FGFR-IN-13
FGFR-IN-13 (compound III-30) is an irreversible covalent fibroblast growth factor receptor (FGFR) inhibitor. FGFR-IN-13 regulates endogenous FGFR1(IC50=0.20±0.02 nM) and FGFR4(IC50=0.40±0.03 nM) mediated signaling pathways by inhibiting the expression of key proteins. FGFR-IN-13 inhibits total-PARP and Bcl-2 protein expressions, and promote Cleaved-PARP and Bax protein expressions in a dose-dependent manner. FGFR-IN-13 has significant antitumor activity and oral activity.
For research use only. We do not sell to patients.
- CAS No.: 2962941-25-7
- Formula: C23H21N5O3
- Molecular Weight:415.44
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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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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | IC50 |
7.93 μM
Compound: III-30
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Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
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[PMID: 38643670] |
| HUVEC | IC50 |
82.14 μM
Compound: III-30
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Cytotoxicity against HUVEC cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Cytotoxicity against HUVEC cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
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[PMID: 38643670] |
| MDA-MB-231 | IC50 |
1.89 μM
Compound: III-30
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Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
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[PMID: 38643670] |
| MDA-MB-435 | IC50 |
9.17 μM
Compound: III-30
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Antiproliferative activity against human MDA-MB-435 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-435 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
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[PMID: 38643670] |
FGFR-IN-13 (10 μM, 9 h) can achieve covalent irreversibly binding with FGFR protein. FGFR-IN-13 inhibits p-FGFR protein expression can reach the level of AZD4547 (HY-13330) and TAS-120 (HY-100818) in MDA-MB-231 cells[1].
FGFR-IN-13 (2.5, 5, 10 μM, 24 h) has better apoptosis-inducing ability than AZD4547 (45.4 % versus 37.3 %) at the same concentration (5 μM) and has a similar mechanism of action to AZD4547, but MDAMB-231 cells are much sensitive to III-30[1].
FGFR-IN-13 (1.25, 2.5, 5 μM, 12 h) inhibits the migration of triple-negative breast cancer cells compatible to AZD4547 at the same concentration[1].
FGFR-IN-13 (2.5, 5, 10 μM, 12 h) is capable of inducing cell apoptosis by generating excess ROS and decreasing MMP[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231 cells
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Concentration:10 μM
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Incubation Time:9 h
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Result:Inhibited the autophosphorylation of FGFR protein for a long period of time, and the expression level of p-FGFR protein in cancer cells is still suppressed even after 8 h of discontinuation.
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Cell Line:MDA-MB-231 cells
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Concentration:2.5 μM, 5 μM and 10 μM
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Incubation Time:24 h
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Result:Induced apoptosis in a dose-dependent manner, and the percentage of induced apoptosis reached 56.8 % at 10 μM.
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Cell Line:MDA-MB- 435, MDA-MB-231, KYSE-150, HepG2 and HUVEC cells
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Concentration:
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Incubation Time:72 h
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Result:Showed better inhibitory effect on KYSE-150 cells (IC50 = 1.93 μM) compared with 2 positive controls.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MDA-MB-231 xenograft tumor mouse model[1]
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Dosage:10 and 30 mg/kg
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Administration:Oral gavage (p.o.)
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Result:Did not cause significant weight loss.
Achieved tumor growth inhibition (TGI) of 64.21% at high doses (30 mg/kg).
Achieved tumor growth inhibition (TGI) of 40.22% at low doses (10 mg/kg).
Chemical Information
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CAS No. 2962941-25-7
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Molecular Weight 415.44
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Formula C23H21N5O3
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SMILES
C=CC(NC1=CC=C(CN2C=NC3=C(C4=CC(OC)=CC(OC)=C4)N=CN=C23)C=C1)=O
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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)
FGFR-IN-13 Related Classifications
HY-163527 Related Classifications
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