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Formula | C12H7N3O2S |
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Molecular Weight | 257.27 | CAS No. | 648450-29-7 | |
Solubility (25°C)* | In vitro | 0.5MNAOH | 3.02 mg/mL (11.73 mM) | |
DMSO | 0.66 mg/mL (2.56 mM) | |||
Water | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | AS-605240 selectively inhibits PI3Kγ with IC50 of 8 nM, over 30-fold and 7.5-fold more selective for PI3Kγ than PI3Kδ/β and PI3Kα in cell-free assays, respectively. | ||||||||
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Targets |
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In 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] | ||||||||
In 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. In a mouse model of collagen-induced arthritis, AS-605240 (50 mg/kg) also suppresses joint inflammation and damage. [1] In an obesity-induced diabetes model (ob/ob mice), AS-605240 (10 mg/kg) lowers blood glucose levels, significantly improves both insulin sensitivity and glucose tolerance without affecting body weight. AS-605240 (30 mg/kg) displays more profound effects with slightly less weight gain. Moreover, AS-605240 reduces the abundance of ATMs and the circulating levels of MCP-1. [3] | ||||||||
Features | The most potent member of a new class of PI3Kγ-selective inhibitors. |
Kinase Assay: |
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Cell Assay: |
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Animal Study: |
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, , Dr. Zhang of Tianjin Medical University
, , Saraswati Sukumar of Johns Hopkins University School of Medicine
Data from [Data independently produced by , , Oncol Lett, 2018, 15(2):2105-2110]
Therapeutic potential of anti-PIK3CG treatment for multiple myeloma via inhibiting c-Myc pathway [ Heliyon, 2024, 10(1):e23165] | PubMed: 38163179 |
Neural progenitor-derived Apelin controls tip cell behavior and vascular patterning [ Sci Adv, 2024, 10(27):eadk1174] | PubMed: 38968355 |
Alcam-a and Pdgfr-α are essential for the development of sclerotome-derived stromal cells that support hematopoiesis [ Nat Commun, 2023, 14(1):1171] | PubMed: 36859431 |
Platelet p110β mediates platelet-leukocyte interaction and curtails bacterial dissemination in pneumococcal pneumonia [ Cell Rep, 2022, 41(6):111614] | PubMed: 36351402 |
Connectivity Mapping Using a Novel sv2a Loss-of-Function Zebrafish Epilepsy Model as a Powerful Strategy for Anti-epileptic Drug Discovery [ Front Mol Neurosci, 2022, 15:881933] | PubMed: 35686059 |
Grape-Seed-Derived Procyanidin Attenuates Chemotherapy-Induced Cognitive Impairment by Suppressing MMP-9 Activity and Related Blood-Brain-Barrier Damage [ Brain Sci, 2022, 12(5)571] | PubMed: 35624958 |
A PI3Kγ signal regulates macrophage recruitment to injured tissue for regenerative cell survival [ Dev Growth Differ, 2022, 64(8):433-445] | PubMed: 36101496 |
Oxytocin signalling in dendritic cells regulates immune tolerance in the intestine and alleviates DSS-induced colitis [ Clin Sci (Lond), 2021, 135(4):597-611] | PubMed: 33564880 |
BTK and PI3K Inhibitors Reveal Synergistic Inhibitory Anti-Tumoral Effects in Canine Diffuse Large B-Cell Lymphoma Cells [ Int J Mol Sci, 2021, 22(23)12673] | PubMed: 34884478 |
Baicalein Potentiated M1 Macrophage Polarization in Cancer Through Targeting PI3Kγ/ NF-κB Signaling [ Front Pharmacol, 2021, 12:743837] | PubMed: 34512367 |
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.