價格 | ¥266 | ¥378 | ¥619 |
包裝 | 1mg | 2mg | 5mg |
最小起訂量 | 1mg |
發(fā)貨地 | 上海 |
更新日期 | 2024-09-29 |
中文名稱:化合物 DEL22379 | 英文名稱:DEL-22379 |
CAS:181223-80-3 | 品牌: TargetMol |
產(chǎn)地: 美國 | 保存條件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
純度規(guī)格: 99.53% | 產(chǎn)品類別: 抑制劑 |
貨號: T6818 |
名稱 | DEL-22379 |
描述 | DEL-22379 is a water-soluble ERK dimerization inhibitor with IC50 of ~0.5 μM. |
細胞實驗 | 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.(Only for Reference) |
激酶實驗 | 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). |
體外活性 | DEL-22379抑制了ERK二聚體的形成,但不影響其磷酸化。在攜帶突變BRAF (V600E)或RAS (Q61L或G12V)的人類細胞系中,DEL-22379顯示出強大的抗增殖效果,并誘導(dǎo)凋亡。[1] |
體內(nèi)活性 | DEL-22379(15 mg/kg,i.p.)在攜帶A375(BRAF突變)和HCT116(KRAS突變)腫瘤的小鼠中阻止了腫瘤生長和轉(zhuǎn)移,但未能阻止注射CHL細胞(WT/WT)的小鼠中腫瘤的形成。[1] |
存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 22.2 mg/mL (50 mM) |
關(guān)鍵字 | ERK | Inhibitor | Extracellular signal regulated kinases | inhibit | DEL 22379 | DEL-22379 | Apoptosis |
相關(guān)產(chǎn)品 | Lidocaine hydrochloride | Metronidazole | 5-Fluorouracil | Stavudine | Tributyrin | Dextran sulfate sodium salt (MW 4500-5500) | Myricetin | Sorafenib | L-Ascorbic acid | Acetylcysteine | Sodium 4-phenylbutyrate | Kaempferol |
相關(guān)庫 | 抑制劑庫 | 經(jīng)典已知活性庫 | 已知活性化合物庫 | 激酶抑制劑庫 | MAPK 抑制劑庫 | 抗衰老化合物庫 | 谷氨酰胺代謝化合物庫 | 抗COVID-19化合物庫 | 疼痛相關(guān)化合物庫 | 表型篩選靶點鑒定庫 |
成立日期 | 2013-04-18 (12年) | 注冊資本 | 566.265100萬人民幣 |
員工人數(shù) | 100-500人 | 年營業(yè)額 | ¥ 1億以上 |
主營行業(yè) | 天然產(chǎn)物,生化試劑,分子生物學(xué),分子砌塊,生物技術(shù)服務(wù) | 經(jīng)營模式 | 貿(mào)易,工廠,試劑,定制,服務(wù) |
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