. Protein Tyrosine Kinase/RTK Apoptosis
  3. VEGFR Apoptosis
  4. Cabozantinib S-malate

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

製品番号: HY-12044 純度: 99.90%
COA 取扱説明書 Technical Support

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.

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CAS 番号 : 1140909-48-3

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>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 70 在庫あり
Solution
10 mM * 1 mL in DMSO USD 70 在庫あり
Solid
5 mg $50 在庫あり
10 mg $70 在庫あり
25 mg $80 在庫あり
50 mg $90 在庫あり
100 mg $120 在庫あり
200 mg $190 在庫あり
500 mg $380 在庫あり
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カスタマーレビュー

Based on 56 publication(s) in Google Scholar

Other Forms of Cabozantinib S-malate:

Cabozantinib S-malate 関連抗体

Top Publications Citing Use of Products

顧客検証

WB

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

    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).

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

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

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

    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 MedChemExpress. Usage Cited in: J Med Chem. 2016 Jan 14;59(1):358-73.  [Abstract]

    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

    VEGFR アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

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    製品説明

    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

    VEGFR2

    0.035 nM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    A549 IC50
    >= 50 nM
    Compound: Cabozantinib L-Malate
    Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
    Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
    		[PMID: 30248654]
    BaF3 IC50
    0.01986 μM
    Compound: Cabozantinib L-malate
    Antiproliferative activity against mouse BA/F3 cells expressing TPR-Met after 72 hrs by CCK8 assay
    Antiproliferative activity against mouse BA/F3 cells expressing TPR-Met after 72 hrs by CCK8 assay
    		[PMID: 27068889]
    EBC-1 IC50
    5.4 nM
    Compound: Cabozantinib L-Malate
    Antiproliferative activity against human EBC1 cells after 72 hrs by MTT assay
    Antiproliferative activity against human EBC1 cells after 72 hrs by MTT assay
    		[PMID: 30248654]
    HUVEC IC50
    0.045 μM
    Compound: Cabozantinib L-malate
    Antiproliferative activity against recombinant human VEGF-stimulated HUVEC after 120 hrs by CCK8 assay
    Antiproliferative activity against recombinant human VEGF-stimulated HUVEC after 120 hrs by CCK8 assay
    		[PMID: 27068889]
    HUVEC IC50
    48.6 nM
    Compound: Cabozantinib L-Malate
    Cytotoxicity against HUVEC after 96 hrs by MTT assay
    Cytotoxicity against HUVEC after 96 hrs by MTT assay
    		[PMID: 30248654]
    NCI-H460 IC50
    45.5 nM
    Compound: Cabozantinib L-Malate
    Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay
    		[PMID: 30248654]
    SNU-5 IC50
    13.2 nM
    Compound: Cabozantinib L-Malate
    Antiproliferative activity against human SNU5 cells after 72 hrs by MTT assay
    Antiproliferative activity against human SNU5 cells after 72 hrs by MTT assay
    		[PMID: 30248654]
    体外実験

    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].

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

    Cabozantinib S-malate 関連抗体
    体内実験

    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    臨床実験
    分子量

    635.59

    分子式

    C32H30FN3O10
    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C([C@H](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
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 100 mg/mL (157.33 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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    純度とドキュメンテーション

    純度: 99.90%

    COA (248 KB) HNMR (181 KB) LCMS (93 KB)

    取扱説明書 (2659 KB)
    参考文献
    キナーゼ実験
    [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.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    細胞実験
    [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.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    動物実験
    [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.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.5733 mL 7.8667 mL 15.7334 mL 39.3335 mL
    5 mM 0.3147 mL 1.5733 mL 3.1467 mL 7.8667 mL
    10 mM 0.1573 mL 0.7867 mL 1.5733 mL 3.9334 mL
    15 mM 0.1049 mL 0.5244 mL 1.0489 mL 2.6222 mL
    20 mM 0.0787 mL 0.3933 mL 0.7867 mL 1.9667 mL
    25 mM 0.0629 mL 0.3147 mL 0.6293 mL 1.5733 mL
    30 mM 0.0524 mL 0.2622 mL 0.5244 mL 1.3111 mL
    40 mM 0.0393 mL 0.1967 mL 0.3933 mL 0.9833 mL
    50 mM 0.0315 mL 0.1573 mL 0.3147 mL 0.7867 mL
    60 mM 0.0262 mL 0.1311 mL 0.2622 mL 0.6556 mL
    80 mM 0.0197 mL 0.0983 mL 0.1967 mL 0.4917 mL
    100 mM 0.0157 mL 0.0787 mL 0.1573 mL 0.3933 mL
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    Cabozantinib S-malate Related Classifications

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    Keywords:

    Cabozantinib1140909-48-3XL184BMS-907351XL 184XL-184BMS907351BMS 907351VEGFRApoptosisVascular endothelial growth factor receptorInhibitorinhibitorinhibit

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