1. Protein Tyrosine Kinase/RTK
  2. FGFR
  3. FGFR4-IN-5

FGFR4-IN-5 

Cat. No.: HY-131704 Purity: 98.06%
Handling Instructions

FGFR4-IN-5 is a potent and selective covalent FGFR4 inhibitor with an IC50 of 6.5 nM. FGFR4-IN-5 exhibits strong anti-tumor activity in vivo and can be used for hepatocellular carcinoma research.

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

FGFR4-IN-5 Chemical Structure

FGFR4-IN-5 Chemical Structure

CAS No. : 1628793-01-0

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 572 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 572 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 500 In-stock
Estimated Time of Arrival: December 31
10 mg USD 850 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
50 mg USD 3000 In-stock
Estimated Time of Arrival: December 31
100 mg USD 4600 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

FGFR4-IN-5 is a potent and selective covalent FGFR4 inhibitor with an IC50 of 6.5 nM. FGFR4-IN-5 exhibits strong anti-tumor activity in vivo and can be used for hepatocellular carcinoma research[1].

IC50 & Target[1]

FGFR4

6.5 nM (IC50)

FGFR2

505 nM (IC50)

In Vivo

FGFR4-IN-5 (oral gavage; 10 mg/kg; single dose) reveals a high Cmax, low clearance, the Cmax values are 423 ng/ml, 588 ng/ml, and 2820 ng/ml in mice, rat and cynamolgus monkey, respectively. And the oral bioavailability are 20, 12, and 27% in mouse, rat, and cyno, respectively[1].
FGFR4-IN-5 (oral gavage; 100 mg/kg; twice daily; 28 days) exhibits strong antitumor activity in an orthotopic Hep3B HTX model[1].
FGFR4-IN-5 (oral gavage; 10, 30, and 100 mg/kg; twice daily; 11 days) results in dose-dependent growth inhibition of resistant tumors. Tumor regression is observed at 30 and 100 mg/kg, with %ΔT/ΔC of 67% and 70%, respectively. However, treatment with sorafenib at 100 mg/kg once daily does not provide any benefit in vivo[1].

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

Animal Model: Hep3B cell bearing mice model[1]
Dosage: 100 mg/kg
Administration: Oral gavage; 100 mg/kg; twice daily; 28 days
Result: Resulted in tumor regression and sustained growth inhibition.
Animal Model: Sorafenib-resistant tumors established to mice bearing Huh7 tumors[1]
Dosage: 10, 30, and 100 mg/kg
Administration: Oral gavage; 10, 30, and 100 mg/kg; twice daily; 11 days
Result: Resulted in dose-dependent growth inhibition of resistant tumors.
Molecular Weight

520.37

Formula

C₂₃H₂₃Cl₂N₅O₅

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

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

DMSO : 100 mg/mL (192.17 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9217 mL 9.6085 mL 19.2171 mL
5 mM 0.3843 mL 1.9217 mL 3.8434 mL
10 mM 0.1922 mL 0.9609 mL 1.9217 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 (4.80 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (4.80 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Product Name:
FGFR4-IN-5
Cat. No.:
HY-131704
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