Potent PDGFR family inhibitor (IC50 values are 1.2, 2, 7.7 and 10.5 nM for KIT, FLT3, PDGFRβ and CSF1R respectively; Kd = 1.3 nM for PDGFRα). Exhibits >30-fold selectivity over a panel of other kinases and exhibits no activity against cytochrome P450. Causes tumor regression of leukemia cell xenografts in mice. Also reduces joint swelling and inflammation in a mouse model of collagen-induced arthritis. Orally active.
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 562.7. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.78 mL||8.89 mL||17.77 mL|
|5 mM||0.36 mL||1.78 mL||3.55 mL|
|10 mM||0.18 mL||0.89 mL||1.78 mL|
|50 mM||0.04 mL||0.18 mL||0.36 mL|
References are publications that support the products' biological activity.
Liu et al (2012) Discovery of AC710, a globally selective inhibitor of platelet-derived growth factor receptor-family kinases. ACS Med.Chem.Lett. 3 997 PMID: 24900421
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