FGFR2-IN-4
FGFR2-IN-4 is a selective, orally active FGFR2 inhibitor, with IC50 values of 10.0 nM and 5.8 nM against wild-type FGFR2 and the FGFR2V565F mutant, respectively. FGFR2-IN-4 induces necroptosis in FGFR2-driven tumor cells. FGFR2-IN-4 induces tumor regression in xenograft models harboring FGFR2 inhibitor-resistant mutations without altering serum phosphate levels. FGFR2-IN-4 is used to investigate FGFR2-driven malignancies, including intrahepatic cholangiocarcinoma and gastric cancer.
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- CAS No.: 3110002-64-4
- Formule: C25H20N8O
- Masse moléculaire:448.48
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
FGFR2 10.0 nM (IC50) |
FGFR2V565F 5.8 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| KATO III stomach cancer cell line | IC50 |
9.0 nM
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Antiproliferative effect against FGFR2-amplified KATOIII human gastric cancer cells.
Antiproliferative effect against FGFR2-amplified KATOIII human gastric cancer cells.
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42675086 |
| BaF3 | IC50 |
37.6 nM
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Antiproliferative activity against FGFR2 N550K mutant-expressing Ba/F3 cells incubated for 3 days assessed by CellTiter-Glo luminescence assay.
Antiproliferative activity against FGFR2 N550K mutant-expressing Ba/F3 cells incubated for 3 days assessed by CellTiter-Glo luminescence assay.
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42675086 |
In Vitro
FGFR2-IN-4 (3 days) displays strong cellular isoform selectivity for FGFR2 over FGFR1, FGFR3, and FGFR4 in engineered Ba/F3 proliferation assays, with an IC50 of 4.0 nM against FGFR2-driven cell growth[1].
FGFR2-IN-4 engages FGFR2 in KATOIII cells via stable, irreversible covalent binding, as demonstrated by persistent suppression of FGFR2 downstream signaling even after the unbound compound is completely washed out[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Ba/F3 cells expressing FGFR1, FGFR2, FGFR3, or FGFR4
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Concentration:9-point threefold serial dilutions
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Incubation Time:3 days
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Result:Inhibits the proliferation of FGFR2-expressing Ba/F3 cells with an IC50 of 4.0 nM.
Results in 44-fold reduced sensitivity in FGFR1-expressing cell line with an IC50 of 175.9 nM.
Results in 23-fold reduced sensitivity in FGFR3-expressing cell line with an IC50 of 93.4 nM.
Shows no detectable anti-proliferative activity in FGFR4-expressing Ba/F3 cells.
In Vivo
FGFR2-IN-4 (10 mg/kg; p.o.; once daily for 11 consecutive days) exhibits potent antitumor activity in the FGFR2M538I xenograft mouse model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c mice (female, 6 weeks old)[1]
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Dosage:10 mg/kg
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Administration:p.o.; daily; 14 days
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Result:Produced 87% tumor growth inhibition.
Maintained stable body weight throughout the 14-day period.
Kept serum phosphate levels within the normal physiological range.
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Animal Model:BALB/c mice (female, 6 weeks old)[1]
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Dosage:10 mg/kg
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Administration:p.o.; daily; 11 days
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Result:Exerted pronounced antitumor activity against FGFR2 M538I mutant tumors.
Achieved significant reduction in tumor weight relative to vehicle-treated animals.
Chemical Information
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CAS No. 3110002-64-4
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Masse moléculaire 448.48
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Formule C25H20N8O
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SMILES
C=CC(NC1=CC=C(C2=C(C#CC3=CN=C(N(C)C=N4)C4=C3)C5=C(N)N=CN=C5N2C)C=C1)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
FGFR2-IN-4 Related Classifications
HY-189204 Related Classifications
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