1. Protein Tyrosine Kinase/RTK
  2. FGFR
  3. 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 FGFR4WT, FGFR3, FGFR4V550L, FGFR2 and FGFR1, respectively.

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FGFR-IN-9 Chemical Structure

FGFR-IN-9 Chemical Structure

CAS No. : 3024090-08-9

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Description

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 FGFR4WT, FGFR3, FGFR4V550L, FGFR2 and FGFR1, respectively[1].

IC50 & Target[1]

FGFR4WT

17.1 nM (IC50)

FGFR3

29.6 nM (IC50)

FGFR4V550L

30.7 nM (IC50)

FGFR2

46.7 nM (IC50)

FGFR1

64.3 nM (IC50)

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 FGFR4WT and Ba/F3 FGFR4V550L 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
T1/2 (h) 1.3 2.37
Tmax (h) / 2
Cmax (ng/mL) / 202
AUCmax (h·ng/mL) 175 965
AUCINF (h·ng/mL) 177 1087
MRTinf (h) 1.13 3.87
F (%) / 61.5
VSS (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.
Molecular Weight

492.59

Formula

C25H28N6O3S

CAS No.
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

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Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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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.

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FGFR-IN-9
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HY-152104
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