WF-47-JS03 |
| Catalog No.GC61381 |
WF-47-JS03 est un inhibiteur puissant et sélectif de la kinase RET avec des IC50 de 1,7 nM et 5,3 nM pour les cellules Ba/F3 transfectées par KIF5B-RET et les cellules cancéreuses du poumon LC-2/ad transfectées par CCDC6-RET, respectivement. WF-47-JS03 démontre une sélectivité > 500 fois contre le récepteur de domaine d'insertion de kinase (KDR). Pénétration cérébrale efficace.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2561413-77-0
Sample solution is provided at 25 µL, 10mM.
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WF-47-JS03 is a potent and selective RET kinase inhibitor with IC50s of 1.7 nM and 5.3 nM for KIF5B-RET transfected Ba/F3 cells, CCDC6-RET transfected LC-2/ad lung cancer cells, respectively. WF-47-JS03 demonstrates >500-fold selectivity against kinase insert domain receptor (KDR). Effective brain penetration[1].
WF-47-JS03 inhibits Tel-KDR transfected Ba/F3 cells, and Ba/F3 wild-type cell lines with IC50s of 0.99 and 1.5 μM, respectively[1].
WF-47-JS03 significantly inhibits tumor growth in RIE KIF5B-RET xenograft mice and is well tolerated at 1, 3, and 10 mg/kg in the 10 day study[1]. Animal Model: Female 6-8 week old Harlan Foxn1 nude mice with RIE-RET-KIF5B transgenic cell line
[1]. Casey J N Mathison , et al. Efficacy and Tolerability of Pyrazolo[1,5- a]pyrimidine RET Kinase Inhibitors for the Treatment of Lung Adenocarcinoma. ACS Med Chem Lett. 2020 Feb 12;11(4):558-565.
Average Rating: 5 (Based on Reviews and 22 reference(s) in Google Scholar.)
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