DEL-22379

製品コードS7921 バッチS792101

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C26H28N4O3
分子量 444.53 CAS No. 181223-80-3
Solubility (25°C)* 体外 DMSO 89 mg/mL (200.21 mM)
Water Insoluble
Ethanol 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 DEL-22379 is a water-soluble ERK dimerization inhibitor with IC50 of ∼0.5 μM.
in vitro DEL-22379 inhibits ERK dimerization without affecting its phosphorylation. In a panel of human cell lines harboring mutant BRAF (V600E) or RAS (Q61L or G12V), DEL-22379 shows potent anti-proliferative effects, and induces apoptosis. [1]
in vivo DEL-22379 (15 mg/kg, i.p.) prevents tumor growth and metastasis in mice bearing A375 (BRAF mutant) and HCT116 (KRAS mutant) tumors, but fails to prevent the formation of tumors in mice injected with CHL cells (WT/WT). [1]

プロトコル(参考用のみ)

キナーゼアッセイ ERK dimerization assay
Compound screening is performed in HEK293T cells treated with the potential inhibitors (10 μM) for 30 min before EGF stimulation. Cellular lysates are tested for ERK dimerization by native PAGE and p-ERK evaluation of the potential positives. In vitro ERK dimerization is assayed using GST-MEK1 ΔN EE purified from bacteria, bound to glutathione sepharose beads, and incubated with 25 μg/ml of purified His-ERK2 plus increasing concentrations of DEL-22379. Western blotting, kinase assays, and luciferase assays are also performed. In silico docking of the DEL-22379 compound is carried out with the modeling tools provided by the OpenEye package (v. 2.1).
細胞アッセイ 細胞株 A panel of human cell lines harboring mutant BRAF (V600E) or RAS (Q61L or G12V)
濃度 ~10 μM
反応時間 48 h
実験の流れ Cellular proliferation is analyzed by Alamar blue assays. Briefly, Cells are plated in 96-well plates at a density of 1000-2000 cells per well. Cells are treated with drug concentrations prepared by serial dilution ranging from 0.1 nM to 10 μM. 48 hr after drug treatment cells are exposed to Alamar Blue and the colorimetric change is measured at 570 and 600 nm. GI50 is estimated by nonlinear regression using GraphPad5 Prism Software.
動物実験 動物モデル Nude mice bearing A375 (BRAF mutant), CHL (WT/WT) or HCT116 (KRAS mutant) tumors
投薬量 15 mg/kg, bid
投与方法 i.p.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Epiregulin as an Alternative Ligand for Leptin Receptor Alleviates Glucose Intolerance without Change in Obesity [ Cells, 2022, 11(3)425] PubMed: 35159237
Epiregulin as an Alternative Ligand for Leptin Receptor Alleviates Glucose Intolerance without Change in Obesity [ Cells, 2022, 11(3)425] PubMed: 35159237
ERK phosphorylation disrupts the intramolecular interaction of capicua to promote cytoplasmic translocation of capicua and tumor growth [ Front Mol Biosci, 2022, 9:1030725] PubMed: 36619173
Systems Modeling Identifies Divergent Receptor Tyrosine Kinase Reprogramming to MAPK Pathway Inhibition [Claas AM, et al. Cell Mol Bioeng, 2018, 11(6):451-469] PubMed: 30524510

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。

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