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


Cat. No.: HY-12823 Purity: 99.33%
Handling Instructions

BLU9931 is a potent, selective, and irreversible FGFR4 inhibitor with an IC50 of 3 nM.

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
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 148 In-stock
Estimated Time of Arrival: December 31
5 mg USD 132 In-stock
Estimated Time of Arrival: December 31
10 mg USD 180 In-stock
Estimated Time of Arrival: December 31
50 mg USD 540 In-stock
Estimated Time of Arrival: December 31
100 mg USD 888 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products

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

    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.

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    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References


    BLU9931 is a potent, selective, and irreversible FGFR4 inhibitor with an IC50 of 3 nM.

    IC50 & Target

    IC50: 3 nM (FGFR4)

    In Vitro

    In MDA-MB-453 cells, BLU9931 potently inhibits phosphorylation of FGFR4 signaling pathway. BLU9931 inhibits proliferation of HCC cell lines that express an intact FGFR4 signaling complex, such as Hep 3B, HUH-7, and JHH-7 cell lines, with EC50 of <1 μM. BLU9931 also inhibits proliferation in PDX-derived cell lines with an intact FGFR4 signaling pathway[1]. BLU9931 induces tumor shrinkage in hepatocellular carcinoma models that express a functioning ligand/receptor complex consisting of FGF19/FGFR4/KLB and adds to a growing list of anti-FGFR4 agents[2].

    In Vivo

    BLU9931 (300 mg/kg, p.o.) leads to tumor regression and prevents this weight loss in mice bearing the FGF19-amplified Hep 3B liver tumors. In mice bearing the FGF19-overexpressing PDX-derived LIXC012 xenografts, treatment with BLU9931 (300 mg/kg, p.o.) also leads to tumor regression[1]

    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 17 mg/mL (33.37 mM; Need ultrasonic and warming)

    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
    10 mM 0.1963 mL 0.9816 mL 1.9632 mL
    *Please refer to the solubility information to select the appropriate solvent.
    Kinase Assay

    FGFR kinase inhibition assays are performed at KM for ATP. Picomolar to low nanomolar concentrations of FGFR proteins are incubated in 1× Kinase Reaction Buffer (KRB) with 1 μM of CSKtide and 50 to 250 of μM ATP at 25°C for 90 minutes in the presence or absence of a dosed concentration series of inhibitor. All reactions are terminated by the addition of Stop buffer, and plates are read on a Caliper EZReader2. IC50 values are fit with a four-parameter log[Inhibitor] versus response model with floating Hill Slope.

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

    Cell Assay

    established and PDX-derived HCC cell lines are seeded in 96-well plates in respective growth media, allowed to attach overnight, and treated with a dilution series of test compounds for two cell-doubling times. Cell viability is determined by CellTiter-Glo, and results represented as background-subtracted relative light units normalized to a DMSO-treated control. Relative EC50 values are determined at 50% inhibition between the top and bottom plateau of the dose-response curve.

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

    Animal Administration

    BLU9931 is formulated in 0.5% carboxymethylcellulose/1% Tween 80 and dosed orally as a suspension twice daily. Sorafenib is dissolved in Cremaphor:EtOH (1:1) and diluted with saline or water to yield the stock solution. Sorafenib is dosed orally once daily. All compound doses are expressed as mg/kg free base. For PK-PD studies, 3 mice are included in each treatment group. Mice receive four doses of compound or vehicle. Blood and tumors are collected 8, 12, 20, and 24 hours following the last dose. The concentration of BLU9931 in plasma is determined by LC/MS-MS. A section of each tumor is immediately frozen in liquid nitrogen and stored at −80°C.

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

    Molecular Weight




    CAS No.





    Room temperature in continental US; may vary elsewhere

    Purity: 99.33%

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    Cat. No.: HY-12823