2H-Isoindole-2-acetamide, 1,3-dihydro-6-(1H-indol-5-yl)-1-oxo-α-phenyl-N-2-thiazolyl-
- CAS No.
- 2748162-29-8
- Chemical Name:
- 2H-Isoindole-2-acetamide, 1,3-dihydro-6-(1H-indol-5-yl)-1-oxo-α-phenyl-N-2-thiazolyl-
- Synonyms
- 2H-Isoindole-2-acetamide, 1,3-dihydro-6-(1H-indol-5-yl)-1-oxo-α-phenyl-N-2-thiazolyl-
- CBNumber:
- CB412229400
- Molecular Formula:
- C27H20N4O2S
- Molecular Weight:
- 464.54
- MDL Number:
- MOL File:
- 2748162-29-8.mol
2H-Isoindole-2-acetamide, 1,3-dihydro-6-(1H-indol-5-yl)-1-oxo-α-phenyl-N-2-thiazolyl- Chemical Properties,Uses,Production
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
Raw materials
Preparation Products
2H-Isoindole-2-acetamide, 1,3-dihydro-6-(1H-indol-5-yl)-1-oxo-α-phenyl-N-2-thiazolyl- Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
TargetMol Chemicals Inc. | 15002134094 | marketing@targetmol.cn | China | 19699 | 58 |
Supplier | Advantage |
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TargetMol Chemicals Inc. | 58 |