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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 1451370-01-6
- Formel: C22H20N6O
- Molecular Weight:384.43
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
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Help & FAQs
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Biologische Aktivität
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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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CAS. Nr. 1451370-01-6
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Molecular Weight 384.43
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Formel 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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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)
TAS-121 Related Classifications
HY-164392 Related Classifications
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