| Company Name: |
TargetMol Chemicals Inc.
|
| Tel: |
15002134094 |
| Email: |
marketing@targetmol.cn |
| Products Intro: |
Product Name:JBJ-02-112-05
CAS:2748162-29-8
Package:25mg/RMB 10600;50mg/RMB 13800;100mg/RMB 17500
|
|
| | 2H-Isoindole-2-acetamide, 1,3-dihydro-6-(1H-indol-5-yl)-1-oxo-α-phenyl-N-2-thiazolyl- Basic information |
| | 2H-Isoindole-2-acetamide, 1,3-dihydro-6-(1H-indol-5-yl)-1-oxo-α-phenyl-N-2-thiazolyl- Chemical Properties |
| density | 1.438±0.06 g/cm3(Predicted) | | pka | 7.58±0.50(Predicted) |
| | 2H-Isoindole-2-acetamide, 1,3-dihydro-6-(1H-indol-5-yl)-1-oxo-α-phenyl-N-2-thiazolyl- Usage And Synthesis |
| Uses | JBJ-02-112-05 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 15 nM for EGFRL858R/T790M[1]. | | in vivo | JBJ-02-112-05 (100 mg/kg; oral gavage; once daily; for 3 days; EGFRL858R/T790M/C797S genetically engineered mice) treatment inhibits phosphorylation of EGFR and downstream signaling pathways[1].
JBJ-02-112-05 exhibits a moderate half-life of 3 hours and a Cmax of 13.7 μM following 3 mg/kg intravenous (i.v.) dose. A 5 mg/kg oral dose of JBJ-02-112-05 achieves a half-life of 16.4 hours and a CCmax of 1.31 μM[1]. | Animal Model: | EGFRL858R/T790M/C797S genetically engineered mice[1] | | Dosage: | 100 mg/kg | | Administration: | Oral gavage; once daily; for 3 days | | Result: | Inhibited phosphorylation of EGFR and downstream signaling pathways.
|
| | IC 50 | EGFRL858R/T790M: 15 nM (IC50) | | References | [1] To C, et al. Single and Dual Targeting of Mutant EGFR with an Allosteric Inhibitor. Cancer Discov. 2019 Jul;9(7):926-943. DOI:10.1158/2159-8290.CD-18-0903 |
| | 2H-Isoindole-2-acetamide, 1,3-dihydro-6-(1H-indol-5-yl)-1-oxo-α-phenyl-N-2-thiazolyl- Preparation Products And Raw materials |
|