TAS-121
TAS-121 is an orally active, selective, covalent, third-generation mutant EGFR-tyrosine kinase inhibitor (EGFR-TKI). TAS-121 inhibits the L858R mutation (IC50=1.7 nM), Ex19del mutation (IC50=2.7 nM), L858R/T790M mutation (IC50=0.56 nM) and Ex19del/T790M mutation (IC50=1.1 nM) and wild-type EGFR (IC50=8.2 nM). TAS-121 inhibits HER2 and HER4 with IC50s of 110 and 2.6 nM, respectively. TAS-121 inhibits phosphorylation of EGFR and its downstream signaling targets to block cell proliferation. TAS-121 induces apoptosis and displays antitumor activity in SW48 (EGFR G719S) and NCI-H1975 (EGFR L858R/T790M) xenograft models.
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- No. CAS: 1451370-01-6
- Fòrmula: C22H20N6O
- Peso molecular:384.43
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
|
EGFR L858R 1.7 nM (IC50) |
EGFR (ex19del) 2.7 nM (IC50) |
EGFR L858R/T790M 0.56 nM (IC50) |
EGFR (ex19del/T790M) 1.1 nM (IC50) |
EGFR (WT) 8.2 nM (IC50) |
HER2 110 nM (IC50) |
HER4 2.6 nM (IC50) |
Chemical Information
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No. CAS 1451370-01-6
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Peso molecular 384.43
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Fòrmula C22H20N6O
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SMILES
NC1=C2C(C3=CC4=C(C=CC=C4)N=C3)=C5N(C[C@H](CC5)NC(C=C)=O)C2=NC=N1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TAS-121 Related Classifications
HY-164392 Related Classifications
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