2. Protein Tyrosine Kinase/RTK
  3. FGFR
  4. BLU9931

BLU9931 is a potent, highly selective, and irreversible fibroblast growth factor receptor 4 (FGFR4) inhibitor with an IC50 of 3 nM and a Kd of 6 nM. BLU9931 has significant antitumor activity.

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

BLU9931 Chemical Structure

BLU9931 Chemical Structure

CAS No. : 1538604-68-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 67 In-stock
Solution
10 mM * 1 mL in DMSO USD 67 In-stock
Solid
1 mg USD 31 In-stock
5 mg USD 61 In-stock
10 mg USD 99 In-stock
50 mg USD 275 In-stock
100 mg USD 495 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 8 publication(s) in Google Scholar

BLU9931 Related Antibodies

Top Publications Citing Use of Products

    BLU9931 purchased from MedChemExpress. Usage Cited in: Int J Oncol. 2017 Nov;51(5):1611-1620.  [Abstract]

    Western blot detection of the expression of related molecules including signal pathway (STAT3), apoptosis (cleaved caspase‑3), cell cycle (cyclin D1 and P27kip1) and epithelial-mesenchymal transition (E-cadherin and vimentin) in HCT116 and SW620 cells when treated by the single and combination of 5-FU and Blu9931.

    View All FGFR Isoform Specific Products:

    View All Isoforms
    FGFR FGFR1 FGFR2 FGFR3 FGFR4 FGF21

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    BLU9931 is a potent, highly selective, and irreversible fibroblast growth factor receptor 4 (FGFR4) inhibitor with an IC50 of 3 nM and a Kd of 6 nM. BLU9931 has significant antitumor activity[1].

    IC50 & Target

    FGFR1

    591 nM (IC50)

    FGFR2

    493 nM (IC50)

    FGFR3

    150 nM (IC50)

    FGFR4

    3 nM (IC50)

    In Vitro

    BLU9931 inhibits proliferation of HCC cell lines that express an intact FGFR4 signaling complex, with EC50s of 0.07 μM, 0.11 μM and 0.02 μM for Hep 3B, HuH7 and JHH7 cells, respectively[1].
    BLU9931 (0.3-300 nM; 1 hour; MDA-MB-453 and Hep 3B cells) treatment demonstrates potent, dose-dependent reduction of phosphorylation of FGFR4 signaling pathway components, including fibroblast growth factor receptor substrate 2 (FRS2), MAPK, and AKT in MDA-MB-453 cells. BLU9931 shows dose-dependent inhibition of the signaling cascade downstream of FGFR4. BLU9931 exhibits potent inhibition of phosphorylation of the FGFR4 pathway components in Hep 3B cells. BLU9931 treatment leads to induction of caspase-3/7 activity, indicative of induction of apoptosis that results in inhibition of signaling downstream of FGFR4[1].
    BLU9931 (100 nM; 0 -24 hours; Hep 3B cells) treatment increases CYP7A1 mRNA expression and the expression of the proliferative marker EGR1 is inhibited[1].

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

    BLU9931 Related Antibodies

    Western Blot Analysis[1]

    Cell Line: MDA-MB-453 and Hep 3B cells
    Concentration: 0.3 nM, 1 nM, 3 nM, 10 nM, 30 nM, 100 nM, 300 nM
    Incubation Time: 1 hour
    Result: Demonstrated potent, dose-dependent reduction of phosphorylation of FGFR4 signaling pathway components, including fibroblast growth factor receptor substrate 2 (FRS2), MAPK, and AKT in MDA-MB-453 and Hep 3B cells.

    RT-PCR[1]

    Cell Line: Hep 3B cells
    Concentration: 100 nM
    Incubation Time: 0 hour, 4 hours, 8 hour, 24 hours
    Result: Increased CYP7A1 mRNA expression. And the expression of the proliferative marker EGR1 was inhibited.
    In Vivo

    BLU9931 (10-100 mg/kg; oral administration; twice every day; for 21 days; mice) treatment demonstrates antitumor activity in HCC xenograft models[1].

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

    Animal Model: Mice injected with Hep 3B cells[1]
    Dosage: 10 mg/kg, 30 mg/kg or 100 mg/kg
    Administration: Oral administration; twice every day; for 21 days
    Result: Resulted in dose-dependent growth inhibition of Hep 3B tumors. Prevented weight loss in a dose-dependent manner.
    Molecular Weight

    509.38

    Formula

    C26H22Cl2N4O3
    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    C=CC(NC1=CC=CC(C)=C1NC2=NC=C3C=C(C4=C(Cl)C(OC)=CC(OC)=C4Cl)C=CC3=N2)=O
    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 : 83.33 mg/mL (163.59 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9632 mL 9.8159 mL 19.6317 mL
    5 mM 0.3926 mL 1.9632 mL 3.9263 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
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    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

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

      Solubility: ≥ 2.08 mg/mL (4.08 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

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

      Solubility: ≥ 2.08 mg/mL (4.08 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.97%

    COA (250 KB) HNMR (276 KB) RP-HPLC (255 KB) LCMS (110 KB)

    Handling Instructions (2659 KB)
    References

    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.9632 mL 9.8159 mL 19.6317 mL 49.0793 mL
    5 mM 0.3926 mL 1.9632 mL 3.9263 mL 9.8159 mL
    10 mM 0.1963 mL 0.9816 mL 1.9632 mL 4.9079 mL
    15 mM 0.1309 mL 0.6544 mL 1.3088 mL 3.2720 mL
    20 mM 0.0982 mL 0.4908 mL 0.9816 mL 2.4540 mL
    25 mM 0.0785 mL 0.3926 mL 0.7853 mL 1.9632 mL
    30 mM 0.0654 mL 0.3272 mL 0.6544 mL 1.6360 mL
    40 mM 0.0491 mL 0.2454 mL 0.4908 mL 1.2270 mL
    50 mM 0.0393 mL 0.1963 mL 0.3926 mL 0.9816 mL
    60 mM 0.0327 mL 0.1636 mL 0.3272 mL 0.8180 mL
    80 mM 0.0245 mL 0.1227 mL 0.2454 mL 0.6135 mL
    100 mM 0.0196 mL 0.0982 mL 0.1963 mL 0.4908 mL
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    BLU9931 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.

    Keywords:

    BLU99311538604-68-0BLU 9931BLU-9931FGFRFibroblast growth factor receptorInhibitorinhibitorinhibit

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