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작성일 : 14-01-20
[Chemdea] PI3K/mTOR Inhibitors (1)
AS 604850 – PI3Kg Inhibitor II / AS041164 – PI3Kg Inhibitor VII / AS-252424 – PI3Kg/CKII Inhibitor AS-605240 – PI3Kg Inhibitor / Compound 15e – PI3Ka Inhibitor
PI3K/mTOR Inhibitors (1)
 
 
Product Name: AS 604850 – PI3Kg Inhibitor II
 
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A cell-permeable thiazolidinedione compound that acts as a potent and ATP-competitive inhibitor of PI 3-Kg (Ki =
180 nM; IC50 = 250 nM). Exhibits great selectivity over PI 3-Ka (IC50 = 4.5 µM), PI 3-Kb and d (IC50 > 20 µM),and shows
little effect towards a large panel of receptors, unrelated enzymes, ion channels, and 38 commonly studied kinases.
Shown to block MCP-1-mediated monocyte chemotaxis in vitro and exhibit etter in vivo efficacy than LY294002 in
blocking RANTES- or thioglycollate-induced peritoneal neutrophil recruitment by oral administration in a murine
peritonitis model.
 
Details
Chemical Formula:
 
C11H5F2NO4
CAS No.:
 
648449-76-7
Molecular weight:
 
285.2
Purity:
≥99% by HPLC
Appearance:
 
Off white solid
Chemical name:
 
 5-(2,2-Difluoro-benzo[1,3]dioxol-5-ylmethylene)-thiazolidine-2,4-dione
Solubility:
 
DMSO (50mg/mL) or ethanol (5mg/mL)
Storage:
Protect from light. Packaged under inert gas
 
References
 
 
Product Name: AS041164 – PI3Kg Inhibitor VII
 
   클릭하시면 닫힙니다.이미지 저장을 원하시면 마우스 오른쪽클릭후 '다른이름으로 저장'을 하세요
 
A cell-permeable thiazolidinedione compound that acts as a potent, ATP-competitive, and isoform-selctive PI3-K inhibitor (g isoform IC50 = 0.07 µM, (a isoform IC50 = 0.24 µM, (b isoform IC50 = 1.45 µM, and (d isoform IC50= 1.70 µM) with
little or no activity against a panel of 38 other commonly studied kinases(<20% inhibition at 1.0 µM). Exhibits similar
pharmacokinetics as LY 294002 via oral administration, but is 3-times as potent (ED50 =27.35 mg/kg, p.o.) in blocking
rhRNATES-induced neutrophil peritoneal recruitment in mice in vivo.Also reported to exhibit significant in vivo
prophylactic efficacy against carrageenan-induced tissue swelling in a rat paw edema model (100 mg/kg, p.o)
 
Details
Chemical Formula:
 
C11H7NO4S
CAS No.:
 
6318-41-8
Molecular weight:
 
249.2
Purity:
99% by HPLC
Appearance:
 
Yellow solid
Chemical name:
 
 5-(Benzo[1,3]dioxol-5-ylmethylene)-thiazolidine-2,4-dione
Solubility:
 
DMSO (40mg/mL)
Storage:
Protect from light. Packaged under inert gas
 
References
 
 
Product Name: AS-252424 – PI3Kg/CKII Inhibitor
 
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AS-252424 is a potent inhibitor of PI3K with selectivity for the γ isoform. It inhibits human recombinant PI3Kγ IC50=
30 nM, PI3Ka IC50= 940 nM, PI3Kb IC50= 20,000 nM and PI3Kd IC50= 20,000 nM respectively.  AS-252424 alsoinhibits
C5a-mediated phosphorylation of Akt in RAW 264.7 macrophages with an IC50= 230 nM. In a mouse model of
peritonitis, PI 3-Kg this compound inhibited neutrophil recruitment 35% at a dose of 10 mg/kg.
 
Details
Chemical Formula:
 
C14H8FNO4S
CAS No.:
 
900515-16-4
Molecular weight:
 
305.3
Purity:
≥98% by HPLC
Appearance:
 
Yellow solid
Chemical name:
 
5-[[5-(4-Fluoro-2-hydroxyphenyl)-2-furanyl]methylene]-2,4-thiazolidinedione
Solubility:
 
DMSO (20mg/mL)
Storage:
Protect from light. Packaged under inert gas
 
References
 
 
Product Name: AS-605240 – PI3Kg Inhibitor
 
   클릭하시면 닫힙니다.이미지 저장을 원하시면 마우스 오른쪽클릭후 '다른이름으로 저장'을 하세요
 
A cell-permeable thiazolidinedionecompound that acts as a potent, selective, and ATP-competitive inhibitor of
phosphatidylinositol 3-kinase g (PI 3-Kg) (Ki = 7.8 nM); p110g IC50 = 8 nM, p110a IC50 = 60 nM, p110b IC50= 270 nM,
p110d IC50 = 300 nM. Does not affect the activity of a wide panel of kinases, receptors,enzymes, and ion channels even
at concentrations as high as 1 µM. Selectivelyblocks MCP-1, but not CSF-1-, dependent Akt phosphorylation and
chemotaxis in primary Pik3cg+/+ murine monocytes and in a human monocytic cell line THP-1 (IC50= 181 nM). Also
shown to exhibit in vivo efficacy in reducing neutrophil chemotaxis in murine peritonitis and arthritis models.
 
Details
Chemical Formula:
 
C12H7N3O2S
CAS No.:
 
648450-29-7
Molecular weight:
 
257.3
Purity:
≥98% by HPLC
Appearance:
 
Pink to reddish solid
Chemical name:
 
5-Quinoxalin-6-ylmethylene-thiazolidine-2,4-dione
Solubility:
 
DMSO (1mg/mL)
Storage:
Protect from light. Packaged under inert gas
 
References
 
 
Product Name: Compound 15e – PI3Ka Inhibitor
 
   클릭하시면 닫힙니다.이미지 저장을 원하시면 마우스 오른쪽클릭후 '다른이름으로 저장'을 하세요
 
A cell-permeable morpholino-thienopyrimidine compound that acts as a potent and isoform-selectiveinhibitor of PI 3-Ks
(p110a IC50 = 2 nM, p110b IC50 = 16 nM, p110g IC50 = 660 nM, and PI 3-K C2b IC50 = 220 nM) andinhibits non-PI 3-K
kinases only at much higher concentrations (IC50 ≥3.4 µM for Cdk2/E, KDR, PKA, and PKCa). Shown to inhibit cell
proliferation (IC50 = 580 nM) and serum-stimulated Akt phosphorylation (IC50 <3 µM) in A375 melanoma cells.
 
Details
Chemical Formula:
 
C16H15N3O2S
CAS No.:
 
371943-05-4
Molecular weight:
 
313.4
Purity:
≥99% by HPLC
Appearance:
 
White solid
Chemical name:
 
3-(4-Morpholinothieno[3,2-d]pyrimidin-2-yl)phenol
Solubility:
 
DMSO (25mg/mL) and DMF (30 mg/mL)
Storage:
Protect from light. Packaged under inert gas
 
Reference
 
 
Ordering informations
 
Catalog No.
Product Name
Size
CD0176
AS 604850 – PI3Kg Inhibitor II
1mg, 5mg, 10mg, 25mg,
50mg & 100mg
 CD0240
AS041164 – PI3Kg Inhibitor VII
1mg, 5mg, 10mg, 25mg,
50mg & 100mg
CD0228
AS-252424 – PI3Kg/CKII Inhibitor
1mg, 5mg, 10mg
& 25mg
CD0248
AS-605240 – PI3Kg Inhibitor
1mg, 5mg, 10mg, 50mg
& 100mg
CD0189
Compound 15e – PI3Ka Inhibitor
1mg, 5mg, 10mg, 25mg
& 50mg
 
 
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