SU14813

SKU: orb1299361

Description

SU14813 is a potent multi-targeted tyrosine kinase inhibitor with antiangiogenic and antitumor properties, exhibiting IC50 values in the low nanomolar range against VEGFR1, VEGFR2, PDGFRβ, and KIT. It has demonstrated efficacy in both in vitro assays and in vivo tumor models, making it a valuable research tool for studying angiogenesis and oncology.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 627908-92-3
• MW: 442.48
• Purity: 99.72% (May vary between batches)
• Formula: C₂₃H₂₇FN₄O₄
• SMILES: Cc1[nH]c(\C=C2/C(=O)Nc3ccc(F)cc23)c(C)c1C(=O)NCC(O)CN1CCOCC1
• Target: VEGFR,PDGFR,c-Kit
• Solubility: DMSO:44 mg/mL (99.44 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.52 mM)

Bioactivity

• Target IC50:
  VEGFR2:50 nM |VEGFR1:2 nM |PDGFRβ:4 nM |c-Kit:15 nM
• In Vivo:
  The plasma concentration required for in vivo target inhibition was estimated to be 100 to 200 ng/mL. Used as monotherapy, SU14813 exhibited 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 enhanced both the inhibition of primary tumor growth and the survival of the tumor-bearing mice compared with administration of either agent alone.
• In Vitro:
  SU14813, a small molecule identified from the same chemical library used to isolate sunitinib, has broad-spectrum RTK inhibitory activity through binding to and inhibition of VEGFR, PDGFR, KIT, and FLT3. In cellular assays, SU14813 inhibited ligand-dependent and ligand-independent proliferation, migration, and survival of endothelial cells and/or tumor cells expressing these targets. SU14813 inhibited VEGFR-2, PDGFR-beta, and FLT3 phosphorylation in xenograft tumors in a dose- and time-dependent fashion.

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Kit, Inhibitor, inhibit, c-Kit, cKit, CD117, Vascular endothelial growth factor receptor, VEGFR, Platelet-derived growth factor receptor, PDGFR, SCFR, SU14813, SU-14813, SU 14813

Compound Identifiers

PubChem CID

10138260