| 產(chǎn)品描述： | Palbociclib (PD 0332991) isethionate is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib isethionate has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma |
| 靶點(diǎn)： |
Cdk4/cyclin D3:9 nM (IC50);Cdk4/cyclin D1:11 nM (IC50);Cdk6/cyclin D2:16 nM (IC50);DYRK1A:2000 nM (IC50);MAPK:8000 nM (IC50);CDK |
| 體內(nèi)研究： |
Palbociclib isethionate (oral adminstration, 75 or 150 mg/kg, daily for 14 days) produces rapid tumor regressions and delays tumor growth. Palbociclib isethionate (oral adminstration, 90 mg/kg, daily for 12 days) reduces Treg numbers and the Treg:CD8 ratio in the spleen and lymph nodes in tumor-free mice, demonstrating the tumor-independent effects. Palbociclib isethionate (oral administration, 100 mg/kg, daily for 1 week) has potent antitumour effects in genetically engineered mosaic mouse model of liver cancer. |
| 參考文獻(xiàn)： |
1. Fry DW, et al. Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts. Mol Cancer Ther. 2004 Nov;3(11):1427-38. 2. Goel S, et al. CDK4/6 inhibition triggers anti-tumour immunity. Nature. 2017 Aug 24;548(7668):471-475. 3. Richard S Finn, et al. PD 0332991, a selective cyclin D kinase 4/6 inhibitor, preferentially inhibits proliferation of luminal estrogen receptor-positive human breast cancer cell lines in vitro. Breast Cancer Res. 2009;11(5):R77. 4. Bollard J, et al. Palbociclib (PD-0332991), a selective CDK4/6 inhibitor, restricts tumour growth in preclinical models of hepatocellular carcinoma. Gut. 2017 Jul;66(7):1286-1296. |
| 溶解性： |
H2O : 50 mg/mL (87.16 mM; Need ultrasonic) DMSO : 10 mg/mL (17.43 mM; Need ultrasonic) |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.743 ml |
8.716 ml |
17.432 ml |
| 5 mM |
0.349 ml |
1.743 ml |
3.486 ml |
| 10 mM |
0.174 ml |
0.872 ml |
1.743 ml |
| 50 mM |
0.035 ml |
0.174 ml |
0.349 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。 |
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