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.
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- CAS No.: 173458-56-5
- 화학식: C14H13ClN4
- 분자량:272.73
-
보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
All EGFR Isoforms
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Biological Activity
|
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
-
분자량 272.73
-
화학식 C14H13ClN4
-
SMILES
ClC1=CC=CC(NC2=NC=NC3=C2C(C)=C(C)N3)=C1
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Synonyms
TRX-13
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)