Resigratinib (Synonyms: KIN-3248)

Name: Resigratinib
Brand: MedChemExpress
SKU: HY-156632
Rating: 4.5 (0 reviews)

Cat. No.: HY-156632 Purity: 99.43%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

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 화학구조

CAS No. : 2750709-91-0

사이즈	재고	수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	해외재고보유	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	해외재고보유	Estimated Time of Arrival: December 31
Solid
1 mg	해외재고보유	Estimated Time of Arrival: December 31
5 mg	해외재고보유	Estimated Time of Arrival: December 31
10 mg	해외재고보유	Estimated Time of Arrival: December 31
25 mg	해외재고보유	Estimated Time of Arrival: December 31
50 mg	해외재고보유	Estimated Time of Arrival: December 31
100 mg	해외재고보유	Estimated Time of Arrival: December 31
200 mg	견적 받기
500 mg	견적 받기

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고객리뷰

Based on 1 Customer Validation

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Biological Activity
순도&문서
References
고객리뷰

제품 설명

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

분자량

523.53

화학식

C₂₆H₂₇F₂N₇O₃

CAS No.

2750709-91-0

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

선적

Room temperature in continental US; may vary elsewhere.

보관

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

용액&용해도

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
10 mM	0.1910 mL	0.9551 mL	1.9101 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.

몰농도 계산기
농도 희석 계산기

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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.
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

mg/kg

Animal weight
(per animal)

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.

순도&문서

Purity: 99.43%

Select Batch:

Data Sheet (277 KB) SDS (252 KB)

COA (253 KB) HNMR (141 KB) LCMS (102 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

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

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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Resigratinib (Synonyms: KIN-3248)

고객리뷰

Resigratinib Related Antibodies

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

순도&문서

References

고객리뷰

Resigratinib Related Antibodies

몰농도 계산기

농도 희석 계산기

Complete Stock Solution Preparation Table

Resigratinib Related Classifications

Keywords:

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