Art. -Nr.: HY-156632

Resigratinib

Name: Resigratinib
Brand: MedChemExpress
SKU: HY-156632
Price: 100.00 USD
Availability: InStock
Rating: 5 (1 reviews)

(Synonyms: KIN-3248)

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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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Reinheit: 99.43%
CAS. Nr.: 2750709-91-0
Formel: C₂₆H₂₇F₂N₇O₃
Molecular Weight:523.53

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Resigratinib Chemical Structure

CAS. Nr.: 2750709-91-0

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Cellular Effect

Cell Line	Type	Value	Description	References
RT-112	IC₅₀	16.2 nM Compound: 11; KIN-3248	Antiproliferative activity against human RT-112 cells expressing FGFR3 K650M mutant assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay Antiproliferative activity against human RT-112 cells expressing FGFR3 K650M mutant assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay	[PMID: 38267212]
RT-112	IC₅₀	22.4 nM Compound: 11; KIN-3248	Antiproliferative activity against human RT-112 cells expressing FGFR3 N540K mutant assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay Antiproliferative activity against human RT-112 cells expressing FGFR3 N540K mutant assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay	[PMID: 38267212]
RT-112	IC₅₀	4 nM Compound: 11; KIN-3248	Antiproliferative activity against human RT-112 cells assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay Antiproliferative activity against human RT-112 cells assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay	[PMID: 38267212]
RT-112	IC₅₀	45.2 nM Compound: 11; KIN-3248	Antiproliferative activity against human RT-112 cells expressing FGFR3 V555M mutant assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay Antiproliferative activity against human RT-112 cells expressing FGFR3 V555M mutant assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay	[PMID: 38267212]
RT-112	IC₅₀	8.2 nM Compound: 11; KIN-3248	Antiproliferative activity against human RT-112 cells expressing FGFR3 assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay Antiproliferative activity against human RT-112 cells expressing FGFR3 assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay	[PMID: 38267212]
SNU-16	IC₅₀	3.6 nM Compound: 11; KIN-3248	Antiproliferative activity against human SNU-16 cells assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay Antiproliferative activity against human SNU-16 cells assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay	[PMID: 38267212]

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.

Cell Viability Assay^[1]

Cell Line:

FGFR2 or FGFR3 expressing Cellular Viability in:
(FGFR2) SNU16, CCLP-1, CCLP-1^V565F, CCLP-1^N550H, CCLP-1^N550K, ICC13-7, ICC13-7^V565F, ICC13-7^N550K
(FGFR3) RT112 (WT), RT112:FGFR3-TACC3, RT112:FGFR3-TACC3, V555M RT112:FGFR3-TACC3^N540K, RT112:FGFR3-TACC3^K650M
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-1^V565F), 2.9 nM (CCLP-1^N550H), 10.2 nM (CCLP-1^N550K), 2.0 nM (ICC13-7), 4.3 nM (ICC13-7^V565F), 8.0 nM (ICC13-7^N550K); 4.0 nM (RT112-WT), 8.2 nM (RT112:FGFR3-TACC3), 45.2 nM (RT112:FGFR3-TACC3), 22.4 nM (V555M RT112:FGFR3-TACC3^N540K), 16.2 nM (RT112:FGFR3-TACC3^K650M), 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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 2750709-91-0
Appearance Solid
Molecular Weight 523.53
Formel C₂₆H₂₇F₂N₇O₃
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
Synonyms

KIN-3248
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9101 mL

9.5506 mL

19.1011 mL

5 mM

0.3820 mL

1.9101 mL

3.8202 mL

10 mM

0.1910 mL

0.9551 mL

1.9101 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Tyhonas JS, et al. Discovery of KIN-3248, An Irreversible, Next Generation FGFR Inhibitor for the Treatment of Advanced Tumors Harboring FGFR2 and/or FGFR3 Gene Alterations. J Med Chem. 2024 Feb 8;67(3):1734-1746. [Content Brief]

[2]. Balasooriya ER, et al. The Irreversible FGFR Inhibitor KIN-3248 Overcomes FGFR2 Kinase Domain Mutations. Clin Cancer Res. 2024 May 15;30(10):2181-2192. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Pemigatinib

Gunagratinib

Infigratinib

Futibatinib

Derazantinib

Rogaratinib

Fexagratinib

Fisogatinib

Zoligratinib

LY2874455

E7090

H3B-6527

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Bioz

Resigratinib

Pemigatinib

Gunagratinib

Infigratinib

Futibatinib

Derazantinib

Rogaratinib

Fexagratinib

Fisogatinib

Zoligratinib

LY2874455

E7090

H3B-6527

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Resigratinib Related Classifications

HY-156632 Related Classifications

Bioz