JBJ-04-125-02 R-isomer
This product is for research use only, not for human use. We do not sell to patients.
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| Size | Price | Stock |
|---|---|---|
| 100mg | $900 | To Be Confirmed |
| 250mg | $1750 | To Be Confirmed |
| 500mg | $2625 | To Be Confirmed |
: Cat #: V37821 CAS #: 2060610-53-7 Purity ≥ 99%
Description: JBJ-04-125-02 R-isomer, the R-enantiomer of JBJ-04-125-02, is a novel, highly potent, mutant-specific, allosteric and orally bioavailable EGFR inhibitor with an IC50 of 0.26 nM for EGFRL858R/T790M.
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| Molecular Weight (MW) | 543.61 |
|---|---|
| Molecular Formula | C29H26FN5O3S |
| CAS No. | 2060610-53-7 |
| SMILES Code | O=C(NC1=NC=CS1)[C@@H](C2=CC(F)=CC=C2O)N(CC3=C4C=C(C5=CC=C(N6CCNCC6)C=C5)C=C3)C4=O |
| Synonyms | JBJ-04-125-02; JBJ 04-125-02; JBJ04-125-02; JBJ-0412502; JBJ 0412502; JBJ0412502; JBJ-04-125-02 R-isomer; |
| Protocol | In Vitro | JBJ-04-125-02 treatment also inhibits cell proliferation in Ba/F3 cells stably transfected with EGFRL858R, EGFRL858R/T790M, or EGFRL858R/T790M/C797S mutations. JBJ-04-125-02 (0-1000 nM; 72 hours; H1975 cells) treatment could inhibit cell proliferation of H1975 cells at low nanomolar concentrations. The ability of JBJ-04-125-02 (0.01-10 μM) to inhibit EGFR phosphorylation using Ba/F3, H1975 and NIH-3T3 cells is examined. JBJ-04-125-02 demonstrates mutant selectivity by inhibiting mutant EGFR and downstream AKT and ERK1/2 phosphorylation. |
|---|---|---|
| In Vivo | 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%. 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. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 1.8396 mL | 9.1978 mL | 18.3955 mL | 36.7911 mL |
| 5mM | 0.3679 mL | 1.8396 mL | 3.6791 mL | 7.3582 mL |
| 10mM | 0.1840 mL | 0.9198 mL | 1.8396 mL | 3.6791 mL |
| 20mM | 0.0920 mL | 0.4599 mL | 0.9198 mL | 1.8396 mL |
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Method for preparing in vivo formulation:
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