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Technical Data
| Formula | C15H17FN6O2S |
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| Molecular Weight | 364.4 | CAS No. | 1159824-67-5 | |
| Solubility (25°C)* | In vitro | DMSO | 5 mg/mL (13.72 mM) | |
| Water | Insoluble | |||
| Ethanol | Insoluble | |||
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* <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.) |
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Biological Activity
| Description | CZC24832 is the first selective PI3Kγ inhibitor with IC50 of 27 nM, with 10-fold selectivity over PI3Kβ and >100-fold selectivity over PI3Kα and PI3Kδ. | ||||
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| Targets |
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| In vitro | CZC24832 has excellent selectivity to PI3Kγ. Out of the 154 identified lipid and protein kinases and the 922 other proteins, only two off targets (PI3Kβ and PIP4K2C) are detected within a 100-fold selectivity window. Despite the high sequence conservation of the human and rodent class I PI3K isoforms, the potency of CZC24832 for PI3Kγ and PI3Kβ is consistently lower by a factor of 2 to 4 in mice and rats compared to humans, but selectivity windows are largely retained. In the BT system, treatment with CZC24832 results in profound inhibition of IL-17A (IC50 =1.5 μM) as well as of B-cell activation markers such as IL-6 and IgG. In addition, strong inhibition of IL17A production is observed in T-cell systems such as human umbilical vein endothelial cells grown in the presence of TH2 blasts, indicating a general role for PI3Kγ kinase activity in the control of TH17 function. Thus, CZC24832 inhibits TH17 cell differentiation. [1] | ||||
| In vivo | In an IL-8–dependent air pouch model, CZC24832 shows a dose dependent reduction of granulocyte recruitment consistent with the degree of inhibition observed in PI3Kγ-null mice. In a therapeutic collagen induced arthritis (CIA) model, mice treated orally with 10 mg CZC24832 per kg body weight twice per day shows a substantial decrease of bone and cartilage destruction as well as of overall clinical parameters. [1] |
Protocol (from reference)
| Animal Study:[1] |
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Customer Product Validation
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, , Blood Cancer J, 2017, 7(3):e539
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Data from [Data independently produced by , , Sci Rep, 2018, 8(1):5558]
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Data from [Data independently produced by , , Leukemia, 2018, 32(9):1958-1969]
Selleck's CZC24832 has been cited by 14 publications
| Roles of PI3Kγ and PI3Kδ in mantle cell lymphoma proliferation and migration contributing to efficacy of the PI3Kγ/δ inhibitor duvelisib [ Sci Rep, 2023, 13(1):3793] | PubMed: 36882482 |
| Combined Treatment with PI3K Inhibitors BYL-719 and CAL-101 Is a Promising Antiproliferative Strategy in Human Rhabdomyosarcoma Cells [ Molecules, 2022, 27(9)2742] | PubMed: 35566091 |
| Time Series Transcriptomic Analysis by RNA Sequencing Reveals a Key Role of PI3K in Sepsis-Induced Myocardial Injury in Mice [ Front Physiol, 2022, 13:903164] | PubMed: 35721566 |
| Inhibition of Phosphoinositide 3-Kinase Gamma Protects Endothelial Cells via the Akt Signaling Pathway in Sepsis-Induced Acute Kidney Injury [ Kidney Blood Press Res, 2022, 47(10):616-630] | PubMed: 36130530 |
| HBx induces hepatocellular carcinogenesis through ARRB1-mediated autophagy to drive the G1/S cycle [ Autophagy, 2021, 1-19] | PubMed: 33866937 |
| Electrotaxis of Glioblastoma and Medulloblastoma Spheroidal Aggregates. [ Sci Rep, 2019, 9(1):5309] | PubMed: 30926929 |
| PI3Kβ is selectively required for growth factor-stimulated macropinocytosis [ J Cell Sci, 2019, 132(16)jcs231639] | PubMed: 31409694 |
| Distinct roles for phosphoinositide 3-kinases γ and δ in malignant B cell migration [Ali AY Leukemia, 2018, 32(9):1958-1969] | PubMed: 29479062 |
| p110α Inhibition Overcomes Stromal Cell-Mediated Ibrutinib Resistance in Mantle Cell Lymphoma [Guan J Mol Cancer Ther, 2018, 17(5):1090-1100] | PubMed: 29483220 |
| Idelalisib impairs TREM-1 mediated neutrophil inflammatory responses [Alflen A Sci Rep, 2018, 8(1):5558] | PubMed: 29615799 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
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.