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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder | |
化学式 | C25H23F3N2O5S |
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分子量 | 520.52 | CAS No. | 1809427-19-7 | |
Solubility (25°C)* | 体外 | DMSO | 100 mg/mL (192.11 mM) | |
Ethanol | 50 mg/mL (96.05 mM) | |||
Water | Insoluble | |||
* <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. |
製品説明 | DT-061 (SMAP) is a bioavailable PP2A activator. It decreases cell viability in HCC827 and HCC3255 cell lines, with IC50 values of 14.3 μM and 12.4 μM respectively. |
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in vivo | PP2A reactivation using single agent SMAP DT-061 is a well-tolerated and orally bioavailable therapeutic strategy that is as efficacious as a combination of kinase inhibitors in antagonizing EGFR-driven TKI-resistant LUAD models. Furthermore, treatment with SMAP can overcome resistance in those models, with an even greater effect when combined with afatinib[1]. |
細胞アッセイ | 細胞株 | HCC827 and H3255 cell lines |
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濃度 | 2.5, 5, 7.5, 10, 12.5, 15, 17.5, or 20 μM | |
反応時間 | 48 h | |
実験の流れ | Cells are treated with DMSO control or 2.5, 5, 7.5, 10, 12.5, 15, 17.5, or 20 μM SMAP DT-061 for 48 hours. |
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動物実験 | 動物モデル | A TKI-resistant EGFR(L858R) patient-derived xenograft (PDX) model (NSG female mice) |
投薬量 | 5 mg/kg | |
投与方法 | by oral gavage |
A transcriptional network governing ceramide homeostasis establishes a cytokine-dependent developmental process [ Nat Commun, 2023, 10.1038/s41467-023-42978-w] | PubMed: 37945603 |
Carboxypeptidase A4 negatively regulates HGS-ETR1/2-induced pyroptosis by forming a positive feedback loop with the AKT signalling pathway [ Cell Death Dis, 2023, 14(12):793] | PubMed: 38049405 |
A Wnt-induced lncRNA-DGCR5 splicing switch drives tumor-promoting inflammation in esophageal squamous cell carcinoma [ Cell Rep, 2023, 42(6):112542] | PubMed: 37210725 |
LCK-Mediated RIPK3 Activation Controls Double-Positive Thymocyte Proliferation and Restrains Thymic Lymphoma by Regulating the PP2A-ERK Axis [ Adv Sci (Weinh), 2022, e2204522] | PubMed: 36161785 |
GSK3β is a critical, druggable component of the network regulating the active NOTCH1 protein and cell viability in CLL [ Cell Death Dis, 2022, 13-9:755] | PubMed: 36050315 |
Arid1a regulates cell cycle exit of transit-amplifying cells through inhibiting the Aurka-Cdk1 axis in mouse incisor [ Development, 2021, dev.198838] | PubMed: 33766930 |
Protein Phosphatase 2A Inhibits Gastric Cancer Cell Glycolysis by Reducing MYC Signaling [ Research Square, 2021, 10.21203/rs.3.rs-362391/v1] | PubMed: None |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。