CL-387785 NEW
| Price | $33 | $53 | $107 |
| Package | 5mg | 10mg | 25mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-14 |
Product Details
| Product Name: CL-387785 | CAS No.: 194423-06-8 |
| Purity: 98.09% | Supply Ability: 10g |
| Release date: 2024/11/14 |
Product Introduction
Bioactivity
| 名稱 | CL-387785 |
| 描述 | CL-387785 (WAY-EKI 785)(EKI785; WAY-EKI 785) is an irreversible inhibitor of EGFR(IC50： 370+/-120 pM); is able to overcome resistance caused by the T790M mutation on a functional level. |
| 細(xì)胞實(shí)驗(yàn) | MTS assays are performed with the CellTiter 96@ AQueous One solution proliferation kit. A total of 10,000 cells per well in 96-well ?at-bottomed plates are incubated with various concentrations of inhibitors for 48 h. The IC50 is determined from dose–response curves using XL?t4.(Only for Reference) |
| 激酶實(shí)驗(yàn) | Liquid scintillation: Stock solutions of 500 μM CL-387785 (prepared in 100% DMSO) are diluted to the desired concentration with 30 mM HEPES, pH 7.4. Ten microliters of CL-387785 at various concentrations are incubated with 3 μL of recombinant enzyme (1:120 dilution in 100 mM HEPES, pH 7.4) on ice for 10 min. Then, 5 μL peptide (400 μM final concentration of RR-SRC composed of Arg-Arg-Leu-Ile-Glu-Asp-Ala-Glu-Tyr-Ala-Ala-Arg-Gly), 10 μL of 4× reaction buffer containing 50 mM HEPES, pH 7.4, 80 μM ATP, 40 mM MnCl2, and 200 μM sodium orthovanadate. 0.30 μL [33P]ATP ( >2500 Ci/mmol), and 12 μL Water are added. After incubation for 90 min at room temperature, the entire volume is spotted onto precut P81 filter papers. The filter discs are washed two times with 0.5% phosphoric acid, and radioactivity is measured using a liquid scintillation counter. Under these conditions, the specific activity of EGF-R kinase is approximately 0.50 pmol/mg/min. |
| 體外活性 | CL-387785 demonstrates significant inhibitory effects on the growth of HCT-116-induced xenograft tumors at a dose of 50 mg/kg. In nude mice expressing EGF-R, CL-387785 administered orally at 80 mg/kg/day effectively suppresses tumor growth. In a mouse model of autosomal recessive polycystic kidney disease, treatment with CL-387785 at 90 mg/kg intraperitoneally in Balb/c-bpk/bpk (BPK) mice significantly reduces cystic lesions in collecting ducts, improves kidney function, decreases abnormalities in bile duct epithelial cells, and extends lifespan. At 25 mg/kg, CL-387785 can reduce the growth of HCA-7-induced xenograft tumors, and a dose of 100 mg/kg completely inhibits tumor growth. |
| 體內(nèi)活性 | CL-387785 effectively blocks EGF-mediated receptor autophosphorylation in cells (IC50: 5 nM). It principally acts as a cellular inhibitor, suppressing cell proliferation in cell lines overexpressing EGF-R or c-erbB-2 (IC50: 31 nM). |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 60 mg/mL (157.39 mM), Sonication is recommended. Ethanol : < 1 mg/mL (insoluble or slightly soluble) H2O : < 1 mg/mL (insoluble or slightly soluble) |
| 關(guān)鍵字 | EKI785 | ErbB-1 | HER1 | CL 387785 | EGFR | WAY-EKI-785 | WAY-EKI785 | CL387785 | inhibit | Inhibitor | EKI 785 | Epidermal growth factor receptor | CL-387785 |
| 相關(guān)產(chǎn)品 | Osimertinib | Lidocaine Hydrochloride hydrate | Lapatinib | Afatinib Dimaleate | Erlotinib hydrochloride | Erlotinib | Neratinib | Chalcone | Osimertinib mesylate | Genistein | Khellin | Gefitinib |
| 相關(guān)庫(kù) | 高選擇性抑制劑庫(kù) | 經(jīng)典已知活性庫(kù) | 膜蛋白靶向化合物庫(kù) | 激酶抑制劑庫(kù) | 酪氨酸激酶分子庫(kù) | 抗卵巢癌化合物庫(kù) | 抑制劑庫(kù) | 已知活性化合物庫(kù) | 臨床前化合物庫(kù) | 抗癌活性化合物庫(kù) |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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United States- Since: 2011-01-07
- Address: 36?Washington?Street, Wellesley?Hills
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