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CCT245737

CCT245737

产品编号 T7080   CAS 1489389-18-5
别名: SRA737

CCT245737 (SRA737) 是一种具有口服活性的选择性 Chk1 抑制剂,IC50值为 1.3 nM。

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CCT245737 Chemical Structure
CCT245737, CAS 1489389-18-5
规格 价格/CNY 货期 数量
1 mg ¥ 269 现货
2 mg ¥ 383 现货
5 mg ¥ 628 现货
10 mg ¥ 980 现货
25 mg ¥ 1,930 现货
50 mg ¥ 3,120 现货
100 mg ¥ 4,630 现货
1 mL * 10 mM (in DMSO) ¥ 693 现货
其他形式的 CCT245737:
产品目录号及名称: CCT245737 (T7080)
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选择批次  
纯度: 99.69%
纯度: 99.23%
纯度: 98.06%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 CCT245737 (SRA737) is an orally active and selective Chk1 inhibitor (IC50: 1.3 nM); CCT245737 shows much less activity against Chk2 (IC50: 2440 nM).
靶点活性 Chk1:1.4 nM (Cell-free)
体外活性 CCT245737 (10 μM) shows >80% inhibition of a panel of 124 kinases[1]. CCT245737 abrogates an etoposide-induced G2 checkpoint in HT29, SW620, MiaPaCa-2, and Calu6 cell lines, with IC50s ranging from 30 to 220 nM[2].
体内活性 CCT245737 (150 mg/kg, p.o) alone significantly inhibits tumor growth in an Eμ-Myc mouse model of human B-cell lymphocytic leukemia[2]. CCT245737 (150 mg/kg, p.o.) inhibits tumor growth in combination with gemcitabine (100 mg/kg i.v.) in HT29 colon cancer xenografts. CCT245737 (300 mg/kg, p.o.) also inhibits the gemcitabine (60 mg/kg, i.v.) induced pSer296 CHK1 autophosphorylation at 24 h in SW620 human colon cancer xenografts[1].
激酶实验 Commercial in vitro 33P radiometric kinase assays is carried out against 124 human kinases using 10 μM CCT245737 at ATP concentrations corresponding to the kinase Km, ATP [2].
细胞实验 Cytotoxicity is determined as the drug concentration that gives 50% inhibition of tumour cell proliferation (GI50) using a 96 h Sulforhodamine B (SRB) assay. Inhibition of intracellular CHK1 activity is measured using a cell-based ELISA for the abrogation of an etoposide-induced G2 checkpoint (mitosis induction assay, MIA). The IC50 for G2 checkpoint abrogation (MIA) is determined in the presence of nocodazole using UCN01 as a positive control. The activity index (AI) is used as a measure of the compounds ability to induce mitosis relative to its toxicity (i.e., ratio of MIA IC50: 96 h SRB GI50). Routine potentiation studies are carried out using a fixed concentration (GI50) of either gemcitabine or SN38 in combination with a range of CCT245737 concentrations to determine the combination GI50 of CCT245737. The ability of CCT245737 to enhance gemcitabine or SN38 cell killing is expressed as a potentiation index (PI) equal to the ratio of the GI50 for CCT245737 alone versus the combination GI50 for CCT245737. PI values > 1 indicate the potentiation of the genotoxic activity. In addition, a series of experiments is carried out using fixed, non- or minimally toxic concentrations of CCT245737 (≤GI20) with a range of different concentrations of gemcitabine or SN38 to determine the extent to which CCT245737 enhances drug cytotoxicity compared with the genotoxic agent alone, i.e. conventional PI (ratio GI50 genotoxic alone: GI50 genotoxic combined with non-toxic CCT245737 concentration, Con PI)[2].
动物实验 Human HT29 colorectal carcinoma cells are injected s.c into the flanks of female NCr athymic mice 6-8 weeks of age. Dosing commenced 5 days after transplantation when tumours reach a mean diameter of 5.5 mm. Gemcitabine (100 mg/kg i.v.) is dosed in saline on days 0, 7 and 14 and compounds 4 (CCT245737) and 41 (150 mg/kg p.o.) in 10% DMSO 20% PEG 400, 5% Tween 80, 65% water, 24 and 48 h after each dose of gemcitabine. Tumours are measured and body weights recorded three times weekly. Animals are culled on an individual basis when tumours reach a predetermined humane endpoint (mean diameter <15 mm)[1].
别名 SRA737
分子量 379.34
分子式 C16H16F3N7O
CAS No. 1489389-18-5

存储

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

溶解度

Ethanol: 5 mg/mL

H2O: Insoluble

DMSO: 50 mg/mL (131.81 mM)

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 2.6362 mL 13.1808 mL 26.3616 mL 65.9039 mL
5 mM 0.5272 mL 2.6362 mL 5.2723 mL 13.1808 mL
10 mM 0.2636 mL 1.3181 mL 2.6362 mL 6.5904 mL
20 mM 0.1318 mL 0.659 mL 1.3181 mL 3.2952 mL
50 mM 0.0527 mL 0.2636 mL 0.5272 mL 1.3181 mL
100 mM 0.0264 mL 0.1318 mL 0.2636 mL 0.659 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. Osborne JD, et al. Multiparameter Lead Optimization to Give an Oral Checkpoint Kinase 1 (CHK1) Inhibitor Clinical Candidate: (R)-5-((4-((Morpholin-2-ylmethyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)pyrazine-2-carbonitrile (CCT245737). J Med Chem. 2016 Jun 9;59(11):5221-37. 2. Walton MI, et al. The clinical development candidate CCT245737 is an orally active CHK1 inhibitor with preclinical activity in RAS mutant NSCLC and Eμ-MYC driven B-cell lymphoma. 3. Liang J, Niu Z, Yu X, et al. Counteracting Genome Instability by p53-dependent Mintosis[J]. bioRxiv. 2020. 4. Liang J, Niu Z, Zhang B, et al. Liang J, Niu Z, Zhang B, et al. p53-dependent elimination of aneuploid mitotic offspring by entosis[J]. Cell Death & Differentiation. 2020: 1-15.

文献引用

1. Liang J, Niu Z, Zhang B, et al. p53-dependent elimination of aneuploid mitotic offspring by entosis. Cell Death & Differentiation. 2020: 1-15 2. Liang J, Niu Z, Zhang B, et al Liang J, Niu Z, Zhang B, et al. p53-dependent elimination of aneuploid mitotic offspring by entosis. Cell Death & Differentiation. 2020: 1-15.
SCH900776 (S-isomer) LY2880070 CCT241533 CHK1-IN-4 CCT244747 PD0166285 Prexasertib dihydrochloride Baricitinib

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 高选择性抑制剂库 抗癌药物库 抗癌活性化合物库 抗癌化合物库 表型筛选靶点鉴定库 临床期小分子药物库 NO PAINS 化合物库 激酶抑制剂库 抑制剂库

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
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% 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

CCT245737 1489389-18-5 Cell Cycle/Checkpoint Chk CCT 245737 CCT-245737 SRA-737 Inhibitor inhibit SRA 737 Checkpoint Kinase (Chk) SRA737 inhibitor

 

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