5-(6-Quinoxalinylmethylene)-2,4-thiazolidinedione

5-(6-Quinoxalinylmethylene)-2,4-thiazolidinedione
  • CAS No.:648450-29-7
Other grades of this product :
5-(6-Quinoxalinylmethylene)-2,4-thiazolidinedione Basic information
Product Name:5-(6-Quinoxalinylmethylene)-2,4-thiazolidinedione
Synonyms:5-(6-Quinoxalinylmethylene)-2,4-thiazolidinedione;AS605240;5-(6-Quinoxalinylmethylene)-2,4-thiazolidine-2,4-dione;PI 3-Kinase Inhibitor (AS605240) B-0301;AS-605240, >=98%;(E)-5-(quinoxalin-6-ylMethylene)thiazolidine-2,4-dione;2,4-Thiazolidinedione, 5-(6-quinoxalinylMethylene)-;AS-605240(AS 605240)
CAS:648450-29-7
MF:C12H7N3O2S
MW:257.27
EINECS:
Product Categories:Inhibitors;API;Akt;mTOR;PI3K
Mol File:648450-29-7.mol
5-(6-Quinoxalinylmethylene)-2,4-thiazolidinedione Chemical Properties
density 1.553±0.06 g/cm3(Predicted)
storage temp. 2-8°C
solubility DMSO: soluble1mg/mL, clear (warmed)
pka6.02±0.20(Predicted)
form powder
color , faint red to orange to dark brown
Safety Information
Hazard Codes Xi
Risk Statements 36/37/38
Safety Statements 26
WGK Germany 3
HS Code 2934100090
MSDS Information
5-(6-Quinoxalinylmethylene)-2,4-thiazolidinedione Usage And Synthesis
UsesAS605240 has been used:
  • as a phosphatidylinositol 3-kinase (PI3K) inhibitor to study its effect on Rab5-positive early endosome (EE) vesicles.
  • as a (PI3K) inhibitor to treat splenocytes for graft-versus-host disease (GVHD) induction.
  • as a class 1A PI3K inhibitor?to treat CD4+?T cells.
Biological ActivityPotent and selective inhibitor of PI 3-kinase γ (PI3K γ ) (IC 50 = 8 nM). Displays 30-fold selectivity over PI3K δ and PI3K β and 7.5-fold selectivity over PI3K α . Suppresses the progression of joint inflammation and damage in both lymphocyte-independent and lymphocyte-dependent mouse models of rheumatoid arthritis. Orally active and ATP-competitive.
Biochem/physiol ActionsAS605240 inhibits human recombinant phosphatidylinositol 3-kinase (PI3K) γ, α, β, and δ by competing with adenosine triphosphate (ATP). It plays a role in protecting injury following ischemic stroke. AS605240 also inhibits the activation of astrocytes under the influence of Interleukin-6 (IL-6) and its soluble receptor (sIL-6R). It reduces collagen deposition and prevents lung inflammation. AS605240 also inhibits the increase of tumor necrosis factor-α (TNF-α) and interleukin-1β (IL-1β) expression instigated by bleomycin. It is effective in preventing pulmonary fibrosis by inhibiting the transforming growth factor β1 (TGF-β1) and T lymphocytes infiltration into lungs.
references[1]. camps m, rückle t, ji h, et al. blockade of pi3kγ suppresses joint inflammation and damage in mouse models of rheumatoid arthritis[j]. nature medicine, 2005, 11(9): 936-943.[2]. marone r, cmiljanovic v, giese b, et al. targeting phosphoinositide 3-kinase—moving towards therapy[j]. biochimica et biophysica acta (bba)-proteins and proteomics, 2008, 1784(1): 159-185.
5-(6-Quinoxalinylmethylene)-2,4-thiazolidinedione Preparation Products And Raw materials

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