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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- CAS. Nr.: 2847092-41-3
- Formel: C28H30FN9O2
- Molecular Weight:543.60
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
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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) |
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.
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.
Chemical Information
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CAS. Nr. 2847092-41-3
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Molecular Weight 543.60
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Formel C28H30FN9O2
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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
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
FGFR-IN-10 Related Classifications
HY-148597 Related Classifications
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