化合物 THZ2|T7296|TargetMol

THZ2
1604810-84-5

￥713 1mg 起订

￥2190 5mg 起订

￥3270 10mg 起订

上海更新日期：2024-12-12

TargetMol中国（陶术生物）

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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 THZ2

英文名称：: THZ2

CAS号：: 1604810-84-5

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：: 98%

产品类别：: 抑制剂

货号：: T7296

Product Introduction

Bioactivity

名称	THZ2
描述	THZ2 (CDK7-IN-1), an analog of THZ1, is a potent and selective CDK7 inhibitor(IC50:13.9 nM),with the potential to treat Triple-negative breast cancer (TNBC).
细胞实验	Cells were firstly seeded into a 96-well plate at a density of 3000 cells per well, and incubated with THZ2 in three parallel wells for 72 h. Then MTT was added to each well at a final concentration of 0.5 mg/ml. After incubation for 4 h, formazan crystals were dissolved in 100 μl of DMSO, and absorbance at 570 nm was measured by plate reader. The concentrations required to inhibit growth by 50% (IC50) were calculated from survival curves using the Bliss method[1].
动物实验	Balb/c nude mice feed on sterilized food and water. Six female nude mice with 5 weeks old were used for two groups. Each mouse was injected subcutaneously with BGC-823 cells (3 × 10^6 in 100 μl of medium) under the shoulder. When the subcutaneous tumors were approximately 0.3 × 0.3 cm^2 (two perpendicular diameters) in size, mice were randomized into two groups, and were injected intraperitoneally with vehicle alone (0.9% saline) and THZ2 (10 mg/kg) once/day at first 16 days and twice/day at last 6 days. The body weights of mice and the two perpendicular diameters (A and B) of tumors were recorded. The tumor volume (V) was calculated according to the formula: V = (π/6) × [(A+B)/2]^3. The mice were anaesthetized after experiment, and tumor tissue was excised from the mice and weight. The rate of inhibition (IR) was calculated according to the formula: IR = [1 - (Mean tumor weight of experimental group/Mean tumor weight of control group)] × 100%[1].
体外活性	在THZ2处理后，六种细胞系的存活率均呈剂量依赖性下降。GES-1细胞对THZ2最不敏感，其IC50值最高，为2.45 μM。THZ2在AGS、BGC-823、MGC-803、MKN-45及SGC-7901细胞中的IC50值分别为0.19 μM、0.69 μM、0.74 μM、0.73 μM及0.68 μM，这些值与这些细胞中CDK7蛋白表达量正相关[1]。
体内活性	通过将BGC-823细胞移植入裸鼠中，建立了异种移植瘤模型。与对照组相比，THZ2处理显著抑制了BGC-823肿瘤的生长，体现在肿瘤体积和重量的显著减少，但裸鼠的体重未见变化。THZ2处理组的肿瘤生长抑制率为44.00%[1]。
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 : 39 mg/mL (68.90 mM)
关键字	inhibit \| THZ 2 \| THZ2 \| Cyclin dependent kinase \| THZ-2 \| CDK \| Inhibitor
相关产品	Sodium Oxamate \| Ribociclib \| Palbociclib monohydrochloride \| Abemaciclib methanesulfonate \| CASIN \| Olomoucine \| Palbociclib \| GW 441756 \| Dinaciclib \| Ro-3306 \| GSK 3 Inhibitor IX \| Abemaciclib
相关库	抑制剂库 \| 抗乳腺癌化合物库 \| 经典已知活性库 \| 抗癌活性化合物库 \| 已知活性化合物库 \| 细胞周期化合物库 \| 抗胰腺癌化合物库 \| 激酶抑制剂库 \| 抗衰老化合物库 \| 共价抑制剂库

CDK7-IN-1|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。

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