2. Protein Tyrosine Kinase/RTK
  3. FGFR
  4. 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.

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FGFR-IN-13

FGFR-IN-13 Chemical Structure

CAS No. : 2962941-25-7

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FGFR-IN-13 Related Antibodies

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Description

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[1].

Cellular Effect
Cell Line Type Value Description References
HUVEC IC50
82.14 μM
Compound: III-30
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
[PMID: 38643670]
HepG2 IC50
7.93 μM
Compound: III-30
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
[PMID: 38643670]
MDA-MB-231 IC50
1.89 μM
Compound: III-30
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
[PMID: 38643670]
MDA-MB-435 IC50
9.17 μM
Compound: III-30
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
[PMID: 38643670]
In Vitro

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.

FGFR-IN-13 Related Antibodies

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 10 μM
Incubation Time: 9 h
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.

Cell Cycle Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 2.5 μM, 5 μM and 10 μM
Incubation Time: 24 h
Result: Induced apoptosis in a dose-dependent manner, and the percentage of induced apoptosis reached 56.8 % at 10 μM.

Cell Proliferation Assay[1]

Cell Line: MDA-MB- 435, MDA-MB-231, KYSE-150, HepG2 and HUVEC cells
Concentration:
Incubation Time: 72 h
Result: Showed better inhibitory effect on KYSE-150 cells (IC50 = 1.93 μM) compared with 2 positive controls.
In Vivo

FGFR-IN-13 (10 and 30 mg/kg, po; everyday for 21 days) inhibits tumor growth in a dose-dependent manne. FGFR-IN-13 has a favorable safety profile and is effective in inhibiting tumor growth at safe doses in MDA-MB-231 xenograft tumor mouse mode[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: MDA-MB-231 xenograft tumor mouse model[1]
Dosage: 10 and 30 mg/kg
Administration: Oral gavage (p.o.)
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).
Molecular Weight

415.44

Formula

C23H21N5O3
CAS No.
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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Purity & Documentation
References
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FGFR-IN-13 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

FGFR-IN-132962941-25-7FGFRFibroblast growth factor receptorFGFR inhibitorIrreversible covalent inhibitorAnti-tumor activityMDA-MB-231 xenograft tumor mouse modelInhibitorinhibitorinhibit

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