AS-605240An inhibitor of PI 3-kinase γ

AS-605240 (CAS 648450-29-7)

AS-605240 | CAS 648450-29-7 is rated 5.0 out of 5 by 1.
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Synonym: 5-(6-Quinoxalinylmethylene)-2,4-thiazolidine-2,4-dione
Application: An inhibitor of PI 3-kinase γ
CAS Number: 648450-29-7
Purity: ≥95%
Molecular Weight: 257.27
Molecular Formula: C12H7N3O2S
* Refer to Certificate of Analysis for lot specific data (including water content).

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.


References

M. Camps, et al.; Nat. Med. 11, 936 (2005). D.F. Barber, et al.; Nat. Med. 11, 933 (2005).

Physical State :
Solid
Solubility :
Soluble in DMSO (0.5 mg/ml), DMF (~0.2 mg/ml), and ethanol (<1 mg/ml at 25° C). Insoluble in water.
Storage :
Store at -20° C
Melting Point :
243.03° C (Predicted)
Boiling Point :
565.14° C (Predicted)
Density :
1.55 g/cm3 (Predicted)
Refractive Index :
n20D 1.79 (Predicted)
IC50 :
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)
Ki Data :
PI 3-K γ : Ki= 7.8 nM
pK Values :
pKa: 7.04 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
5289247
MDL Number :
MFCD11100415
SMILES :
C1=CC2=NC=CN=C2C=C1/C=C\3/C(=O)NC(=O)S3

Download SDS (MSDS)

Certificate of Analysis

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Rated 5 out of 5 by from Oghumu et al Oghumu 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
Date published: 2015-06-26
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