| Identification | Back Directory | [Name]
Ethanone, 1-[7-[[2-[[4-(4-ethyl-1-piperazinyl)phenyl]amino]-4-pyridinyl]amino]-2,3-dihydro-1H-indol-1-yl]- | [CAS]
2919575-27-0 | [Synonyms]
UCL-TRO-1938
Ethanone, 1-[7-[[2-[[4-(4-ethyl-1-piperazinyl)phenyl]amino]-4-pyridinyl]amino]-2,3-dihydro-1H-indol-1-yl]- | [Molecular Formula]
C27H32N6O | [MOL File]
2919575-27-0.mol | [Molecular Weight]
456.58 |
| Chemical Properties | Back Directory | [Boiling point ]
677.0±55.0 °C(Predicted) | [density ]
1.243±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(Predicted) | [form ]
Solid | [pka]
8.22±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
UCL-TRO-1938 is a potent small molecule allosteric activator of PI3Kα with an EC50 value of approximately 60 μM. UCL-TRO-1938 can induce cell proliferation and has cardioprotective effects from ischaemia reperfusion injury and enhances nerve regeneration following nerve crush[1][2][3][4][5]. | [in vivo]
UCL-TRO-1938 (10 mg/kg or 5 μM, 100 μM, i.v., a single dose 15 min prior to reperfusion or a single dose for 21 days) provides cardioprotection and stimulates nerve regeneration in model of ischaemia reperfusion injury in mice and rat sciatic nerve crush model of peripheral nerve injury and regeneration[1].
| Animal Model: | Model of ischaemia reperfusion injury in mice and rat sciatic nerve crush model of peripheral nerve injury and regeneration | | Dosage: | 10 mg/kg or 5 μM, 100 μM | | Administration: | i.v., a single dose 15 min prior to reperfusion or a single dose for 21 days | | Result: | Provided substantial tissue protection from IRI, increasing tissue survival and reducing infarct size, and significantly increased neurite outgrowth in dissociated adult rat dorsal root ganglion (DRG) cultures. |
| [References]
[1] Gong GQ, et al. A small-molecule PI3Kα activator for cardioprotection and neuroregeneration. Nature. 2023 Jun;618(7963):159-168. DOI:10.1038/s41586-023-05972-2
[2] Shi H, et al. miR-30c-5p inhibits esophageal squamous cell carcinoma progression by repressing the PI3K/AKT signaling pathway. Thorac Cancer. 2024 Oct;15(30):2206-2216. DOI:10.1111/1759-7714.15427
[3] Najam O. Exploring the role of cardiac mast cells in acute myocardial infarction and ischaemia-reperfusion injury[D]. UCL (University College London), 2023.
[4] Kingwell K. PI3K activator taps route to regeneration. Nat Rev Drug Discov. 2023 Jul;22(7):537. DOI:10.1038/d41573-023-00097-7
[5] Ni C, et al. An inappropriate decline in ribosome levels drives a diverse set of neurodevelopmental disorders. bioRxiv [Preprint]. 2024 Jan 9:2024.01.09.574708. DOI:10.1101/2024.01.09.574708 |
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