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Dalpiciclib hydrochloride

    
10mM in DMSO

源叶(MedMol)
V58255 一键复制产品信息
2891598-76-6
C25H31ClN6O2
483.01
货号 规格 价格 上海 北京 珠海 重庆 武汉 购买数量
V58255-1ml
10mM in DMSO

¥4030.00

货期:3-5天 - - - -
产品介绍 参考文献 质检证书(COA) 摩尔浓度计算器 相关产品
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
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