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AZD3759

AZD3759 structure

CAS No:
1626387-80-1
Formula:
C22H23ClFN5O3
Chemical Name:
AZD3759
Categories:
Pharmaceutical Intermediates > Bulk Drug Intermediates

Description

AZD3759 is a potent, oral active, central nervous system-penetrant, EGFR inhibitor. At Km ATP concentrations, the IC50s are 0.3, 0.2, and 0.2 nM for EGFRwt, EGFRL858R, and EGFRexon 19Del, respectively.

AZD-3759 is under investigation in clinical trial NCT03360929 (Evaluate Safety, Tolerability, Pharmacokinetics and Anti-tumor Activity of AZD3759).|Zorifertinib is an orally available inhibitor of the epidermal growth factor receptor (EGFR), with potential antineoplastic activity. Upon oral administration, zorifertinib binds to and inhibits the activity of EGFR as well as certain mutant forms of EGFR. This prevents EGFR-mediated signaling, and may lead to both induction of cell death and inhibition of tumor growth in EGFR-overexpressing cells. EGFR, a receptor tyrosine kinase mutated in many tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization.

AZD3759 Basic Attributes

Molecular Weight：

459.9

Exact Mass：

459.147339

UNII：

67SX9H68W2

NCI Thesaurus Code：

C118289

Characteristics

PSA：

79.8

XLogP3：

4.1

Appearance：

white to off-white solid

Density：

1.4±0.1 g/cm3

Melting Point：

192.4 °C(醇、酯), 193.3 °C (水)

Flash Point：

299.3±30.1 °C

Refractive Index：

1.632

Storage Conditions：

3 years -20℃ powder, 6 months -80℃ in solvent

Drug Information

MeSH Entry Terms：

4-((3-chloro-2-fluorophenyl)amino)-7-methoxyquinazolin-6-yl 2,4-dimethylpiperazine-1-carboxylate

Computed Properties

Molecular Weight:459.9
XLogP3:4.1
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:8
Rotatable Bond Count:5
Exact Mass:459.1473455
Monoisotopic Mass:459.1473455
Topological Polar Surface Area:79.8
Heavy Atom Count:32
Complexity:649
Defined Atom Stereocenter Count:1
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

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