JBJ-04-125-02 manufacturers
- JBJ-04-125-02
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- $2500.00 / 100mg
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2025-10-27
- CAS:2060610-53-7
- Min. Order:
- Purity:
- Supply Ability: 10g
- JBJ-04-125-02
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- $2500.00 / 100mg
-
2025-08-22
- CAS:2060610-53-7
- Min. Order:
- Purity:
- Supply Ability: 10g
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| | JBJ-04-125-02 Basic information |
| Product Name: | JBJ-04-125-02 | | Synonyms: | JBJ-04-125-02 R-isomer;2H-Isoindole-2-acetamide, α-(5-fluoro-2-hydroxyphenyl)-1,3-dihydro-1-oxo-6-[4-(1-piperazinyl)phenyl]-N-2-thiazolyl-, (αR)-;JBJ0412502,JBJ 04 125 02;(R)-2-(5-Fluoro-2-hydroxyphenyl)-2-(1-oxo-6-(4-(piperazin-1-yl)phenyl)isoindolin-2-yl)-N-(thiazol-2-yl)acetamide;(2R)-2-(5-Fluoro-2-hydroxyphenyl)-2-{1-oxo-6-[4-(piperazin-1-yl)phenyl]-1,3-dihydro-2H-isoindol-2-yl}-N-(1,3-thiazol-2-yl)acetamide | | CAS: | 2060610-53-7 | | MF: | C29H26FN5O3S | | MW: | 543.62 | | EINECS: | | | Product Categories: | | | Mol File: | 2060610-53-7.mol |  |
| | JBJ-04-125-02 Chemical Properties |
| density | 1.424±0.06 g/cm3(Predicted) | | storage temp. | Store at -20°C | | pka | 7.24±0.50(Predicted) |
| | JBJ-04-125-02 Usage And Synthesis |
| Uses | JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 0.26 nM for EGFRL858R/T790M. JBJ-04-125-02 can inhibit cancer cell proliferation and EGFRL858R/T790M/C797S signaling. JBJ-04-125-02 has anti-tumor activities[1]. | | in vivo | JBJ-04-125-02 (50 mg/kg; oral gavage; once daily; for 15 weeks; EGFRL858R/T790M/C797S genetically engineered mice) treatment leads to marked tumor regressions within 4 weeks of treatment[1].
JBJ-04-125-02 exhibits a moderate half-life of 3 hours and a high area under curve of 728,577 min?ng/mL (AUClast) following 3 mg/kg intravenous (i.v.) dose. A 20 mg/kg oral dose of JBJ-04-125-02 achieves an average maximal plasma concentration of 1.1 μmol/L with an oral bioavailability of 3%[1]. | Animal Model: | EGFRL858R/T790M/C797S genetically engineered mice (GEM)[1] | | Dosage: | 50 mg/kg | | Administration: | Oral gavage; once daily; for 15 weeks | | Result: | Led to marked tumor regressions within 4 weeks of treatment.
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| | IC 50 | EGFR (L858R/T790M): 0.26 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 |
| | JBJ-04-125-02 Preparation Products And Raw materials |
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