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

Resigratinib (KIN-3248) is an irreversible and orally active covalent inhibitor of FGFR1-4 that effectively inhibits wild-type and drug-resistant mutations (such as FGFR2 V565F, FGFR3 V555M). Resigratinib covalently binds to the Cys492 site of FGFR, blocks the FGFR signaling pathway, inhibits tumor cell proliferation and induces apoptosis. Resigratinib can be used for the study of FGFR2/3-driven solid tumors (such as cholangiocarcinoma and bladder cancer).

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Resigratinib Chemical Structure

Resigratinib Chemical Structure

CAS No. : 2750709-91-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

Resigratinib Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

Resigratinib (KIN-3248) is an irreversible and orally active covalent inhibitor of FGFR1-4 that effectively inhibits wild-type and drug-resistant mutations (such as FGFR2 V565F, FGFR3 V555M). Resigratinib covalently binds to the Cys492 site of FGFR, blocks the FGFR signaling pathway, inhibits tumor cell proliferation and induces apoptosis. Resigratinib can be used for the study of FGFR2/3-driven solid tumors (such as cholangiocarcinoma and bladder cancer)[1][2].

In Vitro

Resigratinib has an IC50 of 0.6-2.3 nM for wild-type FGFR1-4 and an IC50 of <25 nM for drug-resistant mutations such as FGFR2 V565F, FGFR3 V555M, and FGFR3 N550K. Resigratinib has a selectivity of >90% for FGFR family kinase activity and weak inhibitory effects on other kinases[1].
Resigratinib (compound 11) (0.1 nM-10 μM; 72 h) inhibits cell viability of cancer cell lines expressing FGFR2 or FGFR3 (e.g., SNU-16, RT112)[1].

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

Resigratinib Related Antibodies

Cell Viability Assay[1]

Cell Line: FGFR2 or FGFR3 expressing Cellular Viability in:
(FGFR2) SNU16, CCLP-1, CCLP-1V565F, CCLP-1N550H, CCLP-1N550K, ICC13-7, ICC13-7V565F, ICC13-7N550K
(FGFR3) RT112 (WT), RT112:FGFR3-TACC3, RT112:FGFR3-TACC3, V555M RT112:FGFR3-TACC3N540K, RT112:FGFR3-TACC3K650M
Concentration: 0.1 nM-10 μM
Incubation Time: 72 h
Result: Showed IC50s of 3.6 nM (SNU16), 3.5 nM (CCLP-1), 5.2 nM (CCLP-1V565F), 2.9 nM (CCLP-1N550H), 10.2 nM (CCLP-1N550K), 2.0 nM (ICC13-7), 4.3 nM (ICC13-7V565F), 8.0 nM (ICC13-7N550K); 4.0 nM (RT112-WT), 8.2 nM (RT112:FGFR3-TACC3), 45.2 nM (RT112:FGFR3-TACC3), 22.4 nM (V555M RT112:FGFR3-TACC3N540K), 16.2 nM (RT112:FGFR3-TACC3K650M), respectively.
In Vivo

Resigratinib (5-15 mg/kg; oral gavage; once daily; for 21-38 days) significantly inhibits tumor growth in FGFR2/3-driven tumor models (including SNU-16 gastric cancer, RT112 bladder cancer, and STO357 gastric adenocarcinoma) in NSG or nude mice. Resigratinib has synergistic antitumor effects with EGFR/MEK inhibitors in vivo[1].

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

Animal Model: Female NSG mice (6-10 weeks old) with SNU-16 (FGFR2-amplified gastric cancer) xenograft model[1]
Dosage: 2, 5, 15 mg/kg
Administration: Oral gavage, once daily, 21 days
Result: Dose-dependent tumor growth inhibition, with TGI of 69%, 81%, and 93% at 2, 5, and 15 mg/kg, respectively.
No significant body weight loss was noted, and phospho-ERK signaling was suppressed in tumor tissues.
Molecular Weight

523.53

Formula

C26H27F2N7O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CNC1=C(C(N)=O)C(C#CC2=C(F)C=C(N(C3CC3)C=N4)C4=C2F)=NN1[C@H]5C[C@@H](N(C5)C(C=C)=O)COC
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 : 100 mg/mL (191.01 mM; Need ultrasonic; 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 1.9101 mL 9.5506 mL 19.1011 mL
5 mM 0.3820 mL 1.9101 mL 3.8202 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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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: ≥ 5 mg/mL (9.55 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (9.55 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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
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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
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9101 mL 9.5506 mL 19.1011 mL 47.7528 mL
5 mM 0.3820 mL 1.9101 mL 3.8202 mL 9.5506 mL
10 mM 0.1910 mL 0.9551 mL 1.9101 mL 4.7753 mL
15 mM 0.1273 mL 0.6367 mL 1.2734 mL 3.1835 mL
20 mM 0.0955 mL 0.4775 mL 0.9551 mL 2.3876 mL
25 mM 0.0764 mL 0.3820 mL 0.7640 mL 1.9101 mL
30 mM 0.0637 mL 0.3184 mL 0.6367 mL 1.5918 mL
40 mM 0.0478 mL 0.2388 mL 0.4775 mL 1.1938 mL
50 mM 0.0382 mL 0.1910 mL 0.3820 mL 0.9551 mL
60 mM 0.0318 mL 0.1592 mL 0.3184 mL 0.7959 mL
80 mM 0.0239 mL 0.1194 mL 0.2388 mL 0.5969 mL
100 mM 0.0191 mL 0.0955 mL 0.1910 mL 0.4775 mL
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Resigratinib 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:

Resigratinib2750709-91-0KIN-3248KIN3248KIN 3248FGFRFibroblast growth factor receptorInhibitorinhibitorinhibit

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