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Rabusertib

Rabusertib

产品编号 T6084   CAS 911222-45-2
别名: LY2603618, IC-83

Rabusertib (IC-83) 是一种有效的选择性的Chk1抑制剂,IC50为 7 nM。它有潜在的化学增强活性,用于各种癌症和肿瘤治疗的试验。

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Rabusertib Chemical Structure
Rabusertib, CAS 911222-45-2
规格 价格/CNY 货期 数量
1 mg ¥ 278 现货
2 mg ¥ 393 现货
5 mg ¥ 659 现货
10 mg ¥ 995 现货
25 mg ¥ 1,930 现货
50 mg ¥ 3,180 现货
100 mg ¥ 4,330 现货
200 mg ¥ 6,170 现货
500 mg ¥ 9,350 现货
1 mL * 10 mM (in DMSO) ¥ 795 现货
产品目录号及名称: Rabusertib (T6084)
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选择批次  
纯度: 99.63%
纯度: 99.40%
纯度: 98.86%
更多批次查询请联系客服
生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Rabusertib (IC-83) is an inhibitor of the cell cycle checkpoint kinase 1 (chk1) with potential chemopotentiating activity. Rabusertib has been used in trials studying the treatment of Cancer, Solid Tumors, Advanced Cancer, Pancreatic Neoplasms, and Non-Small Cell Lung Cancer.
靶点活性 Chk1:7 nM
体外活性 Chk1 is an ATP-dependent serine-threonine kinase and a key component in the DNA replication-monitoring checkpoint system activated by double-stranded breaks (DSBs). Chk1 contributes to all currently defined cell cycle checkpoints, including G1/S, intra-S-phase, G2/M, and the mitotic spindle checkpoint. By inhibiting the activity of chk1, LY2603618 prevents the repair of DNA caused by DNA-damaging agents, thus potentiating the antitumor efficacies of various chemotherapeutic agents. However, preClinicalal data involving LY2603618 has not been published until now. [1] Inhibition of Chk1 is predicted to enhance the effects of antimetabolites, such as gemcitabine. [2] LY2603618 treatment impairs DNA synthesis, increases DNA damage (via mitotic defects), induces apoptosis, and has synergistic activity with pemetrexed, especially in p53 mutant tumor cells. [3]
体内活性 In xenograft models, LY2603618 delays tumor growth when given in combination with pemetrexed. [3]
激酶实验 Protein kinase assays are performed variously. Assays are performed on the following protein kinases: ABL, AKT1, ARG, CAMK2, CDK1, CDK2, CHK1, CHK2, DAPK1, EGFR, EPHA1, EPHB2, EPHB3, EPHB4, ERK1, ERK2, FES, FGFR1, FGFR3, FGFR4, FGR, HCK, HER2, INSR, JNK1, JNK2, LCK, MET, NTRK1, NTRK2, p38α, p38β, p38δ, p38γ, p70S6K, PDGFRα, PDGFRβ, PDK1, PKCα, ROCK2, ROS, RSK2, SGK1, SRC, SYK, TAK1, TYRO3, VEGFR2, VEGFR3, YES, ZAP70[1].
细胞实验 LY2603618 is prepared in DMSO (10 mM) and stock, and then diluted 1000-fold into medium[1]. Cells are plated at 2.5×103 per well, on 96-well tissue culture plates and incubated for one cell doubling (18-24 h). Gemcitabine dilutions are set up by half-log steps across a final concentration range of 1-1000 nM. LY2603618 is prepared by dilutions in DMSO to 5000× final concentration, and then diluted 1000-fold into medium to generate 5× stocks for addition to wells. Approximately 24 h after Gemcitabine addition, LY2603618 is added. Each combination is done in triplicate. After a period of two cell doublings following LY2603618 addition, MTS/PMS reagent is added to each well according to the manufacturer's instructions. Absorbance is read on a Spectra Max 250 spectrophotometer at 490 nm and the data analyzed with GraphPad Prism 4.0. Dose-response curves are fit by non-linear regression, with bottom fits constrained to 0 % inhibition[1].
别名 LY2603618, IC-83
分子量 436.3
分子式 C18H22BrN5O3
CAS No. 911222-45-2

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 11 mg/mL (25.2 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.292 mL 11.46 mL 22.92 mL 57.3 mL
5 mM 0.4584 mL 2.292 mL 4.584 mL 11.46 mL
10 mM 0.2292 mL 1.146 mL 2.292 mL 5.73 mL
20 mM 0.1146 mL 0.573 mL 1.146 mL 2.865 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
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. King C, et al. Invest New Drugs. 2014, 32(2):213-26. 2. Emiliano Calvo1, et al. Mol Cancer Ther, 2011, A94. 3. Govindan R. J Thorac Oncol, 2011, 6(11 Suppl 4), S1757.

文献引用

1. Zhang L, Wirth M, Patra U, et al.Actionable loss of SLF2 drives B‐cell lymphomagenesis and impairs the DNA damage response.EMBO Molecular Medicine.2023: e16431.
BML-277 CCT241533 CHK1-IN-4 CCT245737 SAR-020106 CHIR-124 Baricitinib ANI-7

相关化合物库

该产品包含在如下化合物库中:
抗癌临床化合物库 抗癌药物库 高选择性抑制剂库 抗癌活性化合物库 抗乳腺癌化合物库 抗抑郁症化合物库 糖酵解化合物库 癌细胞分化化合物库 抗癌细胞代谢库 抗胰腺癌化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

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: 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 μL,一共给药动物10 只,您使用的配方为5% 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 μL DMSO (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:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步: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
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Rabusertib 911222-45-2 Autophagy Cell Cycle/Checkpoint PI3K/Akt/mTOR signaling Chk PDK inhibit LY2603618 Inhibitor IC-83 IC 83 Checkpoint Kinase (Chk) LY 2603618 IC83 LY-2603618 inhibitor

 

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