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.
For research use only. We do not sell to patients.
- CAS No.: 2640352-86-7
- Formula: C23H22D3N7O3
- Molecular Weight:450.51
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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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) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Sf9 | IC50 |
0.5 nM
Compound: 29
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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 a
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 a
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[PMID: 36356320] |
| Sf9 | IC50 |
1 nM
Compound: 29
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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 m
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 m
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[PMID: 36356320] |
| 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.
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.
Chemical Information
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CAS No. 2640352-86-7
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Molecular Weight 450.51
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Formula C23H22D3N7O3
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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]
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
FGFR2/3-IN-1 Related Classifications
HY-151903S Related Classifications
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