Pralsetinib (Cat No.:I020039), also known as BLU-667, CS 3009, Gavreto, is a potent and selective RET (c-RET) inhibitor with an IC50 value of 0.4 nM for WT RET (c-RET) . It also has potent inhibitory effects on some common RET (c-RET) oncogenic mutations, with IC50~0.4 nM.
| Catalog Number | I020039 |
| CAS Number | 2097132-94-8 |
| Molecular Formula | C₂₇H₃₂FN₉O₂ |
| Purity | 95% |
| Storage | Store at 4°C |
| IUPAC Name | N-[(1S)-1-[6-(4-fluoropyrazol-1-yl)pyridin-3-yl]ethyl]-1-methoxy-4-[4-methyl-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]cyclohexane-1-carboxamide |
| InChI | InChI=1S/C27H32FN9O2/c1-16-11-22(33-23-12-17(2)35-36-23)34-25(31-16)19-7-9-27(39-4,10-8-19)26(38)32-18(3)20-5-6-24(29-13-20)37-15-21(28)14-30-37/h5-6,11-15,18-19H,7-10H2,1-4H3,(H,32,38)(H2,31,33,34,35,36)/t18-,19?,27?/m0/s1 |
| InChIKey | GBLBJPZSROAGMF-SIYOEGHHSA-N |
| SMILES | CC1=CC(=NN1)NC2=NC(=NC(=C2)C)C3CCC(CC3)(C(=O)NC(C)C4=CN=C(C=C4)N5C=C(C=N5)F)OC |
| Reference | [1]. 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. |
