| Identification | Back Directory | [Name]
Pyrazolo[1,5-a]pyrimidine-5,7-diamine, 3-(3,4-dimethoxyphenyl)-N5-(1,2,2,6,6-pentamethyl-4-piperidinyl)-6-phenyl- | [CAS]
2561413-77-0 | [Synonyms]
Pyrazolo[1,5-a]pyrimidine-5,7-diamine, 3-(3,4-dimethoxyphenyl)-N5-(1,2,2,6,6-pentamethyl-4-piperidinyl)-6-phenyl- | [Molecular Formula]
C30H38N6O2 | [MOL File]
2561413-77-0.mol | [Molecular Weight]
514.66 |
| Hazard Information | Back Directory | [Uses]
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]. | [in vivo]
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]. | Animal Model: | Female 6-8 week old Harlan Foxn1 nude mice with RIE-RET-KIF5B transgenic cell line | | Dosage: | 1, 3, 10 mg/kg | | Administration: | Dosed orally, 1x daily for 10 days | | Result: | Inhibited tumor growth in RIE KIF5B-RET xenograft mice. |
| [References]
[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. DOI:10.1021/acsmedchemlett.0c00015 |
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