371242-69-2
IC-87114
CAS: 371242-69-2
Molecular Formula: C22H19N7O
371242-69-2 - Names and Identifiers
371242-69-2 - Physico-chemical Properties
| Molecular Formula | C22H19N7O |
| Molar Mass | 397.43 |
| Density | 1.43 |
| Appearance | White powder solid. |
| Storage Condition | -20℃ |
| In vitro study | IC87114 is a potent and selective inhibitor of PI3Kδ. IC87114 acts on PI3Kδ with an IC50 of 0.5 μm and is 50-fold more selective than the other PI3K subtypes. Depending on the cell type treated with IC87114, PI3Kδ acts in the TNFα-induced signal to reduce Akt phosphorylation and PDK1 enzyme activity. IC87114 inhibits neutrophil polarization, fMLP-stimulated PIP3 production and chemotaxis. IC87114 significantly reduced ovalbumin (OVA)-induced entry of all granulocytes, eosinophils, neutrophils, and lymphocytes into the lung, as well as levels of IL-4, IL-5, IL-13, and RANTES, this effect was dose-dependent. IC87114 also reduced total IgE,OVA-specific IgE and LTC4 serum levels. IC87114 significantly reduced OVA-induced expansion of IL-4, IL-5, IL-13, ICAM-1, VCAM-1, RANTES, and eotaxin, and also significantly reduced OVA-induced phosphorylation of Akt serine, akt is a downstream effector of the PI3K signaling pathway. IC87114 inhibits acute myelogenous leukemia proliferation and enhances the effect of topoisomerase II inhibitors on specific PI3Kδ subtypes. |
| In vivo study | The PI3Kδ inhibitor IC87114 acts in a murine model of inflammatory response to block the extracellular secretion of TNF1α-stimulated elastase from neutrophils. In vivo, IC87114 acts on disease models with suitable pharmacokinetic properties. |
371242-69-2 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.516 ml | 12.581 ml | 25.162 ml |
| 5 mM | 0.503 ml | 2.516 ml | 5.032 ml |
| 10 mM | 0.252 ml | 1.258 ml | 2.516 ml |
| 5 mM | 0.05 ml | 0.252 ml | 0.503 ml |
Last Update：2024-01-02 23:10:35
371242-69-2 - Reference Information
| biological activity | IC-87114 is a selective PI3Kδ inhibitor with an IC50 of 0.5 μm, the selectivity for PI3Kδ is 58 and 100 times higher than for PI3Kγ and PI3Kα/β, respectively. |
| In vitro studies | IC87114 is a potent and selective inhibitor of PI3Kδ. IC87114 acts on PI3Kδ with an IC50 of 0.5 μm and is 50-fold more selective than the other PI3K subtypes. Depending on the cell type treated with IC87114, PI3Kδ acts in the TNFα-induced signal to reduce Akt phosphorylation and PDK1 enzyme activity. IC87114 inhibits neutrophil polarization, fMLP-stimulated PIP3 production and chemotaxis. IC87114 significantly reduced ovalbumin (OVA)-induced entry of all granulocytes, eosinophils, neutrophils, and lymphocytes into the lung, as well as levels of IL-4, IL-5, IL-13, and RANTES, this effect was dose-dependent. IC87114 also reduced total IgE,OVA-specific IgE and LTC4 serum levels. IC87114 significantly reduced OVA-induced expansion of IL-4, IL-5, IL-13, ICAM-1, VCAM-1, RANTES, and eotaxin, and also significantly reduced OVA-induced phosphorylation of Akt serine, akt is a downstream effector of the PI3K signaling pathway. IC87114 inhibits acute myelogenous leukemia proliferation and enhances the effect of topoisomerase II inhibitors on specific PI3Kδ subtypes. |
| in vivo study | PI3Kδ inhibitor IC87114 acts on mouse model with inflammatory response, blocks the extracellular secretion of TNF1α-stimulated elastase from neutrophils. In vivo, IC87114 acts on disease models with suitable pharmacokinetic properties. |
| signature | IC-87114 was the first PI3K subtype selective inhibitor. |
Last Update：2024-04-09 21:11:58
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Product Name: IC-87114 Visit Supplier Webpage Request for quotation
CAS: 371242-69-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 371242-69-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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