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AZD3759

Chemical Structure : AZD3759

CAS No.: 1626387-80-1

AZD3759 (AZD-3759, AZD 3759)

Catalog No.: PC-45549Not For Human Use, Lab Use Only.

AZD3759 is a potent, orally active, BBB-penetrating EGFR inhibitor (IC50=7.2 nM, L858R pEGFR).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

AZD3759 is a potent, orally active, BBB-penetrating EGFR inhibitor (IC50=7.2 nM, L858R pEGFR).
AZD3759 fully penetrate the blood-brain barrier (BBB), with equal free concentrations in the blood, cerebrospinal fluid, and brain tissue; causes tumor regression in subcutaneous xenograft, leptomeningeal metastasis (LM), and brain metastasis (BM) lung cancer models and prevents the development of BM in nude mice.

Physicochemical Properties

M.Wt 459.9011
Formula C22H23ClFN5O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1-Piperazinecarboxylic acid, 2,4-dimethyl-, 4-[(3-chloro-2-fluorophenyl)amino]-7-methoxy-6-quinazolinyl ester, (2R)-

References

1. Zeng Q, et al. J Med Chem. 2015 Oct 22;58(20):8200-15.

2. Yang Z, et al. Sci Transl Med. 2016 Dec 7;8(368):368ra172.

3. Tan CS, et al. Lung Cancer. 2016 Mar;93:59-68.

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