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Silmitasertib

产品编号 T2259Cas号 1009820-21-6
别名 CX-4945, 5-[(3-氯苯基)氨基]-苯并[C]-2,6-萘啶-8-羧酸

Silmitasertib (CX-4945) 是一种可口服的高度选择性 CK2抑制剂,Ki 为 0.38 nM。

Silmitasertib

Silmitasertib

纯度: ≥95%
产品编号 T2259 别名 CX-4945, 5-[(3-氯苯基)氨基]-苯并[C]-2,6-萘啶-8-羧酸Cas号 1009820-21-6

Silmitasertib (CX-4945) 是一种可口服的高度选择性 CK2抑制剂,Ki 为 0.38 nM。

规格价格库存数量
1 mg¥ 372现货
2 mg¥ 538现货
5 mg¥ 828现货
10 mg¥ 1,330现货
25 mg¥ 2,480现货
50 mg¥ 3,750现货
100 mg¥ 5,390现货
500 mg¥ 11,200现货
1 mL x 10 mM (in DMSO)¥ 987现货
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纯度:≥95%
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产品介绍

生物活性
产品描述
Silmitasertib (CX-4945) is a potent, orally bioavailable inhibitor of casein kinase 2 (CK2; Ki: 0.38 nM).
靶点活性
CK2:1 nM (cell free)
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].
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].
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].
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].
别名CX-4945, 5-[(3-氯苯基)氨基]-苯并[C]-2,6-萘啶-8-羧酸
化学信息
分子量349.77
分子式C19H12ClN3O2
CAS No.1009820-21-6
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 50 mg/mL (142.95 mM)
溶液配制表
DMSO
1mg5mg10mg50mg
1 mM2.8590 mL14.2951 mL28.5902 mL142.9511 mL
5 mM0.5718 mL2.8590 mL5.7180 mL28.5902 mL
10 mM0.2859 mL1.4295 mL2.8590 mL14.2951 mL
20 mM0.1430 mL0.7148 mL1.4295 mL7.1476 mL
50 mM0.0572 mL0.2859 mL0.5718 mL2.8590 mL
100 mM0.0286 mL0.1430 mL0.2859 mL1.4295 mL

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
TargetMol | Animal experiments比如您的给药剂量是 10 mg/kg ,每只动物体重 20 g ,给药体积 100 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent DMSO+ 30%PEG300+ 5%Tween 80 + 60% ddH2O. 那么您的工作液浓度为 2 mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
%Tween 80
%ddH2O

剂量转换

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关键词

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