FGFR-IN-10

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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.

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

FGFR-IN-10 Chemical Structure

CAS No. : 2847092-41-3

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•Related Small Molecules:

•Related Proteins:

View All FGFR Isoform Specific Products:

View All Isoforms

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 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

Biological Activity
Purity & Documentation
References
Customer Review

Description

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.

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)	C_max (ng/mL)	AUC_last/D (h·mg/mL)	T_1/2 (h)	Cl_obs (mL/min/kg)	V_ss_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.

2847092-41-3

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

Handling Instructions (2659 KB)

References

[1]. Zhu Wei, et al. Heterocyclic compound serving as FGFR inhibitor and application thereof: World Intellectual Property Organization, WO2022206939. 2022-10-06.

FGFR-IN-10 Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

Mass		Concentration		Volume		Molecular Weight *
	=		×		×

The dilution calculator equation

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

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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