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Cat. No.: HY-189241

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FGFR-IN-29

FGFR-IN-29 is an orally active pan-FGFR inhibitor that suppresses the kinase activities of FGFR1, FGFR2, FGFR3, and FGFR4. FGFR-IN-29 blocks the intracellular phosphorylation process of FGFR and arrests downstream tumor cell proliferation signaling. FGFR-IN-29 inhibits tumor growth in solid tumor xenograft mouse models. FGFR-IN-29 is applicable for cancer-related research.

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

Formula: C₃₈H₄₀ClF₃N₆O₄
Molecular Weight:737.21

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

FGFR-IN-29 Chemical Structure

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Use of MCE Products

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

IC₅₀ & Target

^[1]

FGFR1

5.70 nM (IC₅₀)

FGFR2

2.37 nM (IC₅₀)

FGFR3

3.78 nM (IC₅₀)

FGFR4

7.67 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
SNU-16	IC50	0.66 nM	Antiproliferative activity against human SNU-16 FGFR2-dependent cancer cells assessed by CCK8 assay after 72 h of incubation. Antiproliferative activity against human SNU-16 FGFR2-dependent cancer cells assessed by CCK8 assay after 72 h of incubation.	42612288
KATO III stomach cancer cell line	IC50	0.72 nM	Antiproliferative activity against human KATO3 FGFR2-dependent cancer cells assessed by CCK8 assay after 72 h of incubation. Antiproliferative activity against human KATO3 FGFR2-dependent cancer cells assessed by CCK8 assay after 72 h of incubation.	42612288
RT-112	IC50	36.61 nM	Antiproliferative activity against human RT112 FGFR3-dependent cancer cells assessed by CCK8 assay after 72 h of incubation. Antiproliferative activity against human RT112 FGFR3-dependent cancer cells assessed by CCK8 assay after 72 h of incubation.	42612288
Huh-7	IC50	8.14 nM	Antiproliferative activity against human HuH-7 FGFR4-dependent cancer cells assessed by CCK8 assay after 72 h of incubation. Antiproliferative activity against human HuH-7 FGFR4-dependent cancer cells assessed by CCK8 assay after 72 h of incubation.	42612288
MDA-MB-453	IC50	10.50 nM	Antiproliferative activity against human MDA-MB-453 FGFR4-dependent cancer cells assessed by CCK8 assay after 72 h of incubation. Antiproliferative activity against human MDA-MB-453 FGFR4-dependent cancer cells assessed by CCK8 assay after 72 h of incubation.	42612288

In Vitro

FGFR-IN-29 (compound 18) exhibits potent and broad-spectrum in vitro antiproliferative activity in multiple human solid tumor cell lines, with IC₅₀ values below 10.5 nM against SNU-16, KATO3, HuH-7 and MDA-MB-453 cells^[1].
FGFR inhibitor 29 (0-500 nM; 2 h) effectively blocks FGFR-mediated signaling in vitro, and its mechanism of action involves inhibiting the phosphorylation of all four FGFR isoforms in intact SNU-16 gastric cancer cells in a concentration-dependent manner after 2 h of treatment^[1].
FGFR-IN-29 is a highly potent pan-FGFR inhibitor, which exhibits nanomolar IC₅₀ values against all four FGFR isoforms (FGFR1 IC₅₀ = 5.70 nM, FGFR2 IC₅₀ = 2.37 nM, FGFR3 IC₅₀ = 3.78 nM, FGFR4 IC₅₀ = 7.67 nM), with acceptable kinase selectivity^[1].

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

Western Blot Analysis^[1]

Cell Line:

SNU-16 human gastric cancer cells
Concentration:

0, 0.8, 4, 20, 100, 500 nM
Incubation Time:

2 h (phosphorylation assay)
48 h (cell lysis pre-treatment)
Result:

Reduces phosphorylation levels of FGFR1, FGFR2, FGFR3, and FGFR4 in SNU-16 cells in a dose-dependent manner, with residual phosphorylated FGFR signal still present at 4 nM, while phosphorylated FGFR1 signal is fully eliminated at 20 nM.

Parmacokinetics

Species	Dose	Route	C_max	T_1/2	T_max	AUC_0-t	AUC_0-∞	MRT_0-t	MRT_0-∞	F	C₀	CL	V_ss
Mice^[1]	2 mg/kg	i.v.	/	1.04 h	0.08 h	858 ng·h/mL	860 ng·h/mL	0.87 h	0.89 h	/	4189 ng/mL	38.90 mL/h/kg	1.99 L/kg
Mice^[1]	10 mg/kg	p.o.	2373 ng/mL	0.81 h	0.33 h	1791 ng·h/mL	1793 ng·h/mL	0.95 h	0.97 h	41.70 %	/	/	/

In Vivo

FGFR-IN-29 (compound 18) (15-60 mg/kg; p.o.; once daily for 21 days) achieves 92.71% tumor growth inhibition in the HuH-7 xenograft mouse model, produces 49.80% tumor growth inhibition in the SNU-16 xenograft mouse model, and exerts 67.61% tumor growth inhibition in the RT112 xenograft mouse model; none of the above effects are accompanied by significant body weight loss^[1].
FGFR-IN-29 (500-1000 mg/kg; p.o.; once daily; 14 days) exhibits an excellent safety profile^[1].

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

Animal Model:

BALB/c nude mice (Female, 5 × 10⁶ HuH-7 cells were inoculated subcutaneously
on the right flank)^[1]
Dosage:

15 mg/kg; 30 mg/kg; 60 mg/kg
Administration:

p.o.; QD; 21 days
Result:

Produced a tumor growth inhibition (TGI) value of 92.71%.
No noticeable body weight loss was observed in treated mice during the full treatment period.

Animal Model:

BALB/c nude mice (Female, 5 × 10⁶ SNU-16 cells were inoculated subcutaneously
on the right flank)^[1]
Dosage:

30 mg/kg
Administration:

p.o.; QD; 21 days
Result:

Produced a tumor growth inhibition (TGI) value of 49.80%.
No noticeable body weight loss was observed in treated mice during the treatment period.

Animal Model:

BALB/c nude mice (Female, 5 × 10⁶ RT112 cells were inoculated subcutaneously
on the right flank)^[1]
Dosage:

30 mg/kg
Administration:

p.o.; QD; 21 days
Result:

Produced a tumor growth inhibition (TGI) value of 67.61%.
No significant loss of body weight was observed during treatment.
Showed no abnormalities in the heart, liver, spleen, lung, and kidney tissues of treated mice via histopathological analysis.

Animal Model:

ICR mice (aged 6-8 weeks)^[1]
Dosage:

500 mg/kg; 1000 mg/kg
Administration:

p.o.; QD; 14 days
Result:

Observed no abnormalities or body weight loss in mice treated with up to 1000 mg/kg once daily for 2 weeks.

Chemical Information

Molecular Weight 737.21
Formula C₃₈H₄₀ClF₃N₆O₄
SMILES

COC1=C(C2CCN(C(C=C)=O)CC2)C=C3C(N=CC=C3OC4=CC=C(NC(NC5=CC=C(CN6CCN(C)CC6)C(C(F)(F)F)=C5)=O)C(Cl)=C4)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Hu S, et al. Optimization of covalent pan-fibroblast growth factor receptor inhibitors for treating solid tumors. European journal of medicinal chemistry. 2026 Aug 16;319:119246.

Calculators

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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.

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100 mg

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