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  3. BLU9931

BLU9931 

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

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

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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
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100 mg USD 888 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products

Publications Citing Use of MCE BLU9931

    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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    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[1]

    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].

    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].

    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.

    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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    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)

    H2O : < 0.1 mg/mL (insoluble)

    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
    10 mM 0.1963 mL 0.9816 mL 1.9632 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: ≥ 2.5 mg/mL (4.91 mM); Clear solution

    • 2.

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

      Solubility: 2.5 mg/mL (4.91 mM); Suspended solution; Need ultrasonic

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (4.91 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References

    Purity: 99.33%

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    Keywords:

    BLU9931BLU 9931BLU-9931FGFRFibroblast growth factor receptorInhibitorinhibitorinhibit

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    Product name:
    BLU9931
    Cat. No.:
    HY-12823
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