1. Protein Tyrosine Kinase/RTK
  2. FGFR

BLU9931 

Cat. No.: HY-12823 Purity: 98.05%
Handling Instructions

BLU9931 is a potent, selective, and irreversible FGFR4 inhibitor with IC50 of 3 nM, about 297-, 184-, and 50-fold selectivity over FGFR1/2/3, respectively.

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
5 mg USD 132 In-stock
10 mg USD 180 In-stock
50 mg USD 540 In-stock
100 mg USD 888 In-stock
200 mg   Get quote  
500 mg   Get quote  

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    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.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    BLU9931 is a potent, selective, and irreversible FGFR4 inhibitor with IC50 of 3 nM, about 297-, 184-, and 50-fold selectivity over FGFR1/2/3, respectively.

    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]

    References
    Preparing Stock Solutions
    Concentration Volume 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
    [1]

    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
    [1]

    BLU9931 is dissolved in DMSO.

    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
    [1]

    BLU9931 is formulated in 0.5% carboxymethylcellulose/1% Tween 80.

    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.

    References
    Molecular Weight

    509.38

    Formula

    C₂₆H₂₂Cl₂N₄O₃

    CAS No.

    1538604-68-0

    SMILES

    C=CC(NC1=CC=CC(C)=C1NC2=NC=C3C=C(C4=C(Cl)C(OC)=CC(OC)=C4Cl)C=CC3=N2)=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: 17 mg/mL

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

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    Inquiry Information

    Product Name:
    BLU9931
    Cat. No.:
    HY-12823
    Quantity: