- ￥313 - 8960
- TargetMol
- T2259
- 2026年07月07日
2 年钻石会员
企业认证
相关产品推荐更多 >
万千商家帮你免费找货
0 人在求购买到急需产品
- 详细信息
- 文献和实验
- 技术资料
- CAS号：
1009820-21-6
- 规格：
1mLx10mM(inDMSO)/1mg/2mg/5mg/10mg/25mg/50mg/100mg/500mg
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥713.0 |
|---|---|---|---|
| 规格： | 1mg | 产品价格： | ￥313.0 |
| 规格： | 2mg | 产品价格： | ￥430.0 |
| 规格： | 5mg | 产品价格： | ￥662.0 |
| 规格： | 10mg | 产品价格： | ￥1064.0 |
| 规格： | 25mg | 产品价格： | ￥1984.0 |
| 规格： | 50mg | 产品价格： | ￥3000.0 |
| 规格： | 100mg | 产品价格： | ￥4312.0 |
| 规格： | 500mg | 产品价格： | ￥8960.0 |
Product Introduction
Bioactivity
| 名称 | Silmitasertib |
| 描述 | Silmitasertib (CX-4945) is a potent, orally bioavailable inhibitor of casein kinase 2 (CK2; Ki: 0.38 nM). |
| 细胞实验 | Various cell lines were seeded at a density of 3000 cells per well 24 h prior to treatment, in appropriate media, and then treated with indicated concentrations of CK2 inhibitors. Suspension cells were seeded and treated on the same day. Following 4 days of incubation, 20 μL of Alamar Blue (10% of volume/well) was added and the cells were further incubated at 37 °C for 4-5 h. Fluorescence with excitation wavelength at 530-560 nm and emission wavelength at 590 nm was measured [3]. |
| 激酶实验 | The 238 kinase selectivity panel was conducted using the Kinase Profiler service, which utilizes a radiometric filter-binding assay. The percent inhibition of each kinase was estimated using 0.5 μmol/L CX-4945 at ATP concentrations equivalent to the Km value for ATP for each respective human recombinant kinase. The determination of IC50 values was done at ATP concentrations equivalent to the Km for ATP for each kinase using 9 concentrations of CX-4945 over a range of 0.0001 to 1 μmol/L. The Ki value (inhibition constant) for CX-4945 against recombinant CK2 was determined by graphing the IC50 values of CX-4945 determined in the presence of various concentrations of ATP against the concentration of ATP. The Ki value is equivalent to the Y-intercept according to the Cheng–Prussoff equation (Ki = IC50/(1+[ATP]/Km), where Ki is the inhibition constant and Km is the Michaelis constant [1]. |
| 动物实验 | Xenografts were initiated by subcutaneous injection of BxPC-3 cells into the right hind flank region of each mouse or BT-474 cells were injected into the mammary fat pad of mice implanted with estrogen pellets. When tumors reached a designated volume of 150-200 mm^3, animals were randomized and divided into groups of 9 to 10 mice per group. CX-4945 was administered by oral gavage twice daily at 25 or 75 mg/kg for 31 and 35 consecutive days for the BT-474 and BxPC-3 models, respectively. Tumor volumes and body weights were measured twice weekly. The length and width of the tumor were measured with calipers and the volume calculated using the following formula: tumor volume = (length × width^2)/2. Percent tumor growth inhibition (TGI) values were calculated on the final day of the study for CX-4945–treated compared to vehicle-treated mice and were calculated as 100 × {1 ? [(TreatedFinal day ? TreatedDay 1)/(ControlFinal day ? ControlDay 1)]}. The significance of the differences between the treated versus vehicle groups were determined using 1-way ANOVA [1]. |
| 体外活性 | The antiproliferative activity of Silmitasertib (CX-4945) against cancer cells correlated with expression levels of the CK2α catalytic subunit. CX-4945 caused cell-cycle arrest and selectively induced apoptosis in cancer cells relative to normal cells. In models of angiogenesis, CX-4945 inhibited human umbilical vein endothelial cell migration, tube formation, and blocked CK2-dependent HIF-1α transcription in cancer cells [1]. Adding CX-4945 after bortezomib treatment, prevented leukemic cells from engaging a functional UPR in order to buffer the bortezomib-mediated proteotoxic stress in ER lumen. Bortezomib/CX-4945 treatment inhibited NF-κB signaling in T-ALL cell lines and primary cells from T-ALL patients, but, in B-ALL cells the drug combination activated NF-κB p65 pro-apoptotic functions [2]. CX-4945 was found to potently inhibit endogenous intracellular CK2 activity with an IC50 of 0.1 μM in Jurkat cells. CX-4945 induced dephosphorylation of Akt(S129) and a rapid dephosphorylation of the Akt substrate p21(T145). CX-4945 induced apoptosis in multiple cancer cell lines [3]. |
| 体内活性 | When administered orally in murine xenograft models, CX-4945 was well tolerated and demonstrated robust antitumor activity with concomitant reductions of the mechanism-based biomarker phospho-p21 (T145) [1]. Mice bearing subcutaneous PC3 tumors were treated with CX-4945 (25 mg/kg, 50 mg/kg, and 75 mg/kg, po, bid). Tumor growth inhibition compared to vehicle-treated control, and a dose-responsive efficacy was observed. Last, CX-4945 was well tolerated in mice as assessed by minimal changes in body weight during the course of treatment compared to vehicle control [3]. |
| 存储条件 | Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | H2O : < 1 mg/mL (insoluble or slightly soluble) Ethanol : < 1 mg/mL (insoluble or slightly soluble) DMSO : 17 mg/mL (48.6 mM), Sonication is recommended. |
| 关键字 | Silmitasertib | Inhibitor | inhibit | CX4945 | CX 4945 | CK2 | CaseinKinase | Casein Kinase | Autophagy |
| 相关产品 | Guanidine hydrochloride | Naringin | Enzalutamide | Aceglutamide | Alginic acid | Cysteamine hydrochloride | Hemin | Hydroxychloroquine | Sildenafil citrate | Stavudine | Tamoxifen | Paeonol |
| 相关库 | Inhibitor Library | Bioactive Compound Library | Anti-Cancer Active Compound Library | Bioactive Compounds Library Max | Kinase Inhibitor Library | Anti-Aging Compound Library | Anti-Viral Compound Library | Membrane Protein-targeted Compound Library | Drug Repurposing Compound Library | Anti-Cancer Clinical Compound Library | Target-Focused Phenotypic Screening Library | Anti-Cancer Drug Library |
风险提示：丁香通仅作为第三方平台，为商家信息发布提供平台空间。用户咨询产品时请注意保护个人信息及财产安全，合理判断，谨慎选购商品，商家和用户对交易行为负责。对于医疗器械类产品，请先查证核实企业经营资质和医疗器械产品注册证情况。
文献和实验该产品被引用文献
官网有文献
相关实验
网络 第十九章 杂环化合物和生物碱 杂环化合物在自然界分布很广，其数量几乎占已知有机化合物的三分之一，用途也很多。许多重要的物质如叶绿素、血红素、核酸以及临床应用的一些有显著疗效的天然药物和合成药物等，都含有杂环化合物的结构。生物碱多是中草药的有效成分，绝大多数是含氮的杂环化合物。本章内容与医学关系密切，具有重要意义。
分子中具有高能键的化合物。在生物体内主要有上式（Ⅰ）和（Ⅱ）两种结构的高能化合物。其作用为贮藏能量（例如 ATP、肌酸磷酸）和作为产生 ATP源的中间代谢产物（例如磷酸烯醇丙酮酸）以及合成反应的中间物质（例如酰基辅酶 A），在蛋白质的结构（ conformation）变化周期的第一阶段上（例如钠钾 ATP酶的羧基磷酸中间体）也具有重要作用。多数高等化合物具有磷酸基，但也有例外。
由不同种元素组成的纯净物叫做化合物。化合物一般有固定的组成。化合物的组成一般可用化学式表示。化合物具有确定的物理性质和化学性质，不同于其组成元素的性质。化合物中的元素不能用简单的机械方法或物理方法分开，而必须用化学方法才能分离。
技术资料暂无技术资料 索取技术资料
文献支持
化合物 Silmitasertib【1009820-21-6】
￥313 - 8960
