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JBJ-02-112-05
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Catalog No. T11713Cas No. 2748162-29-8
JBJ-02-112-05 is a potent, mutant-selective, allosteric, and orally active inhibitor of EGFR, with an IC50 of 15 nM for EGFR L858R/T790M [1].
JBJ-02-112-05
😃Good
Catalog No. T11713Cas No. 2748162-29-8
JBJ-02-112-05 is a potent, mutant-selective, allosteric, and orally active inhibitor of EGFR, with an IC50 of 15 nM for EGFR L858R/T790M [1].
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 25 mg | $1,520 | 10-14 weeks | |
| 50 mg | $1,980 | 10-14 weeks | |
| 100 mg | $2,500 | 10-14 weeks |
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Product Introduction
Bioactivity
Chemical Properties
| Description | JBJ-02-112-05 is a potent, mutant-selective, allosteric, and orally active inhibitor of EGFR, with an IC50 of 15 nM for EGFR L858R/T790M [1]. |
| Targets&IC50 | EGFR (L858R/T790M):15 nM |
| In vitro | In Ba/F3 cells, JBJ-02-112-05 inhibits the activities of wildtype EGFR, EGFR L858R, EGFR L858R/T790M, and EGFR L858R/T790M/C797S with IC50 values of 9.29 μM, 8.35 μM, 8.53 μM, and 2.13 μM, respectively [1]. JBJ-02-112-05 exhibits mutant selectivity by inhibiting mutant EGFR and downstream AKT and ERK1/2 phosphorylation in Ba/F3 cells stably transfected with EGFR L858R, EGFR L858R/T790M, and EGFR L858R/T790M/C797S mutations [1]. |
| In vivo | Administering JBJ-02-112-05 (100 mg/kg; oral gavage; once daily for 3 days) to EGFR L858R/T790M/C797S genetically engineered mice effectively inhibits the phosphorylation of EGFR and downstream signaling pathways [1]. This compound has a moderate half-life of 3 hours and reaches a peak concentration (Cmax) of 13.7 μM after an intravenous (i.v.) dose of 3 mg/kg. Furthermore, a 5 mg/kg oral dosage achieves a prolonged half-life of 16.4 hours with a Cmax of 1.31 μM [1]. |
| Molecular Weight | 464.54 |
| Formula | C27H20N4O2S |
| Cas No. | 2748162-29-8 |
| Relative Density. | 1.438 g/cm3 (Predicted) |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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