产品名称 AZD 3759
产品货号 Axon 2563 CAS [1626387-80-1] MF C22H23ClFN5O3MW 459.90 Purity: 98% Optical purity: Optically pure Soluble in 0.1N HCl(aq) and DMSO Description Potent, orally active, brain-penetrant, EGFR tyrosine kinase inhibitor (IC50 value 7.2 nM for inhibition of cellular phosphorylation on L858R cell lines), that shows tumor regression in the mouse model with brain metastasis. At 1 µM, AZD 3759 showed less than 50% inhibition against 115 out of a panel of 124 recombinant protein and lipid kinases, and was neither a direct inhibitor nor a time-dependent inhibitor for a series of Cytochrome isoforms, suggesting a low enzyme induction liability. KEYWORDS: AZD 3759 | supplier | EGFR inhibitor | AZD3759 | CAS [1626387-80-1] | [1626387-81-2] | EGF | EGFR | Inhibitor | orally active | brain-penetrant | RTK | CNS | tumor regression | metastases | clinical trial | central nervous system
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产品品牌 axonmedchem
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AZD 3759

Based on 62 reference(s) in Google Scholar 9 10 62

Axon 2563

CAS [1626387-80-1]

MF C22H23ClFN5O3
MW 459.90

  • Purity: 98%
  • Optical purity: Optically pure
  • Soluble in 0.1N HCl(aq) and DMSO

AZD 3759

Description

Potent, orally active, brain-penetrant, EGFR tyrosine kinase inhibitor (IC50 value 7.2 nM for inhibition of cellular phosphorylation on L858R cell lines), that shows tumor regression in the mouse model with brain metastasis. At 1 µM, AZD 3759 showed less than 50% inhibition against 115 out of a panel of 124 recombinant protein and lipid kinases, and was neither a direct inhibitor nor a time-dependent inhibitor for a series of Cytochrome isoforms, suggesting a low enzyme induction liability.

KEYWORDS: AZD 3759 | supplier | EGFR inhibitor | AZD3759 | CAS [1626387-80-1] | [1626387-81-2] | EGF | EGFR | Inhibitor | orally active | brain-penetrant | RTK | CNS | tumor regression | metastases | clinical trial | central nervous system

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