FGFR-IN-28
FGFR-IN-28 is a FGFR inhibitor with inhibitory activity against multiple subtypes of the FGFR family, with an IC50 of 4.4 nM against FGFR4. FGFR-IN-28 inhibits kinase activity and phosphorylation processes, and blocks the downstream MAPK and AKT signaling pathways. FGFR-IN-28 induces cellular DNA damage, cell cycle arrest, apoptosis and ferroptosis, and reduces the adhesion, invasion and metastasis abilities of cancer cells. FGFR-IN-28 exhibits anti-tumor activity in in vitro experiments on colon cancer cells, and inhibits tumor growth in colon cancer xenograft models. FGFR-IN-28 can be used in colon cancer-related research.
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- CAS No.: 2634677-16-8
- Formule: C24H19Cl3N4O4
- Masse moléculaire:533.79
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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
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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FGFR1 10 nM (IC50) |
FGFR2 21 nM (IC50) |
FGFR3 50 nM (IC50) |
FGFR4 4.4 nM (IC50) |
Akt |
p38 MAPK |
Bax |
Bcl-2 |
PARP |
FGFR-IN-28 (F1-7) dose-dependently inhibits the kinase activity of recombinant FGFR1, FGFR2, FGFR3, and FGFR4 proteins with IC50 values of 10, 21, 50, and 4.4 nmol/L, respectively[1].
FGFR-IN-28 (48 h) dose-dependently reduces the viability of HCT-116, RKO, and SW620 human colon cancer cells with IC50 values of 1.271 μM, 2.046 μM, and 1.433 μM[1].
FGFR-IN-28 (1.0-4.0 μM; 24 h) dose-dependently inhibits the phosphorylation of FGFR, AKT, and MAPK in HCT-116, RKO, and SW620 human colon cancer cells following 12 h of treatment, without altering total FGFR protein levels[1].
FGFR-IN-28 (2.0 μM; 12 h) alters the transcriptome of HCT-116 human colon cancer cells, significantly enriching genes in the MAPK signaling, apoptosis, and ferroptosis pathways[1].
FGFR-IN-28 (1.0-4.0 μM; 24 h) dose-dependently inhibits colony formation in HCT-116, RKO, and SW620 human colon cancer cells[1].
FGFR-IN-28 (1.0-4.0 μM; 48 h) dose-dependently induces apoptosis in HCT-116, RKO, and SW620 human colon cancer cells[1].
FGFR-IN-28 (1.0-4.0 μM; 24 h) dose-dependently modulates apoptosis-related protein expression in HCT-116, RKO, and SW620 human colon cancer cellst, increasing cleaved-PARP and Bax while decreasing Bcl-2[1].
FGFR-IN-28 (4.0 μM) induces cell death in HCT-116 human colon cancer cells via both apoptosis and ferroptosis after 48 h of treatment, as shown by reduced cell death when co-treated with Z-VAD (HY-164388) or ferrostatin-1 (HY-100579), respectively[1].
FGFR-IN-28 (1.0-4.0 μM; 24 h) dose-dependently increases expression of the DNA damage biomarker γ-H2AX in HCT-116 and RKO human colon cancer cells after 24 h of treatment[1].
FGFR-IN-28 (1.0-4.0 μM; 24 h) dose-dependently induces DNA fragmentation, measured via increased comet tail formation, in HCT-116, RKO, and SW620 human colon cancer cells after 24 h of treatment[1].
FGFR-IN-28 (2.0-4.0 μM; 24 h) dose-dependently reduces DNA synthesis and cell proliferation in HCT-116 human colon cancer cells, as measured by decreased EdU incorporation following 24 h of treatment[1].
FGFR-IN-28 (1.0-4.0 μM; 24 h) dose-dependently induces G2/M cell cycle arrest in HCT-116, RKO, and SW620 human colon cancer cells after 24 h of treatment, accompanied by reduced expression of CyclinB1, MDM2, and CDK1[1].
FGFR-IN-28 (1.0-4.0 μM; pretreatment duration not specified; 1 h adhesion incubation) dose-dependently inhibits the adhesion ability of HCT-116, RKO, and SW620 human colon cancer cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human colon cancer cell lines HCT-116, RKO, SW620
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Concentration:1, 2, 4 μM
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Incubation Time:24 h
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Result:Inhibited FGFR phosphorylation in a dose-dependent manner, while total FGFR protein levels remained unchanged.
Reduced phosphorylation levels of downstream signaling proteins AKT and MAPK.
Increased expression of apoptotic markers cleaved-PARP and Bax.
Decreased expression of anti-apoptotic protein Bcl-2.
Increased expression of the DNA damage biomarker γ-H2AX in a dose-dependent manner in both HCT-116 and RKO cells.
Decreased expression of G2/M phase-associated proteins CyclinB1, MDM2, and CDK1 in a dose-dependent manner in HCT-116 and RKO cells.
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Cell Line:human colon cancer cell lines HCT-116, RKO, SW620
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Concentration:1, 2, 4 μM
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Incubation Time:24 h (initial treatment, followed by 7 days of culture in fresh medium)
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Result:Reduced colony formation of HCT-116, RKO, and SW620 cells in a dose-dependent manner.
Showed greater efficacy than the positive control AZD4547 (HY-13330) at 4 μM.
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Cell Line:human colon cancer cell lines HCT-116, RKO, SW620
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Concentration:1, 2, 4 μM
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Incubation Time:48 h
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Result:Increased the proportion of apoptotic cells in HCT-116, RKO, and SW620 cell lines.
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Cell Line:human colon cancer cell line HCT-116
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Concentration:1, 2, 4 μM
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Incubation Time:24 h
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Result:Reduced the number of EdU-positive cells in a dose-dependent manner, indicating decreased DNA synthesis and cell proliferation.
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Cell Line:human colon cancer cell lines HCT-116, RKO, SW620
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Concentration:1, 2, 4 μM
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Incubation Time:24 h
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Result:Increased the proportion of cells arrested in the G2/M phase.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (nu/nu) (female, 4-6 weeks old)[1]
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Dosage:20 mg/kg; 40 mg/kg
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Administration:i.p.; daily; 14 days
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Result:Reduced tumour volume relative to vehicle control. Slowed tumour growth at 20 mg/kg and nearly arrested tumour growth at 40 mg/kg, with markedly decreased tumour weight across treatment groups.
Inhibited FGFR and MAPK phosphorylation in tumour tissue in a dose-dependent manner.
Modulated the expression of apoptosis-related proteins, induced DNA damage, suppressed cell proliferation and facilitated tumour cell apoptosis.
Chemical Information
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CAS No. 2634677-16-8
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Masse moléculaire 533.79
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Formule C24H19Cl3N4O4
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SMILES
O=C(C1=CC(NC(CCl)=O)=CC=C1)NC2=NNC3=C2C=CC(C4=C(Cl)C(OC)=CC(OC)=C4Cl)=C3
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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)
FGFR-IN-28 Related Classifications
HY-184250 Related Classifications
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