SU14813 maleate

Research use only, not for human use.

A broad-spectrum RTKs inhibitor with IC50 ranging from 2 to 50 nM for VEGFR-1, VEGFR-2, PDGFRs, KIT, FLT3, and CSF1R/FMS.

A broad-spectrum RTKs inhibitor with IC50 ranging from 2 to 50 nM for VEGFR-1, VEGFR-2, PDGFRs, KIT, FLT3, and CSF1R/FMS; shows poor activity for EGFR and c-Met in biochemical assays; inhibits VEGFR-2, PDGFR-β, and KIT phosphorylation in porcine aorta endothelial cells with IC50 of 5.2, 9.9, and 11.2 nM respectively; active in xenograft tumor models.Breast Cancer Phase 2 Discontinued.

SU14813 inhibits ligand-dependent and ligand-independent proliferation, migration, and survival of endothelial cells and/or tumor cells expressing these targets. SU14813 inhibits cellular ligand-dependent phosphorylation of VEGFR-2 (transfected NIH 3T3 cells), PDGFR-β (transfected NIH 3T3 cells), KIT (Mo7e cells), and FLT3-internal tandem duplication (FLT3-ITD; MV4;11 cells) as well as FMS/CSF1R (transfected NIH 3T3 cells). SU14813 inhibits VEGFR-2, PDGFR-β, and KIT phosphorylation in porcine aorta endothelial cells overexpressing these targets, with cellular IC50 values of 5.2, 9.9, and 11.2 nM, respectively. SU14813 inhibits the growth of U-118MG with an IC50 of 50 to 100 nM.

SU14813 inhibits VEGFR-2, PDGFR-β, and FLT3 phosphorylation in xenograft tumors in a dose- and time-dependent fashion. The plasma concentration required for in vivo target inhibition is estimated to be 100 to 200 ng/mL. Used as monotherapy, SU14813 exhibits broad and potent antitumor activity resulting in regression, growth arrest, or substantially reduced growth of various established xenografts derived from human or rat tumor cell lines. Treatment in combination with docetaxel significantly enhances both the inhibition of primary tumor growth and the survival of the tumor-bearing mice compared with administration of either agent alone.

SU-14813 maleate | SU 14813 maleate

Angiogenesis

VEGFR

VEGFR

Cancer

Breast Cancer

849643-15-8

558.5554

C27H31FN4O8

>98% (HPLC)

10 mM in DMSO

CC1=C(NC(=C1C(=O)NCC(CN2CCOCC2)O)C)C=C3C4=C(C=CC(=C4)F)NC3=O.C(=CC(=O)O)C(=O)O

1H-Pyrrole-3-carboxamide, 5-[(Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-N-[(2S)-2-hydroxy-3-(4-morpholinyl)propyl]-2,4-dimethyl-, (2Z)-2-butenedioate (1:1)

(-20℃)

With Ice Pack

≥ 2 years