For research use only. Not for therapeutic Use.
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 and 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].
| Catalog Number | I045874 |
| CAS Number | 2561413-77-0 |
| Synonyms | 3-(3,4-dimethoxyphenyl)-5-N-(1,2,2,6,6-pentamethylpiperidin-4-yl)-6-phenylpyrazolo[1,5-a]pyrimidine-5,7-diamine |
| Molecular Formula | C30H38N6O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C30H38N6O2/c1-29(2)16-21(17-30(3,4)35(29)5)33-27-25(19-11-9-8-10-12-19)26(31)36-28(34-27)22(18-32-36)20-13-14-23(37-6)24(15-20)38-7/h8-15,18,21H,16-17,31H2,1-7H3,(H,33,34) |
| InChIKey | YRBWLEAMGAGYBK-UHFFFAOYSA-N |
| SMILES | CC1(CC(CC(N1C)(C)C)NC2=NC3=C(C=NN3C(=C2C4=CC=CC=C4)N)C5=CC(=C(C=C5)OC)OC)C |
| Reference | [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. |
