A dual inhibitor of VEGFR and FGFR (IC50s = 5-26 and 6-35 nM for VEGFR1-3 and FGFR1-4

ODM-203 – 25 mg

Brand:
Cayman
CAS:
1430723-35-5
Storage:
-20
UN-No:
Non-Hazardous - /

ODM-203 is a dual inhibitor of VEGFR and FGFR (IC50s = 5-26 and 6-35 nM for VEGFR1-3 and FGFR1-4, respectively).{59184} It is selective for VEGFR1-3 and FGFR1-4 over a panel of 308 kinases at 1 µM, but does inhibit the receptor tyrosine kinases PDGFRα, PDGFRβ, and DDR1 (IC50s = 35, 169, and 6 nM, respectively), as well as MAP4K4, MINK1, RET, SIK2, YES1, and Tie2 (IC50s = 49, 41, 8, 23, 152, and 174 nM, respectively). ODM-203 inhibits FGFR-dependent proliferation in H1581 lung, SNU-16 stomach, and RT4 bladder cancer cells (IC50s = 104, 132, and 192 nM, respectively) and VEGF-induced tube formation by human umbilical vein endothelial cells (HUVECs; IC50 = 33 nM). In vivo, ODM-203 (20 and 40 mg/kg) decreases tumor volume in an RT4 mouse xenograft model. It also reduces tumor growth and intratumor phosphorylation of FGFR in a SNU-16 mouse xenograft model when administered at a dose of 30 mg/kg.  

 

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Description

A dual inhibitor of VEGFR and FGFR (IC50s = 5-26 and 6-35 nM for VEGFR1-3 and FGFR1-4, respectively); selective for VEGFR1-3 and FGFR1-4 over a panel of 308 kinases at 1 µM; inhibits PDGFRα, PDGFRβ, and DDR1 (IC50s = 35, 169, and 6 nM, respectively), as well as MAP4K4, MINK1, RET, SIK2, YES1, and Tie2 (IC50s = 49, 41, 8, 23, 152, and 174 nM, respectively; inhibits FGFR-dependent proliferation in H1581 lung, SNU-16 stomach, and RT4 bladder cancer cells (IC50s = 104, 132, and 192 nM, respectively) and VEGF-induced tube formation by HUVECs (IC50 = 33 nM); decreases tumor volume in a RT4 mouse xenograft model at 20 and 40 mg/kg; reduces tumor growth and intratumor phosphorylation of FGFR in a SNU-16 mouse xenograft model at 30 mg/kg

Formal name: N-[2′,4′-difluoro-5-[5-(1-methyl-1H-pyrazol-4-yl)-1H-benzimidazol-1-yl][1,1′-biphenyl]-3-yl]-cyclopropanesulfonamide

Synonyms: 

Molecular weight: 505.5

CAS: 1430723-35-5

Purity: ≥98%

Formulation: A crystalline solid

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