2. Protein Tyrosine Kinase/RTK
  3. FGFR
  4. FGFR2/3-IN-1

FGFR2/3-IN-1 is a potent and selective FGFR2 and FGFR3 (FGFR) inhibitor with IC50s of 1 nM and 0.5 nM, respectively. FGFR2/3-IN-1 displays >40-fold selectivity over FGFR1/FGFR4 and other kinome. FGFR2/3-IN-1 also inhibits FGFR3 V555L and V555M mutants with IC50s of 2.7 nM and 6.1 nM, respectively.

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FGFR2/3-IN-1

FGFR2/3-IN-1 Chemical Structure

CAS No. : 2640352-86-7

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FGFR2/3-IN-1 Related Antibodies

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Description

FGFR2/3-IN-1 is a potent and selective FGFR2 and FGFR3 (FGFR) inhibitor with IC50s of 1 nM and 0.5 nM, respectively. FGFR2/3-IN-1 displays >40-fold selectivity over FGFR1/FGFR4 and other kinome. FGFR2/3-IN-1 also inhibits FGFR3 V555L and V555M mutants with IC50s of 2.7 nM and 6.1 nM, respectively[1].

Application

1. This compound can be used as a tracer.
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.

IC50 & Target[1]

FGFR2

1 nM (IC50)

FGFR3

0.5 nM (IC50)

FGFR3 V555L

2.7 nM (IC50)

FGFR3 V555M

6.1 nM (IC50)

FGFR1

21 nM (IC50)

FGFR4

145 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
Sf9 IC50
0.5 nM
Compound: 29
Inhibition of N-terminal His-Avi tagged recombinant human FGFR3 (447 to 761 residues) expressed in an Sf9 infected baculovirus expression system using biotin-EQEDEPEGDYFEWLE-amide as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 1 hr by HTRF assay
Inhibition of N-terminal His-Avi tagged recombinant human FGFR3 (447 to 761 residues) expressed in an Sf9 infected baculovirus expression system using biotin-EQEDEPEGDYFEWLE-amide as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 1 hr by HTRF assay
[PMID: 36356320]
Sf9 IC50
1 nM
Compound: 29
Inhibition of N-terminal GST tagged recombinant human FGFR2 (400 to 821 residues) expressed in an Sf9 infected baculovirus expression system using biotin-EQEDEPEGDYFEWLE-amide as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 1 hr by HTRF assay
Inhibition of N-terminal GST tagged recombinant human FGFR2 (400 to 821 residues) expressed in an Sf9 infected baculovirus expression system using biotin-EQEDEPEGDYFEWLE-amide as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 1 hr by HTRF assay
[PMID: 36356320]
In Vitro

FGFR2/3-IN-1 (compound 29) has a clean CYP profile (CYP3A4 IC50 >25 μM). FGFR2/3-IN-1 displays excellent potency (whole blood, IC50 = 177 nM) in a whole blood (WB) assay[1].

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

FGFR2/3-IN-1 Related Antibodies
In Vivo

FGFR2/3-IN-1 (compound 29) is advanced into rat pharmacokinetics studies. Clearance in the i.v. arm is low (hepatic blood flow (HBF) = 35%), with a moderate half-life (t1/2 = 1.7 h). In the p.o. dose, FGFR2/3-IN-1 demonstrates good exposure (AUC = 5108 nM·h) and high oral bioavailability (F% = 82)[2].

rat i.v. rat p.o.
dose (mg/kg) 1.0 dose (mg/kg) 3.0
HBF% 35 Cmax (nM) 2303
Vdss (L/kg) 1.6 AUC (nM·h) 5108
T1/2 (h) 1.7 F% 82

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

450.51

Formula

C23H22D3N7O3
CAS No.
SMILES

[2H]C([2H])(NC(C1=CC(C2=C3N=C(C(C4=CN(N=C4)C(C)C)=CN3N=C2)O[C@@H]5COCC5)=CN=C1)=O)[2H]
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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FGFR2/3-IN-1 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:

FGFR2/3-IN-12640352-86-7FGFRFibroblast growth factor receptorFGFR2FGFR3FGFR3 V555LFGFR3 V555Moral bioavailabilityInhibitorinhibitorinhibit

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