Pralsetinib (Blu667) |
| カタログ番号GC31780 |
プラルセチニブ (Blu667) (BLU-667) は、非常に強力な選択的 RET 阻害剤です。プラルセチニブ (Blu667) (BLU-667) は、WT RET、RET 変異体 V804L、V804M、M918T および CCDC6-RET 融合を、それぞれ 0.4、0.3、0.4、0.4、および 0.4 nM の IC50 で阻害します。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2097132-94-8
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Pralsetinib (Blu667) is a highly potent and selective RET inhibitor with an IC50 of 0.4 nM for wild type RET kinase.
Pralsetinib (Blu667) is a RET inhibitor extracted from patent US20170121312A1, compound example 129[1]. Pralsetinib (Blu667) demonstrates more than 10-fold increased potency over approved MKIs against oncogenic RET variants and resistance mutants. Pralsetinib (Blu667) demonstrates potent activity (IC50=0.4 nM) against common oncogenic RET alterations, including RET M918T, an activating mutation found in MTC, as well as the CCDC6-RET fusion observed in PTC and NSCLC. Pralsetinib (Blu667) suppresses RET pathway signaling in a panel of RET-driven cell lines: LC2/ad (CCDC6-RET, NSCLC), MZ-CRC-1 (RET M918T, MTC), and TT (RET C634W, MTC)[2].
Pralsetinib (Blu667) potently inhibits growth of NSCLC and thyroid cancer xenografts driven by various RET mutations and fusions without inhibiting vascular endothelial growth factor receptor 2 (VEGFR-2). Pralsetinib (Blu667) showed potent dose dependent activity against both KIF5B-RET Ba/F3 and KIF5B-RET V804L Ba/F3 allograft tumors with doses as low as 10 mg/kg twice-daily[2].
[1]. Brumaker J, et al. Inhibitors of ret. US20170121312A1. [2]. Subbiah V, et al. Precision Targeted Therapy With BLU-667 for RET-Driven Cancers. American Association for Cancer Research. 10.1158/2159-8290.CD-18-0338.
Average Rating: 5 (Based on Reviews and 11 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *