| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
AS-605240 is a novel, potent, orally bioactive andATP-competitiveinhibitor of PI3-kinase γ (PI3Kγ) with potential anti-inflammatory activity. With an IC50 of 8 nM, it selectively inhibits PI3Kγ and, in cell-free assays, is >30-fold and 7.5-fold more selective for PI3Kγ than PI3Kδ/β and PI3Kα, respectively. Inflammatory illnesses may be treated with AS605240. According to studies, taking AS605240 orally significantly reduced collagen buildup and prevented lung inflammation.
| Targets |
PI3Kα (IC50 = 60 nM); PI3Kβ (IC50 = 270 nM); PI3Kδ (IC50 = 300 nM); PI3Kγ (IC50 = 8 nM); PI3Kγ (Ki = 7.8 nM); Autophagy
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| ln Vitro |
AS-605240 is an ATP-competitive PI3Kγ inhibitor, with Ki values of 7.8 nM. AS-605240 is isoform-selective, for AS-605240 also inhibits PI3Kα, β, and δ, with IC50 of 60, 270, and 300 nM, respectively. AS-605240 inhibits C5a-mediated PKB phosphorylation with IC50 of 90 nM. In bone marrow-derived monocytes (BMDMs), AS-605240 (1 μM) blocks MCP-1- or CSF-1-induced PKB phosphorylation. [1] At SC-CA1 synapses in mice, AS-605240 (100 nM) eliminates NMDAR LTD, without affecting mGluR LTD, depotentiation, and LTP. [2] With an IC50 of 90 nM, AS-605240 blocks PKB phosphorylation caused by C5a. AS-605240 (1 M) prevents MCP-1 or CSF-1 from inducing PKB phosphorylation in bone marrow-derived monocytes (BMDMs). [1] When used at mice's SC-CA1 synapses, AS-605240 (100 nM) completely eliminates NMDAR LTD while having no effect on mGluR LTD, depotentiation, or LTP. [2]
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| ln Vivo |
In RANTES-induced mouse model of peritonitis, AS-605240 reduces neutrophil chemotaxis with ED50 of 9.1 mg/kg. In a αCII-induced arthritis, AS-605240 (50 mg/kg) protects against αCII-IA symptom. AS-605240 (50 mg/kg) also reduces joint inflammation and damage in a mouse model of collagen-induced arthritis. [1] AS-605240 (10 mg/kg) significantly improves insulin sensitivity and glucose tolerance in an obesity-induced diabetes model (ob/ob mice) without changing body weight. It also significantly lowers blood glucose levels. With a little less weight gain, AS-605240 (30 mg/kg) exhibits more significant effects. Additionally, AS-605240 lowers both the MCP-1 circulation levels and the abundance of ATMs. [3]
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| Enzyme Assay |
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. By adding 250 g of Neomycin-coated Scintillation Proximity Assay (SPA) bead, the kinase reaction is stopped, and the process is then continued.
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| Cell Assay |
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. The next step is to measure cell proliferation by pulse-dosing the cultures with 1 μCi of tritiated thymidine [3H].
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| Animal Protocol |
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). Additionally, five rats are given 50 mg/kg of AS605240 to see if it has any side effects at the same time as the other four groups. Rats in groups (c), (d), and those receiving only AS605240 are given 25, 50, and 50 mg/kg of the drug orally by gavage, whereas rats in groups (control) and BLM are given only equivalence saline on day 1 (the day rats are given BLM is marked as day 0). For 28 days, the same dosage is administered once daily.
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| References |
| Molecular Formula |
C12H7N3O2S
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|---|---|
| Molecular Weight |
257.2679
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| Exact Mass |
257.0259
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| Elemental Analysis |
C, 56.02; H, 2.74; N, 16.33; O, 12.44; S, 12.46
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| CAS # |
648450-29-7
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| Related CAS # |
648450-29-7
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| Appearance |
Solid powder
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| SMILES |
C1=CC2=NC=CN=C2C=C1/C=C\3/C(=O)NC(=O)S3
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| InChi Key |
SQWZFLMPDUSYGV-UXBLZVDNSA-N
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| InChi Code |
InChI=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-
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| Chemical Name |
(5Z)-5-(quinoxalin-6-ylmethylidene)-1,3-thiazolidine-2,4-dione
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| Synonyms |
AS 605240; AS605240; AS-605240
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~0.4 mg/mL (~1.6 mM)
Water: <1 mg/mL Ethanol: <1 mg/mL |
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| Solubility (In Vivo) |
0.5% CMC+0.25%Tween 80: 11mg/mL (Please use freshly prepared in vivo formulations for optimal results.)
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| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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