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COTI-2

产品编号 T4325 CAS 1039455-84-9

别名: COTI 2, COTI2

COTI-2是一种具有口服活性的低毒性抗癌药物，是 p53 突变体激活剂。它通过激活突变型 p53 和抑制PI3K/AKT/mTOR 途径发挥作用，通过 p53 依赖和非依赖机制在 HNSCC 中具有抗肿瘤活性。它诱导多种人肿瘤细胞凋亡，可将突变型 p53 转化为野生型构象。

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COTI-2, CAS 1039455-84-9

规格	价格/CNY	货期
1 mg	￥ 269	现货
2 mg	￥ 378	现货
5 mg	￥ 622	现货
10 mg	￥ 987	现货
25 mg	￥ 1,950	现货
50 mg	￥ 2,890	现货
100 mg	￥ 4,330	现货
500 mg	￥ 9,360	现货
1 mL * 10 mM (in DMSO)	￥ 683	现货

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纯度: 99.49%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	COTI-2, an orally available thiosemicarbazone, is an activator of mutant forms of the p53 protein with potential antineoplastic activity.
体外活性	COTI-2 (72 h) potently inhibits the proliferation rate of all the tested cell lines. In COLO-205, HCT-15, and SW620 cell lines, COTI-2 markedly inhibits tumor cell proliferation. Relatively low concentrations of COTI-2 are active against all human glioblastoma cell lines tested (U87-MG, SNB-19, SF-268, and SF-295). In SHP-77 cells, COTI-2 treatment with IC50 concentrations causes the induction of early apoptosis among 40 to 47% of total cells.
体内活性	In the HT-29 human colorectal tumor xenografts, COTI-2 (10 mg/kg) markedly inhibits tumor growth. Except for reducing tumor volumes at specific times post-treatment, COTI-2 also increases the time required for tumors to reach specified volumes. In the SHP-77 SCLC xenograft model, COTI-2 (3 mg/kg) also markedly inhibits tumor growth. COTI-2 can reduce U87-MG tumor volumes at specific times post-treatment and lengthen the time required for U87-MG xenografts to grow in nude mice. Control tumors in mice treated with vehicle alone take only 5 days to reach an average volume of 828 mm3 while tumors in animals treated with COTI-2 take double that time (10 days) to reach a similar mean volume (857 mm3). Regardless of the route of administration, COTI-2 potently inhibits OVCAR-3 xenograft growth.
激酶实验	The interaction of COTI-2 with 227 kinases is tested using the AMBIT BIOSCIENCES KINOMESCAN assay. In brief, streptavidin-coated magnetic beads are treated with biotinylated small molecule ligands for 30 min at 25°C to generate affinity resins for kinase assays. The liganded beads are blocked with excess biotin and washed with blocking buffer (1% BSA, 0.05% Tween 20, 1 mM DTT) to remove unbound ligand and to reduce non-specific binding. Binding reactions are assembled by combining phage lysates, liganded affinity beads, and COTI-2 in 1× binding buffer (20% SeaBlock, 0.17× PBS, 0.05% Tween 20, 6 mM DTT). All reactions are carried out in polystyrene 96-well plates that have been pre-treated with blocking buffer in a final volume of 0.1 mL.
细胞实验	COTI-2 is dissolved in 100% dimethyl sulfoxide stock solution and diluted in medium plus FBS such that final DMSO concentrations are 0.5 to 1.0% depending on the experiment.SHP-77 cells are cultured with various concentrations of COTI-2 for 48 h. Cells are then washed twice with 1× cold PBS and stained with Annexin V and 7AAD according to the manufacturer's instructions. Briefly, 5 μL of Annexin V and 7AAD are added to 1×105 cells and incubated for 15 min at room temperature in the dark. Then 400 μL of the 1× binding buffer (100 mM HEPES, pH 7.4, 140 mM NaCl, 2.5 mM CaCl2) is added to the cells. Finally, cells are analyzed using a flow cytometer.
动物实验	SHP-77 and HT-29 cells are injected in 50% matrigel into flanks of NCr-nu mice (2×106 cells per injection site) (n=5 mice per group). In the case of SHP-77 xenografts, treatment with COTI-2 begins prior to the appearance of palpable tumors. One day after injection of SHP-77 cells, animals receive 3 mg/kg of COTI-2 (once every two days, up to 38 days). Tumor sizes are estimated at 5, 10, 17, 24, and 38 days, by standard caliper measurements. In the case of HT-29 xenografts, the capacity of COTI-2 to suppress the growth of established tumors is assessed. HT-29 xenografts are allowed to grow to 200 mm3 before starting IP treatment with COTI-2 (10 mg/kg, 5 days a week for 7 weeks) or saline IP. Tumor growth is measured every 4 days by caliper measurement.

别名	COTI 2, COTI2
分子量	366.48
分子式	C19H22N6S
CAS No.	1039455-84-9

存储

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

溶解度

DMSO: 5 mg/mL (13.64 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	2.7287 mL	13.6433 mL	27.2866 mL	68.2165 mL
	5 mM	0.5457 mL	2.7287 mL	5.4573 mL	13.6433 mL
	10 mM	0.2729 mL	1.3643 mL	2.7287 mL	6.8217 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

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

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参考文献

1. Bykov VJN,etal.Targeting mutant p53 for efficient cancer therapy.Nat Rev Cancer. 2018 Feb;18(2):89-102. 2. Salim KY,etal.COTI-2, a novel small molecule that is active against multiple human cancer cell lines in vitro and in vivo.Oncotarget. 2016 Jul 5;7(27):41363-41379. 3. Duffy MJ, et al. Mutant p53 as a target for cancer treatment. Eur J Cancer. 2017 Sep;83:258-265.

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

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

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 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 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

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

COTI-2 1039455-84-9 Apoptosis p53 COTI 2 inhibit Inhibitor HNSCC COTI2 low anti-cancer anti-proliferative toxicity TNBC MDM-2/p53 orally inhibitor

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COTI-2

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords