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Lazertinib

Lazertinib structure

CAS No:
1903008-80-9
Formula:
C30H34N8O3
Chemical Name:
Lazertinib
Synonyms:
GNS1480
Categories:
Biochemical Engineering > Inhibitors

Description

Lazertinib is under investigation in clinical trial NCT04487080 (A Study of Amivantamab and Lazertinib Combination Therapy Versus Osimertinib in Locally Advanced or Metastatic Non-small Cell Lung Cancer).|Lazertinib is an orally available third-generation, selective inhibitor of certain forms of the epidermal growth factor receptor (EGFR) with activating mutations, including the resistance mutation T790M, exon 19 deletions (Del19), and the L858R mutation, with potential antineoplastic activity. Upon administration, lazertinib specifically and irreversibly binds to and inhibits selective EGFR mutants, which prevents EGFR mutant-mediated signaling and leads to cell death in EGFR mutant-expressing tumor cells. Lazertinib may inhibit programmed cell death-1 ligand 1 (PD-L1) and inflammatory cytokines in specific cancer cells harboring certain EGFR mutations. Compared to some other EGFR inhibitors, lazertinib may have therapeutic benefits in tumors with T790M- or L858R-mediated drug resistance. In addition, lazertinib penetrates the blood-brain barrier (BBB). This agent shows minimal activity against wild-type EGFR (wtEGFR), and does not cause dose-limiting toxicities, which occur during the use of non-selective EGFR inhibitors and inhibit wtEGFR. EGFR, a receptor tyrosine kinase (RTK) mutated in many tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization.

Lazertinib Basic Attributes

Molecular Weight：

554.64

Exact Mass：

554.27538698

UNII：

4A2Y23XK11

NCI Thesaurus Code：

C148147

Characteristics

PSA：

110

XLogP3：

3.4

Density：

1.27±0.1 g/cm3(Predicted)

Safety Information

GHS Classification：

|Danger|H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]|P201, P202, P260, P261, P264, P270, P272, P280, P281, P301+P312, P302+P352, P308+P313, P314, P321, P330, P333+P313, P363, P405, and P501|The GHS information provided by 1 company from 1 notification to the ECHA C&L Inventory.

Drug Information

MeSH：

Agents that inhibit PROTEIN KINASES. (See all compounds classified as Protein Kinase Inhibitors.)

MeSH Entry Terms：

2-Propenamide, N-(5-((4-(4-((dimethylamino)methyl)-3-phenyl-1H-pyrazol-1-yl)-2-pyrimidinyl)amino)-4-methoxy-2-(4-morpholinyl)phenyl)-

Computed Properties

Molecular Weight:554.6
XLogP3:3.4
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:9
Rotatable Bond Count:10
Exact Mass:554.27538698
Monoisotopic Mass:554.27538698
Topological Polar Surface Area:110
Heavy Atom Count:41
Complexity:837
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

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