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- 产品描述： THZ2 是一种THZ1的类似物，是 CDK7 的选择性抑制剂，其IC50值为13.9 nM。THZ2 可有效抑制TNBC细胞的克隆形成生长，其IC50值约为10 nM
- 靶点： CDK7(Cell-free assay):13.9 nM
- 体外研究： 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
- 体内研究： THZ2 is well tolerated in nude mice. The growth rate of tumors in mice treated with THZ2 is markedly reduced as compared to that of control tumors, demonstrating an anti-tumor activity of THZ2. Both acute and chronic exposure to THZ2 significantly reduces CTD phosphorylation of RNAPII at all three phosphorylation sites (S2, S5, and S7), indicating that CDK7 is efficiently targeted in the tumor cells. Compared to vehicle-treated tumors, tumor tissues isolated from mice treated with THZ2 has reduced proliferation and increased apoptosis. THZ2 is able to efficiently reduce tumor cell proliferation and induce cell death in vivo
- 细胞实验： Cell lines: BT549, CAMA1, HCC1187, HCC1569, HCC38, MDAMB-231, MDA-MB-415, MDA-MB-468, T47D, ZR-75-1, HEK293T cells Concentrations: 200 nM, 500 nM Incubation Time: 24 h, 48 h Method: Cell Proliferation Assay: For 96-well plate assay, cells are plated at the density of 2000 cells per well, and on the next day treated with 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.
- 动物实验： Animal Models: Nude mice (Foxn1nu) Dosages: 10 mg/kg Administration: IP
- 参考文献：
1. Yubao Wang, et al. CDK7-dependent transcriptional addiction in triple-negative breast cancer. Cell. 2015 Sep 24;163(1):174-86.
- 溶解性： Soluble in DMSO
- 保存条件： -20℃
- 配置溶液浓度参考：
1mg 5mg 10mg 1 mM 1.767 ml 8.833 ml 17.666 ml 5 mM 0.353 ml 1.767 ml 3.533 ml 10 mM 0.177 ml 0.883 ml 1.767 ml 50 mM 0.035 ml 0.177 ml 0.353 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)
