Comparison

FGFR1/DDR2 inhibitor 1

Item no. CS-0082049-5mg
Manufacturer ChemScene
Amount 5mg
Category
Type Molecules
Specific against other
ECLASS 10.1 32169090
ECLASS 11.0 32169090
UNSPSC 12000000
Alias 2308497-58-5
Similar products 2308497-58-5
Available
CAS
2308497-58-5
Purity
>98%
MWt
501.50
Formula
C28H22F3N5O
Solubility
10 mM in DMSO
Clinical Information
No Development Reported
Pathway
Protein Tyrosine Kinase/RTK; Protein Tyrosine Kinase/RTK
Target
Discoidin Domain Receptor; FGFR
Biological Activity
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: IC50: 31.1 nM (FGFR1), 108.4 nM (KG-1), 3.2 nM (DDR2)[1]. In Vitro: FGFR1/DDR2 inhibitor 1 (compound 11k) (25-200 uM; 2 hours) shows significant inhibition of FGFR2 phosphorylation in a dose-dependent manner in SNU16 cells. FGFR1/DDR2 inhibitor 1 shows (60-250 uM; 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]. 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].
Research Area
Cancer

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Amount: 5mg
Available: In stock
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