1. Protein Tyrosine Kinase/RTK
  2. FGFR
    Discoidin Domain Receptor
  3. FGFR1/DDR2 inhibitor 1

FGFR1/DDR2 inhibitor 1 

Cat. No.: HY-114311
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FGFR1/DDR2 inhibitor 1 is an orally active inhibitor of fibroblast growth factor receptor 1 (FGFR1) and discoindin domain receptor 2 (DDR2), with IC50 values of 31.1 nM and 3.2 nM, respectively. Antitumor activity.

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

FGFR1/DDR2 inhibitor 1 Chemical Structure

FGFR1/DDR2 inhibitor 1 Chemical Structure

CAS No. : 2308497-58-5

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Description

FGFR1/DDR2 inhibitor 1 is an orally active inhibitor of fibroblast growth factor receptor 1 (FGFR1) and discoindin domain receptor 2 (DDR2), with IC50 values of 31.1 nM and 3.2 nM, respectively. Antitumor activity[1].

IC50 & Target[1]

FGFR1

31.1 nM (IC50)

DDR2

3.2 nM (IC50)

In Vitro

FGFR1/DDR2 inhibitor 1 (compound 11k) (25-200 μM; 2 hours) shows significant inhibition of FGFR2 phosphorylation in a dose-dependent manner in SNU16 cells. FGFR1/DDR2 inhibitor 1 shows (60-250 μM; 2 hours) significant inhibition of DDR2 phosphorylation in a dose-dependent manner in H2286 cells[1].
FGFR1/DDR2 inhibitor 1 significantly inhibits the proliferation of FGFR-driven cancer cell lines with IC50s of 108.4, 93.4, 31.8 and 306.6 nM against KG-1, SNU-16, NCI-H716 and UMUC14 respectively. FGFR1/DDR2 inhibitor 1 demonstrates substantially activity against the DDR2-driven cancer cell line NCI-H2286 (93.0 nM)[1].

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

In Vivo

FGFR1/DDR2 inhibitor 1 (10-20 mg/kg; p.o.; once daily for 7 days) has profound anti-tumor efficacy in NCI-H1581 tumor model[1].
SCID mice bearing NCI-H2286 tumors were randomized and treated with FGFR1/DDR2 inhibitor 1 at doses of 10 mg/kg for 10 consecutive days. FGFR1/DDR2 inhibitor 1 could suppress tumor growth with tumor growth inhibition rates (TGI) of 82.8%[1].

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

Animal Model: Nude mice bearing NCI-H1581 tumors[1]
Dosage: 10 or 20 mg/kg
Administration: P.o.; once daily for 7 days
Result: Suppressed tumor growth in a dose-dependent manner with tumor growth inhibition rates (TGI) of 59.7% and 98.1% at doses of 10 and 20 mg/kg, respectively.
Molecular Weight

501.50

Formula

C₂₈H₂₂F₃N₅O

CAS No.

2308497-58-5

SMILES

O=C(NC1=CC=CC(C(F)(F)F)=C1)C2=CC=C(C)C(C3=CC4=C(C=C3)C(C5=CN(C6CC6)N=C5)=NN4)=C2

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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.

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Keywords:

FGFR1/DDR2 inhibitor 1FGFRDiscoidin Domain ReceptorFibroblast growth factor receptorphosphorylationNCI-H2286tumorSCIDmiceNudeNCI-H1581cellsInhibitorinhibitorinhibit

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FGFR1/DDR2 inhibitor 1
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HY-114311
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