Pyrazolo[1,5-a]pyrimidine-5,7-diamine, 3-(3,4-dimethoxyphenyl)-N5-(1,2,2,6,6-pentamethyl-4-piperidinyl)-6-phenyl-

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Pyrazolo[1,5-a]pyrimidine-5,7-diamine, 3-(3,4-dimethoxyphenyl)-N5-(1,2,2,6,6-pentamethyl-4-piperidinyl)-6-phenyl- Basic information
Product Name:Pyrazolo[1,5-a]pyrimidine-5,7-diamine, 3-(3,4-dimethoxyphenyl)-N5-(1,2,2,6,6-pentamethyl-4-piperidinyl)-6-phenyl-
Synonyms: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
MF:C30H38N6O2
MW:514.66
EINECS:
Product Categories:
Mol File:2561413-77-0.mol
Pyrazolo[1,5-a]pyrimidine-5,7-diamine, 3-(3,4-dimethoxyphenyl)-N5-(1,2,2,6,6-pentamethyl-4-piperidinyl)-6-phenyl- Structure
Pyrazolo[1,5-a]pyrimidine-5,7-diamine, 3-(3,4-dimethoxyphenyl)-N5-(1,2,2,6,6-pentamethyl-4-piperidinyl)-6-phenyl- Chemical Properties
density 1.21±0.1 g/cm3(Predicted)
pka10.26±0.10(Predicted)
form Solid
color White to off-white
Safety Information
MSDS Information
Pyrazolo[1,5-a]pyrimidine-5,7-diamine, 3-(3,4-dimethoxyphenyl)-N5-(1,2,2,6,6-pentamethyl-4-piperidinyl)-6-phenyl- Usage And Synthesis
UsesWF-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
Pyrazolo[1,5-a]pyrimidine-5,7-diamine, 3-(3,4-dimethoxyphenyl)-N5-(1,2,2,6,6-pentamethyl-4-piperidinyl)-6-phenyl- Preparation Products And Raw materials
Tag:Pyrazolo[1,5-a]pyrimidine-5,7-diamine, 3-(3,4-dimethoxyphenyl)-N5-(1,2,2,6,6-pentamethyl-4-piperidinyl)-6-phenyl-(2561413-77-0) Related Product Information
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