1. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Apoptosis
  2. EGFR Apoptosis Bcl-2 Family Survivin
  3. 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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JS04

JS04 Chemical Structure

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Description

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[1].

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.

Apoptosis Analysis[1]

Cell Line: H1975 NSCLC
Concentration: 10 and 20 μM
Incubation Time: 48 h
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.

Cell Cycle Analysis[1]

Cell Line: H1975 NSCLC
Concentration: 10 and 20 μM
Incubation Time: 48 h
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

JS04 (6.25-100 μM; immersion treatment; continuous administration; from 5.5 to 6 hours post-fertilization to 96 hours post-fertilization) exhibits favorable acute safety in zebrafish (Danio rerio) embryos[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: AB-WT (fertilised embryos)[1]
Dosage: 6.25 μM; 12.5 μM; 25 μM; 50 μM; 100 μM
Administration: immersion; continuous; 5.5-6 hpf through 96 hpf
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.
Molecular Weight

382.89

Formula

C20H23ClN6

SMILES

CNC1=NC(NC2=CC=C(C=C2)N3CCN(CC3)C)=NC4=CC(Cl)=CC=C41

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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JS04
Cat. No.:
HY-182031
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