|
AS-605240
Cayman Chemical Item Number 10007707
Description
Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of phosphatidylinositol at the three position to produce the second messengers PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3.1↗,2↗,3↗ PI3Kγ is a class 1B PI3K that is composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit, whereas PI3Kα, β, and δ are class 1A enzymes composed of p110 and p85 subunits4↗ AS-605240 is an orally active inhibitor of PI3-kinase γ that suppresses joint inflammation in mouse models of rheumatoid arthritis.5↗ It inhibits human recombinant PI3Kγ, α, β, and δ in an ATP-competitive manner with IC50 values of 8, 60, 270, and 300 nM, respectively.5↗ AS-605240 inhibits C5a-mediated phosphorylation of protein kinase B in RAW 264 cells with an IC50 value of 90 nM. In vivo, AS-605240 reduced RANTES-induced peritoneal neutrophil recruitment in a mouse model of leukocyte chemotaxis with an ED50 value of 9.1 mg/kg.
Formal Name 5-(6-quinoxalinylmethylene)-2,4-thiazolidinedione
CAS Number 648450-29-7
Molecular Formula C12H7N3O2S
Formula Weight 257.3
Formulation A crystalline solid
Purity >98%
λmax 249, 297, 337, 352 nm
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES O=C1NC(=O)/C(=C\c2ccc3nccnc3c2)\S1
InCHI Code 1S/C12H7N3O2S/c16-11-10(18-12(17)15-11)6-7-1-2-8-9(5-7)14-4-3-13-8/h1-6H,(H,15,16,17)/b10-6-
InCHI Key SQWZFLMPDUSYGV-POHAHGRESA-N |