AS-605240 is a potent, cell permeable and ATP-competitive inhibitor of PI 3-kinase p110 γ (PI 3-kinase γ) (IC50 = 8 nM). AS-605240 also exhibits selectivity over other PI 3-kinase isoforms. This compound supresses the progress of joint inflammation and damage in both lymphocyte-independent and lymphocyte-dependent mouse models of rheumatoid arthritis. AS-605240 is an inhibitor of PI 3-kinase p110 α, PI 3-kinase p110 β and PI 3-kinase p110 δ.
M. Camps, et al.; Nat. Med. 11, 936 (2005). D.F. Barber, et al.; Nat. Med. 11, 933 (2005).
Soluble in DMSO (0.5 mg/ml), DMF (~0.2 mg/ml), and ethanol (<1 mg/ml at 25° C). Insoluble in water.
Store at -20° C
243.03° C (Predicted)
565.14° C (Predicted)
1.55 g/cm3 (Predicted)
n20D 1.79 (Predicted)
PI 3-kinase p110 γ : IC50 = 8 nM (human); PI 3-kinase p110 α: IC50 = 60 nM (human); C5a-mediated phosphorylation of protein kinase B: IC50 = 90 nM (RAW 264 cells); PI 3-kinase p110β: IC50 = 0.27 µM (human); PI 3-kinase p110 δ: IC50 = 0.3 µM (human)
PI 3-K γ : Ki= 7.8 nM
pKa: 7.04 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
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Rated 5 out of
Oghumu et alOghumu et al. (PubMed ID 23749323) found that AS-605240 for treatment of L. mexicana infection reduced parasitic load in mice via PI3K inhibition. -SCBT Publication Review
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