2. Protein Tyrosine Kinase/RTK
  3. FGFR
  4. Rogaratinib

Rogaratinib  (Synonyms: BAY1163877)

Cat. No.: HY-100019 Purity: 99.86%
COA Handling Instructions

Rogaratinib (BAY1163877) is a potent and selective fibroblast growth factor receptor (FGFR) inhibitor. Rogaratinib inhibits FGFRs with IC50s of 11.2 nM (FGFR1), <1 nM (FGFR2), 18.5 nM (FGFR3), 127 nM (VEGFR3/FLT4), 201 nM (FGFR4), respectively.

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

Rogaratinib Chemical Structure

Rogaratinib Chemical Structure

CAS No. : 1443530-05-9

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 216 In-stock
Solution
10 mM * 1 mL in DMSO USD 216 In-stock
Solid
1 mg USD 80 In-stock
5 mg USD 210 In-stock
10 mg USD 380 In-stock
50 mg USD 1400 In-stock
100 mg USD 2250 In-stock
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Customer Review

Based on 4 publication(s) in Google Scholar

Rogaratinib Related Antibodies

Top Publications Citing Use of Products

    Rogaratinib purchased from MedChemExpress. Usage Cited in: IOP Conf Ser Mater Sci Eng. 562 (2019) 012128.

    Effects of BAY1163877 on the Expression of p-FGFR1/FGFR1 and p-STAT3/STAT3 Protein in Breast Cancer Cell Lines MDA-MB-231 and MCF-7 are showed.

    View All FGFR Isoform Specific Products:

    View All Isoforms
    FGFR FGFR1 FGFR2 FGFR3 FGFR4 FGF21

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Rogaratinib (BAY1163877) is a potent and selective fibroblast growth factor receptor (FGFR) inhibitor. Rogaratinib inhibits FGFRs with IC50s of 11.2 nM (FGFR1), <1 nM (FGFR2), 18.5 nM (FGFR3), 127 nM (VEGFR3/FLT4), 201 nM (FGFR4), respectively[1][2].

    IC50 & Target[1]

    FGFR1

     

    FGFR2

     

    FGFR3

     

    FGFR4

     

    In Vitro

    Of the 24 cell lines, 2 FGFR1-amplified lung cancer (LC) cell lines, H1581 and DMS114, show extreme sensitivity to Rogaratinib (BAY1163877) (GI50 values ranging from 36 to 244 nM). Treatment with Rogaratinib results in a significant decrease in colonies formed by H1581P cells, but not by H1581AR and BR cells. Ectopic expression of Met significantly induces resistance to Rogaratinib in MTT assays. Met overexpression induces activation of downstream extracellular signal-regulated kinase 1/2 (ERK1/2) and AKT, which cannot be abrogated by Rogaratinib treatment[1].

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

    Rogaratinib Related Antibodies
    Clinical Trial
    Molecular Weight

    466.56

    Appearance

    Solid

    Formula

    C23H26N6O3S
    CAS No.
    SMILES

    O=C1NCCN(CC2=C(COC)C(C3=CC4=CC(C)=CC(OC)=C4S3)=C5C(N)=NC=NN52)C1
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 5 mg/mL (10.72 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1433 mL 10.7167 mL 21.4335 mL
    5 mM 0.4287 mL 2.1433 mL 4.2867 mL
    10 mM 0.2143 mL 1.0717 mL 2.1433 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: ≥ 0.56 mg/mL (1.20 mM); Clear solution

    • 2.

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

      Solubility: ≥ 0.56 mg/mL (1.20 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 0.56 mg/mL (1.20 mM); Clear solution

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

    Purity: 99.86%

    COA (261 KB) HNMR (251 KB) LCMS (95 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [1]

    Cells (3000 cells/well) are seeded on 96-well plates at 37°C. After overnight incubation, the cells are treated with Rogaratinib for 72 h. Then, MTT reagent [3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazoliumbromide] is added to each well and incubated for 4 h at 37°C. MTT solubilization solution/stop mix is added to each well, mixed, and the plates are incubated overnight at 37°C. After measuring the absorbance at 570 nm, the data are graphically displayed[1].

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

    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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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

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    × = ×
    C1   V1   C2   V2

    Keywords:

    Rogaratinib1443530-05-9BAY1163877BAY 1163877BAY-1163877FGFRFibroblast growth factor receptorInhibitorinhibitorinhibit

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