DY3002
DY3002 is a selective and highly potent EGFR inhibitor with activity in overcoming T790M-mediated drug resistance in non-small cell lung cancer. DY3002 exhibited superior inhibitory effects against EGFR T790M mutants in kinase assays (IC50 = 0.71 nM), compared to weaker inhibitory effects against wild-type EGFR (IC50 = 448.7 nM). DY3002 was significantly superior to rociletinib and osimertinib in selectivity, showing an extremely high selectivity index (SI = 632.0). In cell experiments, DY3002 had an IC50 value of 0.037 μM against H1975 cells, showing enhanced inhibitory potency. In addition, DY3002 was superior to other alternative compounds in terms of biological properties and did not cause hyperglycemia.
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- CAS. Nr.: 2020015-37-4
- Formel: C24H25ClN6O2
- Molecular Weight:464.95
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-431 | IC50 |
0.382 μM
Compound: 10c
|
Antiproliferative activity against human A431 cells incubated for 72 hrs by MTT assay
Antiproliferative activity against human A431 cells incubated for 72 hrs by MTT assay
|
[PMID: 28395219] |
| A549 | IC50 |
4.45 μM
Compound: 10c
|
Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay
Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay
|
[PMID: 28395219] |
| HCC827 | IC50 |
0.044 μM
Compound: 10c
|
Antiproliferative activity against human HCC827 cells incubated for 72 hrs by MTT assay
Antiproliferative activity against human HCC827 cells incubated for 72 hrs by MTT assay
|
[PMID: 28395219] |
| NCI-H1975 | IC50 |
0.037 μM
Compound: 10c
|
Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTT assay
Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTT assay
|
[PMID: 28395219] |
Chemical Information
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CAS. Nr. 2020015-37-4
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Molecular Weight 464.95
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Formel C24H25ClN6O2
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SMILES
C=CC(NC1=CC=CC(NC2=NC(NC3=CC=C(C=C3)CN4CCOCC4)=NC=C2Cl)=C1)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)