SAR-020106 NEW
| Price | $44 | $97 | $172 |
| Package | 1mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-11 |
Product Details
| Product Name: SAR-020106 | CAS No.: 1184843-57-9 |
| Purity: 97.78% | Supply Ability: 10g |
| Release date: 2024/11/11 |
Product Introduction
Bioactivity
| 名稱 | SAR-020106 |
| 描述 | SAR-020106 is a potent, ATP-competitive, and selective CHK1 inhibitor with an IC50 of 13.3 nmol/L on the isolated human enzyme. |
| 體外活性 | SAR-020106 potentiated the efficacies of irinotecan and gemcitabine in SW620 human colon carcinoma xenografts in nude mice[2] |
| 體內(nèi)活性 | SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC(50) of 13.3 nmol/L on the isolated human enzyme. This compound abrogates an etoposide-induced G(2) arrest with an IC(50) of 55 nmol/L in HT29 cells, and significantly enhances the cell killing of gemcitabine and SN38 by 3.0- to 29-fold in several colon tumor lines in vitro and in a p53-dependent fashion. Biomarker studies have shown that SAR-020106 inhibits cytotoxic drug-induced autophosphorylation of CHK1 at S296 and blocks the phosphorylation of CDK1 at Y15 in a dose-dependent fashion both in vitro and in vivo. Cytotoxic drug combinations were associated with increased gammaH2AX and poly ADP ribose polymerase cleavage consistent with the SAR-020106-enhanced DNA damage and tumor cell death. Irinotecan and gemcitabine antitumor activity was enhanced by SAR-020106 in vivo with minimal toxicity. SAR-020106 represents a novel class of CHK1 inhibitors that can enhance antitumor activity with selected anticancer drugs in vivo and may therefore have clinical utility[1]. |
| 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 : 12 mg/mL (31.34 mM) |
| 關(guān)鍵字 | SAR020106 | cycle | SN38 | selectivity | SW620 | cancer | inhibit | colon | cells | SAR-020106 | SAR 020106 | Checkpoint Kinase (Chk) | antitumor | arrest | Inhibitor |
| 相關(guān)產(chǎn)品 | Rabusertib | CCT245737 | BML-277 | Prexasertib | PD0166285 | CHK1-IN-3 | CHK1-IN-4 hydrochloride | A-443654 | Prexasertib dihydrochloride | BX795 | ANI-7 | Baricitinib |
| 相關(guān)庫(kù) | 經(jīng)典已知活性庫(kù) | 激酶抑制劑庫(kù) | 抑制劑庫(kù) | NO PAINS 化合物庫(kù) | 已知活性化合物庫(kù) | 細(xì)胞周期化合物庫(kù) | 抗癌化合物庫(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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