2. Protein Tyrosine Kinase/RTK PI3K/Akt/mTOR Cell Cycle/DNA Damage Apoptosis NF-κB Metabolic Enzyme/Protease Immunology/Inflammation
  3. FGFR Akt PERK Apoptosis Ferroptosis Reactive Oxygen Species (ROS)
  4. FGFR-IN-27

FGFR-IN-27 is an orally active, broad-spectrum FGFR inhibitor, with an IC50 of 0.24 nM against human FGFR1, 0.71 nM against FGFR2, 0.87 nM against FGFR3, and 6.50 nM against FGFR4. FGFR-IN-27 inhibits cancer cell proliferation and blocks tumor growth. FGFR-IN-27 reduces the phosphorylation levels of AKT and ERK, induces apoptosis and ferroptosis, increases ROS levels, and decreases GSH levels. FGFR-IN-27 can be used in the research of hepatocellular carcinoma.

For research use only. We do not sell to patients.

FGFR-IN-27

FGFR-IN-27 Chemical Structure

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FGFR-IN-27 Related Antibodies

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Description

FGFR-IN-27 is an orally active, broad-spectrum FGFR inhibitor, with an IC50 of 0.24 nM against human FGFR1, 0.71 nM against FGFR2, 0.87 nM against FGFR3, and 6.50 nM against FGFR4. FGFR-IN-27 inhibits cancer cell proliferation and blocks tumor growth. FGFR-IN-27 reduces the phosphorylation levels of AKT and ERK, induces apoptosis and ferroptosis, increases ROS levels, and decreases GSH levels. FGFR-IN-27 can be used in the research of hepatocellular carcinoma[1].

IC50 & Target[1]

FGFR1

0.24 nM (IC50)

FGFR2

0.71 nM (IC50)

FGFR3

0.87 nM (IC50)

FGFR4

6.5 nM (IC50)

In Vitro

FGFR-IN-27 (Compound 1a) (0.1 nM-10000 nM; 3 days) inhibits the proliferation of human Huh7, MHCC97-H, HepG2, MCF7 and MDA-MB-231 cells, with IC50 values of 11.0 nM, 91.2 nM, 485 nM, 4430 nM and 3380 nM, respectively[1].
FGFR-IN-2 inhibits migration and proliferation of human Huh7 hepatocellular carcinoma cells[1].
FGFR-IN-27 (0.01-10 μM) inhibits the downstream signaling pathway of FGFR in human Huh7 hepatocellular carcinoma cells by dose-dependently reducing the phosphorylation levels of AKT and ERK[1].
FGFR-IN-27 (10-100 nM; 24 h) induces apoptosis in human Huh7 hepatocellular carcinoma cells[1].
FGFR-IN-27 (0.1 μM) induces ferroptosis in human Huh7 hepatocellular carcinoma cells, increases ROS levels, and decreases glutathione (GSH) levels[1].

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

FGFR-IN-27 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: human hepatocellular carcinoma Huh7, MHCC97-H, HepG2 cells; human breast cancer MCF7, MDA-MB-231 cells
Concentration: 0.1, 1, 10, 100, 1000, 10000 nM
Incubation Time: 3 days
Result: Inhibited proliferation of Huh7 cells with an IC50 of 11.0 nM.
Inhibited proliferation of MHCC97-H cells with an IC50 of 91.2 nM.
Inhibited proliferation of HepG2 cells with an IC50 of 485 nM.
Inhibited proliferation of MCF7 cells with an IC50 of 4430 nM.
Inhibited proliferation of MDA-MB-231 cells with an IC50 of 3380 nM.

Apoptosis Analysis[1]

Cell Line: human hepatocellular carcinoma Huh7 cells
Concentration: 10, 50, 100 nM
Incubation Time: 24 h
Result: Induced apoptosis in Huh7 cells significantly at 10 nM.
Induced apoptosis in Huh7 cells significantly at 50 nM.
Induced apoptosis in Huh7 cells significantly at 100 nM.
Increased apoptosis rates of Huh7 cells with higher concentrations.
Parmacokinetics
Species Dose Route T1/2 Cmax AUC0-24 MRT Bioavailability Tmax
Mice[1] 2 mg/kg i.v. 1.20 h 8540 ng/mL 2501 ng·h/mL 0.63 h 66.9 % /
Mice[1] 5 mg/kg p.o. 0.995 h 4694 ng/mL 4156 ng·h/mL 1.08 h 66.9 % 0.25 h
In Vivo

FGFR-IN-27 (10-50 mg/kg; p.o.; once daily; for 15 consecutive days) achieves tumor growth inhibition rates of 54.5% and 90.5%, respectively, in BALB/c nude mice bearing Huh7 hepatocellular carcinoma xenografts, with no systemic toxicity observed[1].

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

Animal Model: BALB/c nude (female, 8 weeks old)[1]
Dosage: 10 mg/kg; 50 mg/kg
Administration: p.o.; daily; 15 days
Result: Achieved a 54.5% tumor growth inhibition (TGI) rate.
Achieved a 90.5% TGI rate, nearly completely suppressing tumor growth.
Caused no significant mouse weight loss throughout the study.
Showed no significant toxicity in major organs (lung, liver, spleen, kidney, heart) via hematoxylin and eosin (HE) staining at therapeutic doses.
Molecular Weight

571.50

Formula

C28H32Cl2N6O3
SMILES

CCN1CCN(CC1)C2=CC=C(C=C2)NC3=CC4=C(CN(C(N4C)=O)C5=C(C(OC)=CC(OC)=C5Cl)Cl)C=N3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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FGFR-IN-27 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-27FGFRAktPERKApoptosisFerroptosisReactive Oxygen Species (ROS)Fibroblast growth factor receptorPKBProtein kinase BProtein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinaseHepG2MHCC97-Hhepatocellular carcinomaFGFR4FGFR3FGFR1Huh7MCF7FGFR2MDA-MB-231Inhibitorinhibitorinhibit

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