CGP-59326
CGP-59326 (TRX-13) is a highly potent and selective epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (IC50=0.027 μM). CGP-59326 blocks the EGFR signaling pathwa, demonstrating highly selective inhibition of EGFR-dependent tumor cells. CGP-59326 is promising for research of cancers.
For research use only. We do not sell to patients.
- CAS No.: 173458-56-5
- Formula: C14H13ClN4
- Molecular Weight:272.73
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All EGFR Isoforms
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Biological Activity
Description
Cellular Effect
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A-431 | ED50 |
1.5 mg/kg
Compound: 13
|
In vivo efficacy following oral administration in nude mouse tumor model, xenograft A431 cells expressing EGF-R
In vivo efficacy following oral administration in nude mouse tumor model, xenograft A431 cells expressing EGF-R
|
[PMID: 8691423] |
| A-431 | IC50 |
0.3 μM
Compound: 13
|
Inhibition of EGF-stimulated tyrosine phosphorylation in A431 cells expressing EGF-R
Inhibition of EGF-stimulated tyrosine phosphorylation in A431 cells expressing EGF-R
|
[PMID: 8691423] |
| Balb/MK | IC50 |
1.4 μM
Compound: 13
|
Inhibition of proliferation of EGF-dependent BALB/MK cells
Inhibition of proliferation of EGF-dependent BALB/MK cells
|
[PMID: 8691423] |
| NIH3T3 | IC50 |
>10 μM
Compound: 13
|
Inhibition of PDGF-stimulated tyrosine phosphorylation in BALB/c 3T3 cells
Inhibition of PDGF-stimulated tyrosine phosphorylation in BALB/c 3T3 cells
|
[PMID: 8691423] |
| NIH3T3 | IC50 |
>100 μM
Compound: 13
|
Inhibition of PDGF-induced c-fos mRNA expression in BALB/c 3T3 cells
Inhibition of PDGF-induced c-fos mRNA expression in BALB/c 3T3 cells
|
[PMID: 8691423] |
| NIH3T3 | IC50 |
>100 μM
Compound: 13
|
Inhibition of PMA/PKC-mediated c-fos mRNA expression in BALB/c 3T3 cells
Inhibition of PMA/PKC-mediated c-fos mRNA expression in BALB/c 3T3 cells
|
[PMID: 8691423] |
| NIH3T3 | IC50 |
2 μM
Compound: 13
|
Inhibition of EGF-induced c-fos mRNA expression in BALB/c 3T3 cells
Inhibition of EGF-induced c-fos mRNA expression in BALB/c 3T3 cells
|
[PMID: 8691423] |
Chemical Information
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CAS No. 173458-56-5
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Molecular Weight 272.73
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Formula C14H13ClN4
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SMILES
ClC1=CC=CC(NC2=NC=NC3=C2C(C)=C(C)N3)=C1
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Synonyms
TRX-13
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)