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| | IPI 145 Basic information |
| Product Name: | IPI 145 | | Synonyms: | IPI145; IPI 145; IPI-145. INK-1197; INK 1197; INK1197;DUVELISIB (IPI-145; INK1197);CS-680;8-chloro-2-phenyl-3-[(1s)-1-(7h-purin-6-ylamino)ethyl]isoquinolin-1-one;IPI-145 (Duvelisib, INK1197);IPI-145;IPI-145 (INK-1197);IPI-145 INK197;8-Chloro-2-phenyl-3-[(1S)-1-(9H-purin-6-ylamino)ethyl]-1(2H)-isoquinolinone | | CAS: | 1201438-56-3 | | MF: | C22H17ClN6O | | MW: | 416.86 | | EINECS: | 200-256-5 | | Product Categories: | reference inhibitors;Inhibitors | | Mol File: | 1201438-56-3.mol |  |
| | IPI 145 Chemical Properties |
| Melting point | 205-206o C | | Boiling point | 757.8±60.0 °C(Predicted) | | density | 1.474±0.06 g/cm3(Predicted) | | storage temp. | -20°C | | solubility | Soluble in DMSO (up to at least 25 mg/ml) | | pka | 10.05±0.10(Predicted) | | form | White solid. | | color | White | | Stability: | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
| | IPI 145 Usage And Synthesis |
| Description | Duvelisib (1201438-56-3) is a potent and selective (IC50’s: PI3Kα = 1602nM, PI3Kβ = 85nM, PI3Kδ= 2.5nM, PI3Kγ = 27nM) dual PI3Kδ/γ inhibitor.1 It inhibits B and T cell proliferation, blocks neutrophil migration, and inhibits basophil activation. Duvelisib antagonizes B-cell receptor cross-linking activated pro-survival signals in primary chronic lymphocytic leukemia cells.2?Duvelisib also shows preclinical/clinical activity against other hematologic malignancies such as Non-Hodgkins lymphoma, T-cell lymphoma, and others.3,4?Useful clinical agent for the treatment of various blood cancers. Low-dose treatment of T-cell-inflamed tumor models of head and neck cancers with Duvelisib enhanced responses to PD-L1 blockade via suppression of myeloid-derived suppressor cells.5?Higher doses reversed the effect due to suppression of tumor-infiltrating T lymphocytes | | Uses | IPI 145 is an 1,2-dihydroisoquinolin-1(2H)-one derivative and has been developed as a modulator of PI3 kinase. | | Definition | ChEBI: 8-chloro-2-phenyl-3-[(1S)-1-(7H-purin-6-ylamino)ethyl]-1-isoquinolinone is a member of isoquinolines. | | target | PI3K-δ | | References | 1) Winkler?et al.?(2013),?PI3K-δ and PI3K-γ Inhibition by IPI-145 Abrogates Immune Response and Suppresses Activity in Autoimmune and Inflammatory Disease Models;?Chem. Biol.?20?1309
2) Dong?et al.?(2014),?IPI-145 antagonizes intrinsic and extrinsic survival signals in chronic lymphocytic leukemia cells;?Blood?124?3583
3) Flinn?et al.?(2018),?Duvelisib, a novel dual inhibitor of PI3K-δ/γ, is clinically active in advances hematologic malignancies;?Blood?131?877
4) Faia?et al.?(2018),?The phosphoinositide-3 kinase (PI3K)-δ,γ inhibitor, duvelisib, shows preclinical synergy with multiple targeted therapies in hematologic malignancies;?PLoS One?13?e0200725
5) Davis?et al.?(2017),?Anti-PD-L1 Efficacy Can Be Enhanced by Inhibition of Myeloid-Derived Suppressor Cells with a Selective Inhibitor of PI3Kδ/γ;?Cancer Res.?77?2607 |
| | IPI 145 Preparation Products And Raw materials |
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