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- 文献和实验
- 技术资料
- 保存条件：
见说明书
- 保质期：
＞1年
- 英文名：
JNJ-10198409 Free Base
- 库存：
期货2-3周
- 供应商：
上海经科化学科技有限公司
- CAS号：
627518-40-5
- 规格：
1mg
供应商：上海经科化学科技有限公司
服务热线：400-0199-638
QQ:472482400(上海经科）
微信号：shjkchem
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本试剂(JNJ-10198409)
仅供科研实验使用,不得用于其他用途！
货 号：J-4567
名 称：JNJ-10198409
别 名：JNJ-10198409 Free Base
C A S ：627518-40-5
分子量：325.34
分子式：C18H16FN3O2
纯 度：HPLC/TLC:>99%
说 明：Storage: Store at or below -20 ºC. Solubility: Soluble in DMSO. Disposal: A
文 献：JNJ-10198409 has anti-PDGFR-β kinase activity with an IC50 of 4.2 nM and potent antiproliferative activity in six of eight human tumor cell lines, with IC50 values of less than 33 nM. Ho, C.Y., et al. "(6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad antiproliferative activity against tumor cells." J. Med. Chem. 48: 8163-8173 (2005). The in vivo inhibitory effect of JNJ-10198409 on PDGF-RTK was confirmed in tumor tissues after administering the compound orally in a nude mouse xenograft model of human LoVo colon cancer. D'Andrea, M.R., et al. "Validation of in vivo pharmacodynamic activity of a novel PDGF receptor tyrosine kinase inhibitor using immunohistochemistry and quantitative image analysis." Mol. Cancer Ther. 4: 1198-1204 (2005). Multiple UDP-glucuronosyltransferase 1A enzymes are responsible for the glucuronidation of JNJ-10198409 in human liver microsomes. Yan, Z., et al. "N-glucuronidation of the platelet-derived growth factor receptor tyrosine kinase inhibitor 6,7-(dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)-(3-fluoro-phenyl)-amine by human UDP-glucuronosyltransferases." Drug Metab Dispos 34: 748-755 (2006). JNJ-10198409 demonstrated potent anti-proliferative activities against human leukemia cells K562 and SUP-B15. It induced cell apoptosis concentration-dependently while the remaining viable cells demonstrated G2/M cell cycle arrest. Using K562 growing as a solid tumor in nude mice, JNJ-10198409 caused dose-dependent inhibition of tumor growth without overt toxicity in vivo. Mei, J., et al. "A novel PDGFR kinase, c-ABL and c-Kit inhibitor with unique anti-proliferative activity inducing specific cell cycle dysregulation in human leukemia cells " Proc. Amer. Assoc. Cancer Res. 45: Abstract #5982 (2005). JNJ-10198409 has both anti-angiogenesis and tumor cell anti-proliferative activities. Mei, J., et al. "A novel PDGF receptor tyrosine kinase inhibitor with dual anti-angiogenesis and tumor cell anti-proliferative activity." Proc. Amer. Assoc. Cancer Res. 45: Abstract #3990 (2004). Tuman R., et al. "Discovery of a novel, dual mechanism anti-angiogenic and anti-proliferative agent with oral anti-tumor activity." Proc. Amer. Assoc. Cancer Res. 45: Abstract #4558 (2004). JNJ-10198409 selectively inhibited neuroblastoma cell growth in alamarBlue® assays and rapidly induced neuroblastoma cell apoptosis without affecting the growth of primary pediatric neural crest-like stem cells. It may function by inhibiting the activity of Src family kinases. Fujitani, M., et al. "Potent and selective cytotoxic and cytostatic activity of JNJ-10198409 against neuroblastoma cells." Chiba Medical J. 88E: 27-34 (2012).
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