上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。
THZ2 纯度: 99.62%
THZ2 是有效,选择性的 CDK7 抑制剂,IC50 值为 13.9 nM。
THZ2 Chemical Structure
CAS No. : 1604810-84-5
规格 | 价格 | 是否有货 | 数量 |
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10 mM * 1 mL in DMSO | ¥4110 | In-stock | |
5 mg | ¥3300 | In-stock | |
10 mg | ¥4900 | In-stock | |
50 mg | ¥14000 | In-stock | |
100 mg | 询价 |
* Please select Quantity before adding items.
THZ2 相关产品
•相关化合物库:
- Covalent Screening Library Plus
- Bioactive Compound Library Plus
- Cell Cycle/DNA Damage Compound Library
- Kinase Inhibitor Library
- Anti-Cancer Compound Library
- Anti-Aging Compound Library
- Covalent Screening Library
- Anti-Breast Cancer Compound Library
- Anti-Blood Cancer Compound Library
生物活性 |
THZ2 is a potent and selective CDK7 inhibitor with an IC50 of 13.9 nM. |
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IC50 & Target[1] |
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体外研究 (In Vitro) |
THZ2 selectively targets CDK7 and potently inhibits the growth of triple-negative but not ER/PR+ breast cancer cells. THZ2 at low nanomolar doses also efficiently suppresses the clonogenic growth of TNBC cells with IC50 of appr 10 nM. THZ2 induces apoptotic cell death in triple-negative but not ER/PR+ breast cancer cells or normal human cells[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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体内研究 (In Vivo) |
THZ2 (10 mg/Kg) markedly reduces the growth rate of tumors in mice and demonstrates an anti-tumor activity. Compared to vehicle-treated tumors, tumor tissues isolated from mice treated with THZ2 has reduced proliferation and increased apoptosis, as indicated by immunostaining against Ki67 and cleaved Caspase 3 respectively. THZ2 in NOD-SCID mice leads to reduced body weight, suggesting that THZ2 mayt be less well-tolerated in this particular mouse strain[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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分子量 |
566.05 |
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Formula |
C31H28ClN7O2 |
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CAS 号 |
1604810-84-5 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
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溶解性数据 |
In Vitro:
DMSO : 21.67 mg/mL (38.28 mM; Need ultrasonic) 配制储备液
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
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参考文献 |
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Cell Assay [1] |
For 96-well plate assay, cells are plated at the density of 2000 cells per well, and on the next day treated with THZ1 or THZ2 of various concentrations. After 48-hour incubation, cells are fixed and stained with crystal violet. The staining is then extracted by adding each well with 10% acetic acid, with absorbance measured at 590 nm with 750 nm as a reference. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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Animal Administration [1] |
Mice: Nude mice (CrTac:NCr-Foxn1nu) are γ-irradiated with a single dose of 400 rads six hours before transplantation of cells. Breast cancer cells are harvested and resupended in 40% Matrigel-Basement Membrane Matrix, LDEV-free, and then injected (100 μL per site) into the fourth pair of mammary fat pads of mice. Tumors are measured in two dimensions by using manual calipers. Tumor volume is calculated using the formula: V=0.5× length × width × width. Animal with tumor established (mean tumor volume of appr 200 mm3) are randomLy divided into two groups, which are then treated with vehicle (10% DMSO in D5W, 5% dextrose in water) or THZ2 (3 mg/mL, prepared in vehicle solutions) at the dose of 10 mg/kg intraperitoneally twice daily. Tumor volume is measure every 2-3 days. Upon harvesting tumors, tumors are cut into half, with one half fixed in formalin overnight and then in 70% ethanol for histopathology analysis, and the other half snap frozen in liquid nitrogen for immunoblotting. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
参考文献 |
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