Ceralasertib NEW
| Price | $43 | $97 | $148 |
| Package | 1mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-17 |
Product Details
| Product Name: Ceralasertib | CAS No.: 1352226-88-0 |
| Purity: 99.99% | Supply Ability: 10g |
| Release date: 2024/11/17 |
Product Introduction
Bioactivity
| 名稱 | Ceralasertib |
| 描述 | Ceralasertib (AZD6738) is an orally active, selective ATR kinase inhibitor with an IC50 of 1 nM. |
| 細胞實驗 | Cells are treated in white walled, clear bottom 96-well plates with the indicated doses of AZD6738, cisplatin, gemcitabine, or combination for 48 h. ATP levels are assessed as surrogate measure of viability was assessed using the CellTiter-Glo Luminescent Cell Viability Assay and Safire 2 plate reader. Raw data are corrected for background luminescence prior to further analysis. For AZD6738 treatment, log dose response curves are generated in GraphPad Prism 6 by nonlinear regression (log(inhibitor) vs. response with variable slope) of log-transformed (x = log(x)) data normalized to the mean of untreated controls. GI values, defined as the dose X at which Y = 50%, were extrapolated from dose response curves. |
| 激酶實驗 | General procedure for the EC50 test: DDR1 is induced by 2 Gg/ml doxycycline for 48 hrs prior to DDR1 activation by rat tail collagen I. The DDR1 over-expressed U2OS is pre-treated by media containing each concentration of the compound for 1 hr and treated by changing the media to the EC50 test media containing 10 Gg/ml collagen and each concentration of the compound for 2 hrs. Each cells is washed with cold PBS three times and lysed with the lysis buffer (50 mMTris, pH 7.5, 1% Triton X-100, 0.1% SDS, 150 mM NaCl, 5 mM EDTA, 100 mMNaF, 2 mM Na3VO4, 1 mM PMSF, 10 Gg/ml aprotinin, and 10 Gg/ml leupeptin). The activation of DDR1 is quantified by density using program ImageJ to determine EC50 following Western blot using anti-activated human DDR1b (Y513). |
| 體外活性 | METHODS: 276 different tumor cell lines were treated with Ceralasertib for 3 days and cell viability was measured by MTS assay. RESULTS: For most cell lines, the median GI50 for 50% growth inhibition (1.47 μmol/L) was higher than the IC90 for ATR cells, with only 13% of the cell lines having a GI50 below the median, and 30% below 1 μmol/L. Hematological cell lines (median GI50= 0.82 μmol/L) generally showed increased sensitivity compared to solid tumor cells (median GI50= 1.68 μmol/L). [1] METHODS: Colorectal cancer cells HT29 were treated with trifluridine (70 μM) and Ceralasertib (0.5 μM) for 48 h, and the expression levels of target proteins were measured by Western Blot. RESULTS: The trifluridine+Ceralasertib group inhibited Chk1 phosphorylation in HT29 cells at 48 h compared to the trifluridine group. Therefore, it was confirmed that Ceralasertib inhibited Chk1 phosphorylation. In HT29 and HCT116 cells, DNA damage was more severe in the trifluridine+Ceralasertib group than in the trifluridine group, which could be confirmed by the increased level of γH2A expression. [2] |
| 體內活性 | METHODS: To assay anti-tumor activity in vivo, Ceralasertib (10-50 mg/kg, 10% DMSO+40% Propylene Glycol+50% deionized water) was orally administered to LoVo, Granta-519, NCI-H23, or 549 xenograft-carrying athymic nude mice bearing LoVo, Granta-519, NCI-H23 or 549 xenografts once daily for 14-28 days. RESULTS: LoVo and Granta-519 showed dose-dependent efficacy, with significant TGI at 50 mg/kg, moderate activity at 25 mg/kg, and no activity at 10 mg/kg. Significant antitumor activity was also observed in NCI-H23 but not in A549 model. [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 | H2O : < 1 mg/mL (insoluble or slightly soluble) Ethanol : 39 mg/mL (94.5 mM) 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 7.6 mg/mL (18.42 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. DMSO : 55 mg/mL (133.33 mM) |
| 關鍵字 | ATM/ATR | inhibit | Ataxia telangiectasia mutated | Ceralasertib | ATM and RAD3 related | Inhibitor | AZD 6738 | AZD-6738 |
| 相關產品 | CP-466722 | Ro 90-7501 | AZ31 | Dactolisib | Berzosertib | Elimusertib | GJ103 sodium salt | KU60019 | (Z)-Mirin | NU6027 | Schisandrin B | AZ32 |
| 相關庫 | 抗結直腸癌化合物庫 | 經典已知活性庫 | 激酶抑制劑庫 | 抗癌臨床化合物庫 | 藥物功能重定位化合物庫 | 抑制劑庫 | 抗衰老化合物庫 | 已知活性化合物庫 | 抗癌藥物庫 | 抗癌活性化合物庫 |
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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