化合物 COTI2|T4325|TargetMol

COTI-2
1039455-84-9

￥269 1mg 起订

￥378 2mg 起订

￥622 5mg 起订

上海更新日期：2024-12-12

TargetMol中国（陶术生物）

VIP3年

联系人：邵小姐

手机：4008200310 拨打

邮箱：marketing@tsbiochem.com

产品详情:

中文名称：: 化合物 COTI2

英文名称：: COTI-2

CAS号：: 1039455-84-9

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.49%

产品类别：: 抑制剂

货号：: T4325

Product Introduction

Bioactivity

名称	COTI-2
描述	COTI-2, an orally available thiosemicarbazone, is an activator of mutant forms of the p53 protein with potential antineoplastic activity.
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.
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.
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.
体外活性	COTI-2（72小时）显著抑制了所有测试细胞系的增殖速率。在COLO-205、HCT-15和SW620细胞系中，COTI-2显著抑制肿瘤细胞增殖。COTI-2的相对低浓度对所有测试的人类胶质母细胞瘤细胞系（U87-MG、SNB-19、SF-268和SF-295）均有效。在SHP-77细胞中，COTI-2处理的IC50浓度导致40至47%的总细胞发生早期凋亡。
体内活性	在HT-29人类结直肠癌异种移植模型中，COTI-2（10 mg/kg）显著抑制肿瘤生长。不仅在特定治疗后时间点减少肿瘤体积，COTI-2还延长肿瘤达到特定体积的时间。在SHP-77 SCLC异种移植模型中，COTI-2（3 mg/kg）同样显著抑制肿瘤生长。COTI-2能在特定治疗后时间点减少U87-MG肿瘤体积，并延长U87-MG异种移植体在裸鼠体内生长所需的时间。仅用载体处理的对照组小鼠的肿瘤，5天内就达到平均体积828 mm3，而用COTI-2处理的动物肿瘤需要双倍时间（10天）达到类似的平均体积（857 mm3）。无论采用何种给药途径，COTI-2均强效抑制OVCAR-3异种移植体的生长。
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 5 mg/mL (13.64 mM)
关键字	inhibit \| Inhibitor \| HNSCC \| low \| anti-cancer \| anti-proliferative \| toxicity \| TNBC \| COTI-2 \| MDM-2/p53 \| Apoptosis \| orally
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COTI2|||COTI 2|TargetMol

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

成立日期	(12年)
注册资本	566.265100万人民币
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主营行业	天然产物,生化试剂,分子生物学,分子砌块,生物技术服务