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FGFR-IN-9

FGFR-IN-9 (Compound 19) is a potent, reversible and orally active FGFR inhibitor with an IC₅₀ of 17.1, 29.6, 30.7, 46.7 and 64.3 nM against FGFR4^WT, FGFR3, FGFR4^V550L, FGFR2 and FGFR1, respectively.

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

CAS No.: 3024090-08-9
Formula: C₂₅H₂₈N₆O₃S
Molecular Weight:492.59

Storage:

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

Data Sheet (274 KB)

FGFR-IN-9 Chemical Structure

CAS No.: 3024090-08-9

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Fluorescent Dye

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

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

Biological Activity

Description

IC₅₀ & Target^[1]

FGFR4^WT

17.1 nM (IC₅₀)

FGFR3

29.6 nM (IC₅₀)

FGFR4^V550L

30.7 nM (IC₅₀)

FGFR2

46.7 nM (IC₅₀)

FGFR1

64.3 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	260 nM Compound: 19	Cytotoxicity against mouse BaF3 cells expressing TEL-fused FGFR4 V550L mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Cytotoxicity against mouse BaF3 cells expressing TEL-fused FGFR4 V550L mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 36480917]
BaF3	IC₅₀	82.5 nM Compound: 19	Cytotoxicity against mouse BaF3 cells expressing wild type TEL-fused FGFR4 assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Cytotoxicity against mouse BaF3 cells expressing wild type TEL-fused FGFR4 assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 36480917]
BaF3	IC₅₀	>2000 nM Compound: 19	Cytotoxicity against mouse BaF3 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Cytotoxicity against mouse BaF3 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 36480917]
Huh-7	IC₅₀	94.7 nM Compound: 19	Cytotoxicity against human Huh-7 cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo assay Cytotoxicity against human Huh-7 cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo assay	[PMID: 36480917]
KATO III stomach cancer cell line	IC₅₀	6 nM Compound: 19	Cytotoxicity against FGFR2-amplified human KATO III stomach cancer cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo assay Cytotoxicity against FGFR2-amplified human KATO III stomach cancer cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo assay	[PMID: 36480917]
NCI-H1581	IC₅₀	24.6 nM Compound: 19	Cytotoxicity against FGFR1-amplified human NCI-H1581 cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo assay Cytotoxicity against FGFR1-amplified human NCI-H1581 cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo assay	[PMID: 36480917]

In Vitro

FGFR-IN-9 (Compound 19) (0-2 mM; 72 h) inhibits HUH7 cells with an IC₅₀ of 94.7 ± 28.6 nM, and inhibits proliferation with IC₅₀s of 82.5 ± 19.2 nM and 260.0 ± 50.2 nM against Ba/F3 FGFR4^WT and Ba/F3 FGFR4^V550L cells, respectively^[1].
FGFR-IN-9 (0-400 nM; 4 h) inhibits FGFR signaling pathway^[1].

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

Western Blot Analysis^[1]

Cell Line:

Ba/F3-TEL-FGFR4 cells
Concentration:

0, 50, 100, 200 and 400 nM
Incubation Time:

4 h
Result:

Showed dose-dependent inhibition of the FGFR4 signal cassette, including the phosphorylation of FGFR4 and its downstream effectors FRS2 and PLCγ.

In Vivo

FGFR-IN-9 (Compound 19) (30 and 45 mg/kg; i.g.; daily for 3 weeks) shows antitumor activity in the HUH7 xenograft mouse model^[1].
In Vivo Pharmacokinetic Profile Data for FGFR-IN-9 (Compound 19) ^[1]

FGFR-IN-9	i.v. 1 mg/kg	p.o. 10 mg/kg
T_1/2 (h)	1.3	2.37
T_max (h)	/	2
C_max (ng/mL)	/	202
AUC_max (h·ng/mL)	175	965
AUC_INF (h·ng/mL)	177	1087
MRT_inf (h)	1.13	3.87
F (%)	/	61.5
V_SS (L/kg)	6.37	/
CL (L/h/kg)	5.65	/

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

Animal Model:

Female BALB/c nude mice, HUH7 xenograft model^[1]
Dosage:

30 and 45 mg/kg
Administration:

Intragastric gavage; daily for 3 weeks
Result:

Resulted in significant tumor growth inhibition with a TGI value of 81% and an IR value of 63% at a dose of 45 mg/kg. No significant body weight loss (<5%) was observed.

Animal Model:

Male CD-1 mice^[1]
Dosage:

1 mg/kg and 10 mg/kg
Administration:

i.v. and p.o. (Pharmacokinetic Analysis)
Result:

Showed good in vivo pharmacokinetic profile.

Chemical Information

CAS No. 3024090-08-9
Molecular Weight 492.59
Formula C₂₅H₂₈N₆O₃S
SMILES

O=S(N1C=CC2=CN=C(NC3=CC=C(N4C[C@H](C)N[C@H](C)C4)C=C3)N=C21)(C5=CC=CC(OC)=C5)=O
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 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)

References

[1]. Xie W, et al. Discovery of 2-Amino-7-sulfonyl-7 H-pyrrolo [2, 3-d] pyrimidine Derivatives as Potent Reversible FGFR Inhibitors with Gatekeeper Mutation Tolerance: Design, Synthesis, and Biological Evaluation. Journal of Medicinal Chemistry, 2022.

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.

Keywords

100 mg

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