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 No.: 2020015-37-4
- 화학식: C24H25ClN6O2
- 분자량:464.95
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Endogenous Metabolite Isoforms
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Biological Activity
|
Cell Line
|
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 No. 2020015-37-4
-
분자량 464.95
-
화학식 C24H25ClN6O2
-
SMILES
C=CC(NC1=CC=CC(NC2=NC(NC3=CC=C(C=C3)CN4CCOCC4)=NC=C2Cl)=C1)=O
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선적
Room temperature in continental US; may vary elsewhere.
-
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)