ZM 306416

SKU: orb1307532

Description

ZM 306416 (CB 676475) is a potent small molecule inhibitor of EGFR with an IC50 below 10 nM and also targets VEGFR1 (IC50: 0.33 μM). This dual-activity compound is a valuable research tool for investigating angiogenesis and tumor growth pathways in both cellular and animal models of cancer.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 690206-97-4
• MW: 333.74
• Purity: 99.37% (May vary between batches)
• Formula: C₁₆H₁₃ClFN₃O₂
• SMILES: COc1cc2ncnc(Nc3ccc(Cl)cc3F)c2cc1OC
• Target: Src,Bcr-Abl,VEGFR
• Solubility: Ethanol:< 1 mg/mL (insoluble or slightly soluble);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.99 mM);DMSO:62 mg/mL (185.77 mM)

Bioactivity

• Target IC50:
  KDR:100 nM|VEGFR1:0.33 μM|FLT1:2 μM|EGFR:<10 nM
• In Vivo:
  When acting on human thyroid follicular cells, ZM306416 (1 μM) decreased nuclear distribution and increased follicle formation; a significant increase in cell death was observed at 3 μM.ZM306416 weakly inhibited VEGF secretion and increased PlGF production.ZM306416 (<10 μM) had a significant inhibitory effect on steady-state phosphorylation of p42/44 MAPK but had no effect on the non phosphorylated forms, but had no effect on the expression of non-phosphorylated forms. In human thyroid follicular cells, ZM306416 (300 nM) completely inhibited PAA secretion, stimulated [125I] uptake, and silenced pVEGFR2 (Y1214) expression. ZM-306416 exhibited selective antiproliferative effects (IC50: 0.09 μM and 0.072 μM) when acting on the epidermal growth factor receptor-naïve non-small cell (type) lung cancer cell lines H3255 and HCC4011. When acting on GeneBLAzer T-Rex RORγ-UAS-bla HEK293T cell line, ZM-306416 had a significant inhibitory effect on ERRα assay (IC50: 7.3 μM).ZM-306416 inhibited granule formation (IC50: 0.67 μM).

Storage & Handling

• Storage: 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

CB676475, CB-676475, CB 676475, BcrAbl, Abl, inhibit, Inhibitor, Src, ZM 306416, ZM306416, ZM-306416, VEGFR1, VEGFR, Vascular endothelial growth factor receptor

Compound Identifiers

PubChem CID

5329006