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Technical Data
| Formula | C23H26N4O3 |
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| Molecular Weight | 406.48 | CAS No. | 1386874-06-1 | |
| Solubility (25°C)* | In vitro | DMSO | 81 mg/mL (199.27 mM) | |
| Ethanol | 8 mg/mL (19.68 mM) | |||
| Water | 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 | Samotolisib (LY3023414, GTPL8918) is an oral ATP competitive inhibitor of the class I PI3K isoforms, mTOR and DNA-PK. | |||
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| In vitro | LY3023414 shows high solubility across a wide pH range. In vitro, inhibition of PI3K/AKT/mTOR signaling by LY3023414 causes G1 cell-cycle arrest and resulted in broad antiproliferative activity in cancer cell panel screens. In cell-based assays, LY3023414 inhibition of PI3K and mTOR is assessed in the PTEN-deficient U87 MG glioblastoma cell line. LY3023414 inhibits the phosphorylation of AKT at position T308 downstream of PI3K at an IC50 of 106 nM. Similarly, LY3023414 inhibits phosphorylation of AKT at position S473 (IC50 = 94.2 nM) by mTORC2 as well as phosphorylation of mTORC1 kinase targets p70S6K (position T389; IC50 =10.6 nM) and 4E-BP1 (positions T37/46; IC50 = 187 nM). The downstream phosphorylation of S6RP at positions pS240/244 (IC50 = 19.1 nM) by p70S6K was inhibited as well, indicating target inhibition along the entire PI3K/AKT/mTOR pathway by LY3023414[1]. | |||
| In vivo | In vivo, LY3023414 demonstrates high bioavailability and dose-dependent dephosphorylation of PI3K/AKT/mTOR pathway downstream substrates such as AKT, S6K, S6RP, and 4E-BP1 for 4 to 6 hours, reflecting the drug's half-life of 2 hours. Intermittent target inhibition is sufficient for its antitumor activity. LY3023414 shows time- and dose-dependent target inhibition in vivo. It is currently being evaluated in phase 1 and 2 trials for the treatment of human malignancies[1]. |
Protocol (from reference)
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Customer Product Validation
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Data from [Data independently produced by , , Oncotarget, 2017, 8(58): 98964-98973]
Selleck's Samotolisib (LY3023414) has been cited by 8 publications
| Protective effect of leukemia inhibitory factor on the retinal injury induced by acute ocular hypertension in rats [ Exp Ther Med, 2023, 25(1):19] | PubMed: 36561619 |
| Functional impact and targetability of PI3KCA, GNAS, and PTEN mutations in a spindle cell rhabdomyosarcoma with MYOD1 L122R mutation [ Cold Spring Harb Mol Case Stud, 2022, 8(1)a006140] | PubMed: 35012940 |
| Microenvironment drives cell state, plasticity, and drug response in pancreatic cancer [ Cell, 2021, 184(25):6119-6137.e26] | PubMed: 34890551 |
| Samotolisib Attenuates Acute Liver Injury Through Inhibiting Caspase-11-Mediated Pyroptosis Via Regulating E3 Ubiquitin Ligase Nedd4 [ Front Pharmacol, 2021, 12:726198] | PubMed: 34483936 |
| Uraemic extracellular vesicles augment osteogenic transdifferentiation of vascular smooth muscle cells via enhanced AKT signalling and PiT-1 expression [ J Cell Mol Med, 2021, 25(12):5602-5614] | PubMed: 33960650 |
| LY3023414 inhibits both osteogenesis and osteoclastogenesis through the PI3K/Akt/GSK3 signalling pathway [ Bone Joint Res, 2021, 10(4):237-249] | PubMed: 33789427 |
| Phosphorylation of PRAS40 contributes to the activation of the PI3K/AKT/mTOR signaling pathway and the inhibition of autophagy following status epilepticus in rats [ Exp Ther Med, 2020, 20(4):3625-3632] | PubMed: 32855714 |
| Autophagy inhibition sensitizes LY3023414-induced anti-glioma cell activity in vitro and in vivo. [ Oncotarget, 2017, 8(58):98964-98973] | PubMed: 29228741 |
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.