DCLK1-IN-1 NEW
| Price | $232 | $374 | $618 |
| Package | 5mg | 10mg | 25mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-14 |
Product Details
| Product Name: DCLK1-IN-1 | CAS No.: 2222635-15-4 |
| Purity: 99.28% | Supply Ability: 10g |
| Release date: 2024/11/14 |
Product Introduction
Bioactivity
| 名稱(chēng) | DCLK1-IN-1 |
| 描述 | DCLK1-IN-1 is a selective, in vivo compatible chemical probe of the kinase domain of doublecortin-like kinase 1 (DCLK1) and a highly selective DCLK1/2 inhibitor with IC50 values ??of 9.5/57.2 nM (DCLK1) and 31/103 nM (DCLK2) by binding and kinase assays, respectively. It has low toxicity and is used to study DCLK1 biology and determine its role in cancer. |
| 體外活性 | METHODS: A NanoBRET tracer (TAE684-NanoBRET-590) was synthesized and a DCLK1 NanoBRET assay was developed to measure the effect of DCLK1-IN-1 on cell proliferation in HCT116 cells. RESULTS The IC50 value of DCLK1-IN-1 against HCT116 cells was 279nM. [1] METHODS: ACHN, 786-O, and CAKI-1 RCC cells were treated with DCLK1-IN-1 (0.5, 1, 5, 10 μM) and subjected to wound healing assays. RESULTS DCLK1-IN-1 exerted a significant anti-migratory effect on ACHN, 786-O, and CAKI-1 RCC cells, with ACHN and CAKI-1 cells showing a typical dose-dependent decrease in wound healing from 0.5 to 10 μM, while 786-O cells showed a significant decrease at a dose of 10 μM. [2] |
| 體內(nèi)活性 | DCLK1-IN-1 (3 mg/kg, intravenous injection; 10 mg/kg, oral administration) has good pharmacokinetic characteristics in mice, with a half-life of 2.09 hours, an area under the curve (AUCinf) of 5506 hr*ng/mL, and an oral bioavailability of 81%. [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 | 2% DMSO+40% PEG300+5% Tween 80+53% Saline : 1 mg/mL, Sonication is recommended.Working solution is recommended to be prepared and used immediately. DMSO : 50 mg/mL (94.78 mM), Sonication is recommended. |
| 關(guān)鍵字 | DCLK1 IN 1 | DCLK1-IN-1 | signaling | PDAC | KRAS | cancer | low | ERK | Inhibitor | selective | DCLK1IN1 | inhibit | DCLK-1-IN-1 | toxicity |
| 相關(guān)庫(kù) | 經(jīng)典已知活性庫(kù) | 激酶抑制劑庫(kù) | NO PAINS 化合物庫(kù) | 已知活性化合物庫(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
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