AC710 |
| رقم الكتالوجGC18167 |
AC710 هو مثبط PDGFR قوي بـ Kds 0.6 ، 1.57 ، 1 ، 1.3 ، 1.0 نانومتر لـ FLT3 ، CSF1R ، KIT ، PDGFRα و PDGFRβ ، على التوالي
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1351522-04-7
Sample solution is provided at 25 µL, 10mM.
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AC710 is a potent, orally active, and selective platelet-derived growth factor receptor-family kinase inhibitor with potential anticancer activity. Its 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.. AC710 causes tumor regression of leukemia cell xenografts in mice. AC710 also reduces joint swelling and inflammation in a mouse model of collagen-induced arthritis. AC710 is now a preclinical development candidate.
REFERENCES:
Liu *†, Brian T. Campbell †, Mark W. Holladay †, Julia M. Ford Pulido ‡, Helen Hua ‡, Dana Gitnick , Michael F. Gardner , Joyce James , Mike A. Breider , Daniel Brigham ‡, Barbara Belli ‡, Robert C. Armstrong ‡, and Daniel K. Treiber. Discovery of AC710, a Globally Selective Inhibitor of Platelet-Derived Growth Factor Receptor-Family Kinases. ACS Med. Chem. Lett., 2012, 3 (12), pp 997–1002
Average Rating: 5 (Based on Reviews and 4 reference(s) in Google Scholar.)
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