An irreversible inhibitor of mutant EGFRs (IC50s = 1.7

Lazertinib – 25 mg

Brand:
Cayman
CAS:
1903008-80-9
Storage:
-20
UN-No:
Non-Hazardous - /

Lazertinib is an irreversible inhibitor of mutant EGFRs (IC50s = 1.7, 2, and 3.3 nM for EGFRL858R/T790M, EGFRDel19/T790M, and EGFRDel19, respectively).{52289} It is selective for mutant EGFRs over wild-type EGFR, HER2, and HER4 (IC50s = 76, 364, and 1,017 nM, respectively). Lazertinib reduces viability of Ba/F3 cells expressing mutant EGFRs (IC50s = 3.3-5.7 nM). In vivo, lazertinib (1, 3, and 10 mg/kg) reduces tumor volume in an EGFRT790M mutant H1975 non-small cell lung cancer (NSCLC) mouse xenograft model.  

 

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SKU: 29670 - 25 mg Category:

Description

An irreversible inhibitor of mutant EGFRs (IC50s = 1.7, 2, and 3.3 nM for EGFRL858R/T790M, EGFRDel19/T790M, and EGFRDel19, respectively); selective for mutant EGFRs over wild-type EGFR, HER2, and HER4 (IC50s = 76, 364, and 1,017 nM, respectively); reduces viability of Ba/F3 cells expressing mutant EGFRs (IC50s = 3.3-5.7 nM); reduces tumor volume in an EGFRT790M mutant H1975 NSCLC mouse xenograft model at 1, 3, and 10 mg/kg

Formal name: N-[5-[[4-[4-[(dimethylamino)methyl]-3-phenyl-1H-pyrazol-1-yl]-2-pyrimidinyl]amino]-4-methoxy-2-(4-morpholinyl)phenyl]-2-propenamide

Synonyms:  YH25448

Molecular weight: 554.6

CAS: 1903008-80-9

Purity: ≥98%

Formulation: A solid

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