RET V804M-IN-1

• CAT Number: I015177
• CAS Number: 2414909-94-5
• Molecular Formula: C19H16N6O
• Molecular Weight: 344.37
• Purity: ≥95%
• Synonyms: 4-[5-(pyridin-3-ylmethylamino)pyrazolo[1,5-a]pyrimidin-3-yl]benzamide
• InChI: InChI=1S/C19H16N6O/c20-18(26)15-5-3-14(4-6-15)16-12-23-25-9-7-17(24-19(16)25)22-11-13-2-1-8-21-10-13/h1-10,12H,11H2,(H2,20,26)(H,22,24)
• InChIKey: LMGXQBQAUALFTB-UHFFFAOYSA-N
• SMILES: C1=CC(=CN=C1)CNC2=NC3=C(C=NN3C=C2)C4=CC=C(C=C4)C(=O)N

RET V804M-IN-1 (compound 5) is a wt-RET -selective inhibitors of RETV804M kinase, with an IC50 of 20 nM[1].
RET V804M-IN-1 (compound 5) exhibits 3.7 and 110 fold selectivity compared to wt-RET and KDR, respectively[1].

Reference

[1]. Rebecca Newton, et al. Discovery and Optimization of wt-RET/KDR-Selective Inhibitors of RET V804M Kinase. ACS Med Chem Lett. 2020 Feb 28;11(4):497-505.
 [Content Brief]