2. Protein Tyrosine Kinase/RTK
  3. FGFR
  4. FGFR-IN-11

FGFR-IN-11 (compound I-5) is an orally active and covalent FGFR inhibitor with IC50 values of 9.9 nM (FGFR1), 3.1 nM (FGFR2), 16 nM (FGFR3), and 1.8 nM (FGFR4), respectively. FGFR-IN-11 inhibits multiple cancer cell proliferation with nanomolar activity. FGFR-IN-11 inhibits tumor growth significantly in xenograft mice models.

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FGFR-IN-11 Chemical Structure

FGFR-IN-11 Chemical Structure

CAS No. : 2658488-68-5

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FGFR-IN-11 Related Antibodies

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Description

FGFR-IN-11 (compound I-5) is an orally active and covalent FGFR inhibitor with IC50 values of 9.9 nM (FGFR1), 3.1 nM (FGFR2), 16 nM (FGFR3), and 1.8 nM (FGFR4), respectively. FGFR-IN-11 inhibits multiple cancer cell proliferation with nanomolar activity. FGFR-IN-11 inhibits tumor growth significantly in xenograft mice models[1].

IC50 & Target[1]

FGFR1

9.9 nM (IC50)

FGFR2

3.1 nM (IC50)

FGFR3

16 nM (IC50)

FGFR4

1.8 nM (IC50)

In Vitro

FGFR-IN-11 (0.3 nM-20 μM, 72 h) inhibits multiple cancer cell growth with nanomolar activity[1].

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

FGFR-IN-11 Related Antibodies

Cell Viability Assay[1]

Cell Line: NCI-H1581, SNU16, Huh-7, Hep3B
Concentration: 0.3 nM-20 μM
Incubation Time: 72 h
Result: Inhibited cell growth with IC50 values of less than 2 nM (NCI-H1581 and SNU16), 15.63 nM (Huh-7) and 52.6 nM (Hep3B).
In Vivo

FGFR-IN-11 (60 mg/kg, p.o., QD for 21 days) inhibits tumor growth significantly and without effect on body weight in the Huh-7 or NCI-H1581 xenograft model in female nude mice[1].
Pharmacokinetic Study of compound I-5[1]

compound I-5 的药代动力学分析[1]

parameters (unit) C0 (ng/mL) Cmax (ng/mL) T1/2 (h) Tmax (h) AUC(0-t) (h•ng/mL) AUC(0-∞) (h•ng/mL) MRT(0-t) (h) MRT(0-∞) (h) CI (mL/kg/min) Vss (mL/kg) F (%)
iv (2 mg/kg) 3295 1836 0.26 0.08 570 572 0.18 0.19 58 1319 /
po (10 mg/kg) / 1802 2.48 0.25 1731 1966 1.99 3.16 / / 60.69

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

Animal Model: Huh-7 xenograft model in female nude mice[1]
Dosage: 15, 30, 60 mg/kg
Administration: Oral administration (p.o.)
Result: Inhibited tumor growth of 88.2% at the dose of 60 mg/kg and had no significant changes in body weight.
Animal Model: NCI-H1581 xenograft model in female nude mice[1]
Dosage: 60 mg/kg
Administration: Oral administration (p.o.)
Result: Inhibited tumor growth of 67% and had no significant changes in body weight.
Molecular Weight

521.01

Formula

C28H29ClN4O4
CAS No.
SMILES

O=C(N1CCC(CC1)C2=CC3=C(OC4=CC=C(C(Cl)=C4)NC(NC5CC5)=O)C=CN=C3C=C2OC)C=C
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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-11 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-112658488-68-5FGFRFibroblast growth factor receptorNCI-H1581SNU16Huh-7Hep3Borally activitycovalentxenograft mice modelsanticancerInhibitorinhibitorinhibit

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