中文名 | NVP-BHG712 isomer |
英文名 | 4-methyl-3-((2-methyl-6-(pyridin-3-yl)-2H-pyrazolo[3,4-d]pyrimidin-4-yl)amino)-N-(3-(trifluoromethyl)phenyl)benzamide |
别名 | 化合物NVP-BHG712 ISOMER |
英文别名 | NVP-BHG712 isomer 4-methyl-3-((2-methyl-6-(pyridin-3-yl)-2H-pyrazolo[3,4-d]pyrimidin-4-yl)amino)-N-(3-(trifluoromethyl)phenyl)benzamide |
CAS | 2245892-85-5 |
化学式 | C26H20F3N7O |
分子量 | 503.48 |
溶解度 | DMSO : 25 mg/mL母液保存:分装冻存,避免反复冻融;-20℃,1个月;-80℃,6个月(稀释后溶液温度低保存可能会析出,尽量现用现配)细胞实验:先用DMSO溶解:再用培养基进行稀释,稀释过程建议分段进行,避免浓度变化过快导致化合物析出。若稀释过程中出现化合物析出的情况, 可采用超声的方法使其复溶。在稀释时要确保工作液中 DMSO 的终浓度尽量在0.1%以下,最高不要超过0.5%,并设置相应浓度的DMSO对照组。动物实验:先用DMSO溶解:再用水或者生理盐水等去稀释,稀释过程建议分段进行,避免浓度变化过快导致化合物析出。若稀释过程中出现化合物析出的情况, 可采用超声的方法使其复溶。可以通过添加助溶剂来帮助溶解,比如植物油、Tween80、甘油、羧甲基纤维素钠和PEG400等。具体方式请参考文献。悬浊液可用于口服和腹腔注射,不会影响产品活性。 |
存储条件 | -20℃ |
靶点 | EPHA2 |
体外研究 | NVP-BHG712 isomer exhibits IC 50 values of 163 nM and 1660 nM for EPHA2 and EPHA4, respectively. |
参考资料 展开查看 | 1: Li T, Wang H, Liu R, Wang X, Huang L, Wu Z, Yin X, Zou S, Duan P. The role of EphB4/ephrinB2 signaling in root repair after orthodontically-induced root resorption. Am J Orthod Dentofacial Orthop. 2021 Mar;159(3):e217-e232. doi: 10.1016/j.ajodo.2020.07.035. Epub 2021 Jan 22. PMID: 33487501. 2: Neuber C, Tröster A, Löser R, Belter B, Schwalbe H, Pietzsch J. The Pyrazolo[3,4-d]pyrimidine-Based Kinase Inhibitor NVP-BHG71 2: Effects of Regioisomers on Tumor Growth, Perfusion, and Hypoxia in EphB4-Positive A375 Melanoma Xenografts. Molecules. 2020 Nov 3;25(21):5115. doi: 10.3390/molecules25215115. PMID: 33153234; PMCID: PMC7662635. 3: Broggini T, Piffko A, Hoffmann CJ, Ghori A, Harms C, Adams RH, Vajkoczy P, Czabanka M. Ephrin-B2-EphB4 communication mediates tumor-endothelial cell interactions during hematogenous spread to spinal bone in a melanoma metastasis model. Oncogene. 2020 Nov;39(47):7063-7075. doi: 10.1038/s41388-020-01473-y. Epub 2020 Sep 28. PMID: 32989254. 4: Wan X, Saban DV, Kim SN, Weng Y, Dammann P, Keyvani K, Sure U, Zhu Y. PDCD10-Deficiency Promotes Malignant Behaviors and Tumor Growth via Triggering EphB4 Kinase Activity in Glioblastoma. Front Oncol. 2020 Aug 7;10:1377. doi: 10.3389/fonc.2020.01377. PMID: 32850441; PMCID: PMC7427606. 5: Andolfo I, Lasorsa VA, Manna F, Rosato BE, Formicola D, Iolascon A, Capasso M. Kinome multigenic panel identified novel druggable EPHB4-V871I somatic variant in high-risk neuroblastoma. J Cell Mol Med. 2020 Jun;24(11):6459-6471. doi: 10.111 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.987 ml | 9.937 ml | 19.874 ml |
5 mM | 0.397 ml | 1.987 ml | 3.975 ml |
10 mM | 0.199 ml | 0.994 ml | 1.987 ml |
5 mM | 0.04 ml | 0.199 ml | 0.397 ml |
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