1. PI3K/Akt/mTOR
    Autophagy
  2. PI3K
    Autophagy

AS-605240 

Cat. No.: HY-10109 Purity: >98.0%
Handling Instructions

AS-605240 is a specific and orally active inhibitor of the PI3Kγ, with an IC50 of 8 nM, and a Ki of 7.8 nM.

For research use only. We do not sell to patients.

AS-605240 Chemical Structure

AS-605240 Chemical Structure

CAS No. : 648450-29-7

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
10 mg USD 60 In-stock
Estimated Time of Arrival: December 31
50 mg USD 238 In-stock
Estimated Time of Arrival: December 31
100 mg USD 336 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

AS-605240 is a specific and orally active inhibitor of the PI3Kγ, with an IC50 of 8 nM, and a Ki of 7.8 nM.

IC50 & Target[2]

PI3Kγ

8 nM (IC50)

PI3Kα

60 nM (IC50)

PI3Kβ

270 nM (IC50)

PI3Kδ

300 nM (IC50)

Autophagy

 

In Vitro

AS-605240 is an isoform-selective inhibitor of PI3Kγ with over 30-fold selectivity for PI3Kδ and β, and 18- and 7.5-fold selectivity over PI3Kα, respectively. AS-605240 shows an inhibitory effect on C5a-mediated PKB phosphorylation in RAW264 mouse macrophages with an IC50 of 0.09 μM. AS-605240 blocks PKB phosphorylation induced by MCP-1 and has little or no effect after stimulation with CSF-1. AS-605240 inhibits MCP-1-mediated phosphorylation of PKB and its downstream substrates GSK3α and β in a concentration-dependent manner. AS605240 suppresses in a dose-dependent manner the proliferation of BDC2.5 CD4+ T cells[2].

In Vivo

AS-605240 (30 mg/kg BW, per os, every 12 h) markedly decreases FoxM1 expression in mouse lungs and fails to restore vascular integrity[1]. AS-605240 reduces RANTES-induced peritoneal neutrophil recruitment, with ED50 of 9.1 mg/kg. In the CCL5 model, AS-605240 shows an ED50 value of 10 mg/kg, in correlation with the percentage of reduction of neutrophil recruitment observed in Pik3cg-/- mice. AS-605240 (50 mg/kg, p.o.) substantially reduces clinical and histological signs of joint inflammation to a similar extent to that of Pik3cg-/- mice[2]. AS605240 (30 mg/kg, i.p.) suppresses intracellular PAkt in splenocytes of NOD mice and delays diabetes onset. AS605240 also prevents autoimmune diabetes in prediabetic NOD mice, and suppresses autoreactive T cells while increasing Tregs in NOD mice. AS605240 (30 mg/kg, i.p.) reverses hyperglycemia in newly hyperglycemic NOD mice, reverses hyperglycemia in early diabetic NOD mice through Tregs and suppresses T-cell infiltration in pancreatic islets while increasing Tregs[3]. AS605240 (25, 50 mg/kg) markedly reduces total cell count and numbers of macrophages, neutrophils and lymphocytes in rats. AS605240 significantly reduces the levels of TNF-α and IL-1β in BALF to 132.7±11.2 pg/mL and 49.2±11.3 pg/mL in 25 mg/kg AS605240 + BLM group and 131.3±10.7 and 49.6±8.8 pg/mL in 50 mg/kg AS605240 + BLM group, respectively. AS605240 inhibits prefibrotic cytokines production in bleomycin-induced pulmonary fibrosis. AS605240 inhibits phosphorylation of Akt of inflammatory cells in bleomycin-induced pulmonary fibrosis model[4].

Solvent & Solubility
In Vitro: 

DMSO : 5.8 mg/mL (22.54 mM; Need warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.8870 mL 19.4348 mL 38.8697 mL
5 mM 0.7774 mL 3.8870 mL 7.7739 mL
10 mM 0.3887 mL 1.9435 mL 3.8870 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[2]

Human PI3Kγ (100 ng) is incubated at RT with kinase buffer (10 mM MgCl2, 1 mM β-glycerophosphate, 1 mM DTT, 0.1 mM Na3VO4, 0.1% Na Cholate and 15 M ATP/100 nCi γ[33P]ATP, final concentrations) and lipid vesicles containing 18 M PtdIns and 250 M of PtdSer (final concentrations), in the presence of inhibitors or DMSO. Kinase reaction is stopped by adding 250 g of Neomycin-coated Scintillation Proximity Assay (SPA) bead and proceeded.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[3]

A total of 5×105 BDC2.5 splenocytes and 50 μg/mL BDC2.5-peptide are incubated in vitro in a 96-well round-bottom plate for 48 h. Then the cultures are pulsed with 1 μCi of tritiated thymidine [3H] to determine cell proliferation.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[4]

In this study, rats are bred for one week to affirm body weight and then randomLy divided into four experimental groups: (a) control group (rats are given vehicle only); (b) BLM group (rats are induced with BLM); (c) BLM + 25 mg/kg AS605240 group (rats are induced with BLM and then administrated with 25 mg/kg AS605240); (d) BLM + 50 mg/kg AS605240 group (the same protocol as the former group except a different dose of 50 mg/kg AS605240). In addition, five rats are given 50 mg/kg AS605240 only to detect whether AS605240 has any side effect simultaneously as the previous four groups. Rats in (c), (d) and AS605240-given-only group are administered orally 25, 50 and 50 mg/kg AS605240 by gavage while rats in control group and BLM group are given only equivalent saline at day-1 (the day rats are given BLM is marked as day-0). The same dosage is maintained once everyday for 28 days.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

257.27

Formula

C₁₂H₇N₃O₂S

CAS No.

648450-29-7

SMILES

O=C(NC/1=O)SC1=C/C2=CC=C3N=CC=NC3=C2

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Purity: >98.0%

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Product Name:
AS-605240
Cat. No.:
HY-10109
Quantity:

AS-605240

Cat. No.: HY-10109