1. Protein Tyrosine Kinase/RTK
  2. FGFR

Dovitinib lactate (Synonyms: CHIR-258 lactate; TKI-258 lactate)

Cat. No.: HY-10207 Purity: 99.77%
Handling Instructions

Dovitinib(CHIR-258; TKI258) lactate is a potent inhibitor of fibroblast growth factor receptor 3 (FGFR3) with an IC50 of 5 nM.

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

Dovitinib lactate Chemical Structure

Dovitinib lactate Chemical Structure

CAS No. : 692737-80-7

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
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Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
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Estimated Time of Arrival: December 31
10 mg USD 96 In-stock
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Estimated Time of Arrival: December 31
50 mg USD 288 In-stock
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Estimated Time of Arrival: December 31
100 mg USD 480 In-stock
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Estimated Time of Arrival: December 31
200 mg USD 840 In-stock
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Estimated Time of Arrival: December 31
500 mg USD 1560 In-stock
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Estimated Time of Arrival: December 31
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Customer Review

Other Forms of Dovitinib lactate:

    Dovitinib lactate purchased from MCE. Usage Cited in: Theranostics. 2018; 8(15):4262-4278.

    BV2 cells are pretreated with 0.1% DMSO (Ctrl), JuA (25 µM) or JuA (25 µM)+SCH772984 (10 µM) for 30 min, followed by administration of Aβ42 (5 μM) for 6 h.

    Dovitinib lactate purchased from MCE. Usage Cited in: Theranostics. 2018; 8(15):4262-4278.

    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 lactate purchased from MCE. Usage Cited in: Theranostics. 2018; 8(15):4262-4278.

    BV2 cells are pretreated with 0.1% DMSO (Ctrl), JuA (25 µM) or JuA (25 µM) with the indicated antagonist of TAM receptor (LDC1267 at 1 µM, UNC2250 at 5 µM, R428 at 5 µM) for 30 min, followed by administration of Aβ42 (5 μM) for 12 h.

    View All FGFR Isoform Specific Products:

    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Dovitinib(CHIR-258; TKI258) lactate is a potent inhibitor of fibroblast growth factor receptor 3 (FGFR3) with an IC50 of 5 nM.

    IC50 & Target[1]

    FGFR3

    5 nM (IC50)

    In Vitro

    Dovitinib potently inhibits FGFR3 with an IC50 of 5 nM in in vitro kinase assays and selectively inhibits the growth of B9 cells and human myeloma cell lines expressing wild-type or activated mutant FGFR3. Addition of interleukin 6 (IL-6) or insulin growth factor 1 or coculture on stroma does not confer resistance to dovitinib. In primary myeloma cells dovitinib inhibits downstream extracellular signal-regulated kinase (ERK) 1/2 phosphorylation with an associated cytotoxic response[1]. Treatment of SK-HEP1 cells with dovitinib results in G2/M cell cycle arrest, inhibition of colony formation in soft agar and blockade of bFGF-induced cell migration. Dovitinib inhibits basal expression and FGF-induced phosphorylation of FGFR-1, FRS2-α and ERK1/2[2].

    In Vivo

    Dovitinib demonstrates significant antitumor and antimetastatic activities in HCC xenograft models. Dovitinib potently inhibits tumor growth of six HCC lines. Inhibition of angiogenesis correlates with inactivation of FGFR/PDGFR-β/VEGFR-2 signaling pathways. Dovitinib also causes dephosphorylation of retinoblastoma, upregulation of p-histone H2A-X and p27, and downregulation of p-cdk-2 and cyclin B1, which results in a reduction in cellular proliferation and the induction of tumor cell apoptosis[2].

    Clinical Trial
    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 2.0725 mL 10.3625 mL 20.7250 mL
    5 mM 0.4145 mL 2.0725 mL 4.1450 mL
    10 mM 0.2072 mL 1.0362 mL 2.0725 mL
    Please refer to the solubility information to select the appropriate solvent.
    Cell Assay
    [2]

    To determine IC50 for SK-HEP1 cells, cells are plated at a density of 2×104 cells per dish. After 48 h, cells are treated with 0, 0.01, 0.1, 1, 5, 10, 50, 100 μM dovitinib in DMEM containing 1% FBS for 24 h. Cell viability is determined with Cell Proliferation Assay. IC50 is calculated by nonlinear regression analysis using GraphPad Prism software[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [2]

    Mice: Six HCC lines (06-0606, 26-0808A, 26-1004, 25-0705A, 5-1318, 21-0208) are used to establish tumors in male SCID mice. or dose-esponse experiments, mice bearing the 06-0606 xenografts re orally given vehicle (5% dextrose) or two doses of dovitinib (50 and 75 mg/kg) daily for 14 days. For time-dependent inhibition of dovitinib targets, mice bearing 06-0606 tumors are given orally 200 μL of either vehicle (n=6) or 50 mg/kg/day of dovitinib (n=10)[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    482.51

    Formula

    C₂₄H₂₇FN₆O₄

    CAS No.

    692737-80-7

    SMILES

    O=C(N1)C(C(NC2=C3)=NC2=CC=C3N4CCN(C)CC4)=C(N)C5=C1C=CC=C5F.O=C(O)C(C)O

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: ≥ 30 mg/mL

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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    Inquiry Information

    Product Name:
    Dovitinib lactate
    Cat. No.:
    HY-10207
    Quantity: