FGFR1/DDR2 inhibitor 1

SKU: orb1218368

Description

FGFR1/DDR2 inhibitor 1 is an inhibitor of discoindin domain receptor 2 (DDR2) and fibroblast growth factor receptor 1 (FGFR1), with IC50 values of 31.1 nM, 108.4 nM and 3.2 nM for FGFR1, KG-1, and DDR2, respectively.

Research Area

Musculoskeletal & Connective Tissue Research; Pharmacology & Drug Discovery

Key Properties

• CAS Number: 2308497-58-5
• MW: 501.5
• Purity: >98% (HPLC)
• Formula: C₂₈H₂₂F₃N₅O
• SMILES: CC1=C(C=C(C=C1)C(=O)NC2=CC=CC(=C2)C(F)(F)F)C3=CC4=C(C=C3)C(=NN4)C5=CN(N=C5)C6CC6
• Target: FGFR
• Solubility: DMSO:250 mg/mL (498.50 mM; Need ultrasonic);H2O:< 0.1 mg/mL (insoluble)

Bioactivity

• 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. 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%. Animal model: Nude mice bearing NCI-H1581 tumors. 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.
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• 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. 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).
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

FGFR