2. Protein Tyrosine Kinase/RTK Metabolic Enzyme/Protease
  3. FGFR Cytochrome P450
  4. FGFR-IN-10

FGFR-IN-10 is an orally active inhibitor of FGFR and Cytochrome P450 (CYPs). FGFR-IN-10 inhibits wide type and V564F mutant FGFR2 with IC50s of 104.1 nM and 43.6 nM, respectively. FGFR-IN-10 also inhibits CYPs with IC50s of 3.33 μM (CYP2C9), 18.75 μM (CYP2C19), 4.34 μM (CYP2CD6), and 0.69 μM (CYP3A4), respectively.

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FGFR-IN-10 Chemical Structure

FGFR-IN-10 Chemical Structure

CAS No. : 2847092-41-3

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FGFR-IN-10 Related Antibodies

Top Publications Citing Use of Products

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FGFR FGFR1 FGFR2 FGFR3 FGFR4 FGF21

View All Cytochrome P450 Isoform Specific Products:

View All Isoforms
CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

FGFR-IN-10 is an orally active inhibitor of FGFR and Cytochrome P450 (CYPs). FGFR-IN-10 inhibits wide type and V564F mutant FGFR2 with IC50s of 104.1 nM and 43.6 nM, respectively. FGFR-IN-10 also inhibits CYPs with IC50s of 3.33 μM (CYP2C9), 18.75 μM (CYP2C19), 4.34 μM (CYP2CD6), and 0.69 μM (CYP3A4), respectively[1].

IC50 & Target[1]

CYP2C9

3.33 μM (IC50)

CYP2C19

18.75 μM (IC50)

CYP2D6

4.34 μM (IC50)

CYP3A4

0.69 μM (IC50)

FGFR2

104.1 nM (IC50)

V564F-FGFR2

43.6 nM (IC50)

In Vitro

FGFR-IN-10 (compound 115) (5 μM; 0-240 min) was stable in the blood of SD rats and human, and its whole blood half-life (t1/2) was >600 min[1].
FGFR-IN-10 (0-10 μM; 72 h) inhibits the growth of SNU-16 and JMSU-1 cells with GI50s of 6 nM and 24 nM, respectively[1].

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

FGFR-IN-10 Related Antibodies
In Vivo

FGFR-IN-10 (10 mg/kg; p.o.; single dose) shows potent oral activity in SD rats, with bioavailability of 60.7%[1].

Pharmacokinetic Analysis in SD Rats[1]

Route Dose (mg/kg) Cmax (ng/mL) AUClast/D (h·mg/mL) T1/2 (h) Cl_obs (mL/min/kg) Vss_obs (L/kg) F (%)
i.v. 5 / 664 1.02 26.0 1.2 /
p.o. 10 2388 402 / / / 60.7

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

543.60

Formula

C28H30FN9O2
CAS No.
SMILES

FC(C=C1C2=CN=C(N=C2N3C[C@H](N([C@@H](C3)C)C(C=C)=O)C)NC4=CN(N=C4)C)=C(C=C1)OC5=NC=CC(C)=N5
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
References
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FGFR-IN-10 Related Classifications

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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.

Keywords:

FGFR-IN-102847092-41-3FGFRCytochrome P450Fibroblast growth factor receptorCYPsInhibitorinhibitorinhibit

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