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 Chemical Structure

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].

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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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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