| 產(chǎn)品描述： | THZ2 是一種THZ1的類似物，是 CDK7 的選擇性抑制劑，其IC50值為13.9 nM。THZ2 可有效抑制TNBC細(xì)胞的克隆形成生長(zhǎng)，其IC50值約為10 nM |
| 靶點(diǎn)： |
CDK7(Cell-free assay):13.9 nM;CDK |
| 體外研究： |
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 |
| 體內(nèi)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 |
| 細(xì)胞實(shí)驗(yàn)： |
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. |
| 動(dòng)物實(shí)驗(yàn)： |
Animal Models: Nude mice (Foxn1nu) Dosages: 10 mg/kg Administration: IP |
| 參考文獻(xiàn)： |
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 |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
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 |
|
| 注意： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
上海工商
危險(xiǎn)品化學(xué)品經(jīng)營(yíng)許可證（不帶存儲(chǔ)）
營(yíng)業(yè)執(zhí)照(三證合一)
北京