1. Protein Tyrosine Kinase/RTK
  2. FLT3
    c-Kit
    FGFR
    VEGFR
    PDGFR
    c-Fms
  3. Dovitinib

Dovitinib  (Synonyms: CHIR-258; TKI258)

Cat. No.: HY-50905 Purity: 99.94%
COA Handling Instructions

Dovitinib (CHIR-258) is an orally active, potent multi-targeted tyrosine kinase (RTK) inhibitor with IC50s of 1, 2, 36, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, CSF-1R, FGFR1/FGFR3, VEGFR1/VEGFR2/VEGFR3 and PDGFRα/PDGFRβ, respectively. Dovitinib has potent antitumor activity.

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

Dovitinib Chemical Structure

Dovitinib Chemical Structure

CAS No. : 405169-16-6

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10 mM * 1 mL in DMSO USD 117 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
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Estimated Time of Arrival: December 31
Solid
10 mg USD 106 In-stock
Estimated Time of Arrival: December 31
50 mg USD 317 In-stock
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100 mg USD 528 In-stock
Estimated Time of Arrival: December 31
200 mg USD 924 In-stock
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500 mg USD 1716 In-stock
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Customer Review

Based on 8 publication(s) in Google Scholar

Other Forms of Dovitinib:

Top Publications Citing Use of Products

    Dovitinib purchased from MCE. Usage Cited in: Theranostics. 2018 Jul 30;8(15):4262-4278.  [Abstract]

    BV2 cells are pretreated with 0.1% DMSO (Ctrl), JuA (25 µM) or JuA (25 µM) with the indicated antagonist of RTKs (Dovitinib at 1 µM, Gefinitib at 2.5 µM, Sunitinib at 2.5 µM and LDC1267 at 1 µM) for 30 min, followed by administration of Aβ42 (5 μM) for 12 h.

    Dovitinib purchased from MCE. Usage Cited in: Front Cell Dev Biol. 2020 May 7;8:287.  [Abstract]

    Determination in L3.6 cells of FGF2-induced FGFR phosphorylation by Western blot in the presence of Dovitinib. FGFR1 and alpha-Tubulin are used as loading controls.

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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Dovitinib (CHIR-258) is an orally active, potent multi-targeted tyrosine kinase (RTK) inhibitor with IC50s of 1, 2, 36, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, CSF-1R, FGFR1/FGFR3, VEGFR1/VEGFR2/VEGFR3 and PDGFRα/PDGFRβ, respectively. Dovitinib has potent antitumor activity[1][2].

    IC50 & Target[1]

    FLT3

    1 nM (IC50)

    c-Kit

    2 nM (IC50)

    FGFR1

    8 nM (IC50)

    FGFR3

    9 nM (IC50)

    VEGFR3

    8 nM (IC50)

    VEGFR1

    10 nM (IC50)

    VEGFR2

    13 nM (IC50)

    PDGFRβ

    27 nM (IC50)

    PDGFRα

    210 nM (IC50)

    CSF-1R

    36 nM (IC50)

    In Vitro

    Dovitinib (CHIR-258) shows more than 10-fold inhibition InsR (IC50=2 μM), EGFR1 (IC50=2 μM), c-Met (IC50>3 μM), EphrinA2 (EphA2; IC50=4 μM), Tie2 (IC50=4 μM), IGFR1 (IC50>10 μM), and HER2 (IC50>10 μM)[1].
    Dovitinib (12.5-400 nM; 48 hours) potently inhibits the FGF-stimulated growth of WT and F384L-FGFR3-expressing B9 cells with IC50 values of 25 nM[1].
    Dovitinib (100, 500 nM; 96 hours) inhibits FGF-mediated ERK1/2 phosphorylation and induces apoptosis of FGFR3-expressing human myeloma cell lines[1].
    Dovitinib (72 hours) inhibits cell proliferation of KMS11 (FGFR3-Y373C), OPM2 (FGFR3-K650E), and KMS18 (FGFR3-G384D) cells with IC50 of values of 90 nM (KMS11 and OPM2) and 550 nM, respectively[1].
    Dovitinib (100 nM) augments Dexamethasone (0.5 μM) cytotoxicity in KMS11 cells[1].
    Dovitinib significantly reduces the basal phosphorylation levels of FGFR-1, FGFR substrate 2α (FRS2-α) and ERK1/2 but not Akt in both SK-HEP1 and 21-0208 cells[2].
    Dovitinib enhances the BMP-2-induced alkaline phosphatase (ALP) induction, which is a representative marker of osteoblast differentiation. Dovitinib also stimulates the translocation of phosphorylated Smad1/5/8 into the nucleus and phosphorylation of mitogen-activated protein kinases, including ERK1/2 and p38[3].
    Dovitinib strongly inhibits both the interaction of TNIK with ATP (Ki, 13 nM) and the activation of Wnt signaling effectors such as β-catenin and TCF4. Dovitinib also induces caspase-dependent apoptosis in IM-9 cells without significant cytotoxicity in PBMCs[4].

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

    Cell Viability Assay[1]

    Cell Line: WT and F384L-FGFR3-expressing B9 cells
    Concentration: 12.5, 25, 50, 100, 200, 300, 400 nM
    Incubation Time: 48 hours
    Result: Potently inhibited the FGF-stimulated growth of the cells.

    Apoptosis Analysis[1]

    Cell Line: KMS11, OPM2, and KMS18 cells
    Concentration: 100 nM or 500 nM
    Incubation Time: 96 hours
    Result: Induced apoptosis of FGFR3-expressing human myeloma cell lines.
    In Vivo

    Dovitinib (CHIR-258; 10-60 mg/kg/day; gavage; for 21 days) has a significant antitumor effect[1].
    Dovitinib (50 and 75 mg/kg) results in 97% and 98% tumor growth inhibition, respectively, and the maximal efficacy is at 50 mg/kg[2].

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

    Animal Model: 6- to 8-week-old female BNX mice with KMS11 cells[1]
    Dosage: 10, 30, 60 mg/kg
    Administration: Gavage; daily for 21 days
    Result: Had a significant antitumor effect in all 3 dose groups with 48%, 78.5%, and 94% growth inhibition in the 10 mg/kg, 30 mg/kg, and 60 mg/kg treatment.
    Clinical Trial
    Molecular Weight

    392.43

    Formula

    C21H21FN6O

    CAS No.
    SMILES

    O=C1NC(C=CC=C2F)=C2C(N)=C1C3=NC4=CC=C(N5CCN(C)CC5)C=C4N3

    Shipping

    Room temperature in continental US; may vary elsewhere.

    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 : 25 mg/mL (63.71 mM; Need ultrasonic and warming)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.5482 mL 12.7411 mL 25.4823 mL
    5 mM 0.5096 mL 2.5482 mL 5.0965 mL
    10 mM 0.2548 mL 1.2741 mL 2.5482 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (6.37 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (6.37 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (6.37 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.94%

    References
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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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