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BLU-667 trans form

Names

[ CAS No. ]:
2097132-93-7

[ Name ]:
BLU-667 trans form

Biological Activity

[Description]:

cis-Pralsetinib (cis-Blu667) is a highly potent and selective inhibitor of rearranged during transfection (RET), with IC50 values ranging from 0.3 to 0.4 nM for WT RET and four enzyme variants (V804L, V804M, M918T, CCDC6-RET), and with broad, robust and anti-tumor activity against multiple RET-driven solid tumor types[1][2].

[Related Catalog]:

Research Areas >> Cancer

[Target]

IC50: 0.4 nM (WT RET), 0.3 nM (RET V804L), 0.4 nM (RET V804M), 0.4 nM (RET M918T), 0.4 nM (CCDC6-RET)[2]


[References]

[1]. http://www.blueprintmedicines.com/wp-content/uploads/2017/10/BLU-667-EORTC-2017-BPM.pdf

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C27H32FN9O2

[ Molecular Weight ]:
533.60


Related Compounds