| 产品描述: | NAB-14 is a potent, selective, orally active and non-competitive GluN2C/2D antagonists with an IC50 of 580 nM for GluN1/GluN2D. NAB-14 shows >800-fold selective for recombinant GluN2C and GluN2D over GluN2A and GluN2B. NAB-14 can cross the blood-brain-barrier. |
| 靶点: |
CDK6:9.9 nM (IC50); CDK4:12.4 nM (IC50) |
| 体外研究: |
Dalpiciclib hydrochloride (oral gavage; 150 mg/kg; once weekly; 3 weeks) shows antitumor activity against ESCC xenografts. Dalpiciclib hydrochloride combined with Paclitaxel (PTX) or Cisplatin (CDDP) offer synergistic inhibitory effects in ESCC xenografts. Dalpiciclib hydrochloride (oral gavage; 37.5 mg/kg, 75 mg/kg, 150 mg/kg; once daily; 30 days) shows antitumor activity in human xenograft models . |
| 体内研究: |
NAB-14 (compound 14) shows inhibition with IC50s of 15 µM and 5.1 µM for GluN1/2AC1/2CC2 and GluN1/2AC1/2CC2 receptors, respectively. NAB-14 (20 µM; 24 h) inhibits native GluN2D-containing receptors in brain slices with no effect on native GluN2A- or GluN2B-containing NMDARs in cultures cortical neurons. NAB-14 (10 µM) reduces the peak amplitude of evoked EPSCs to 55 ± 3.0%, and significantly reduced the τW of EPSC deactivation. NAB-14 (10 µM) decreases the peak amplitude and charge transfer of interneuron EPSCs to 59 ± 9.9% and 63 ± 9.7%, respectively. And NAB-14 decreases τW for interneuron EPSCs from 150 ± 12 ms to 101 ± 14 ms. |
| 参考文献: |
1. Jose Manuel Perez-Garcia, et al. Perez-Garcia JM, Cortes J, Llombart-Cussac A. CDK4/6 inhibitors in breast cancer: spotting the difference. Nat Med. 2021 Nov;27(11):1868-1869. 2. Pin Zhang, et al. A phase 1 study of dalpiciclib, a cyclin-dependent kinase 4/6 inhibitor in Chinese patients with advanced breast cancer. Biomark Res. 2021 Apr 12;9(1):24. 3. Jiayuan Wang, et al. CDK4/6 inhibitor-SHR6390 exerts potent antitumor activity in esophageal squamous cell carcinoma by inhibiting phosphorylated Rb and inducing G1 cell cycle arrest. J Transl Med. 2017 Jun 2;15(1):127. 4. Fei Long, et al. Preclinical characterization of SHR6390, a novel CDK 4/6 inhibitor, in vitro and in human tumor xenograft models. Cancer Sci. 2019 Apr;110(4):1420-1430. |
| 保存条件: |
-80°C 12个月; -20°C 6个月, 干燥 |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.07 ml |
10.352 ml |
20.704 ml |
| 5 mM |
0.414 ml |
2.07 ml |
4.141 ml |
| 10 mM |
0.207 ml |
1.035 ml |
2.07 ml |
| 50 mM |
0.041 ml |
0.207 ml |
0.414 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |