JS04
JS04 is a EGFRL858R/T790M kinase inhibitor. JS04 activates both endogenous and exogenous apoptosis (apoptosis) pathways and induces G2/M phase arrest of the cell cycle. JS04 is applicable to the research of drug-resistant non-small cell lung cancer.
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- Formule: C20H23ClN6
- Masse moléculaire:382.89
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
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Activité biologique
Description
IC50 & Target
[1]|
EGFRL858R/T790M |
Bcl-2 |
Bcl-xL |
In Vitro
JS04 (72 h) potently inhibits the proliferation of H1975 and A549 non-small cell lung cancer (NSCLC) cells, with IC50 values of 8.11 μM and 11.58 μM, respectively; meanwhile, this compound exhibits a favorable safety window against human Hs27 fibroblasts, with a selectivity index of 2.52[1].
JS04 (10-20 μM; 48 h) induces dose-dependent apoptosis in H1975 cells[1].
JS04 (10-20 μM; 48 h) induces G2/M cell cycle arrest in H1975 cells[1].
JS04 (72 h) can simultaneously activate the intrinsic apoptotic pathway (downregulating the expression of BCL-2, BCL-xL and Survivin) and the extrinsic apoptotic pathway (upregulating the expression of TRAIL R2/DR5)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:H1975 NSCLC
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Concentration:10 and 20 μM
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Incubation Time:48 h
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Result:At 20 μM, induced 74% total apoptotic cell death.
At 10 μM, produced a lower level of apoptosis compared to 20 μM, as confirmed by reduced viable cell populations.
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Cell Line:H1975 NSCLC
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Concentration:10 and 20 μM
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Incubation Time:48 h
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Result:At 20 μM, caused an approximately 3 to 4-fold increase in the G2/M cell population (35% of cells in G2/M phase), with a concomitant decrease in G0/G1 phase cells.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:AB-WT (fertilised embryos)[1]
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Dosage:6.25 μM; 12.5 μM; 25 μM; 50 μM; 100 μM
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Administration:immersion; continuous; 5.5-6 hpf through 96 hpf
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Result:Caused 100% embryo mortality at 100 μM and 96 hpf.
Resulted in < 20% mortality across all time points at 6.25, 12.5, and 25 μM.
Chemical Information
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Masse moléculaire 382.89
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Formule C20H23ClN6
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SMILES
CNC1=NC(NC2=CC=C(C=C2)N3CCN(CC3)C)=NC4=CC(Cl)=CC=C41
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
JS04 Related Classifications
HY-182031 Related Classifications
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