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AZD3759
- Optical Purity: Optically pure
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C22H23ClFN5O3
- MW: 459.9
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, AZD3759 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.
More Information
| Parent CAS No. | 1626387-80-1 |
|---|---|
| Chemical Name | (R)-4-(3-chloro-2-fluorophenylamino)-7-methoxyquinazolin-6-yl 2,4-dimethylpiperazine-1-carboxylate |
| SMILES | N1(C(OC2C(OC)=CC3C(C=2)=C(NC2=CC=CC(Cl)=C2F)N=CN=3)=O)CCN(C)C[C@H]1C |&1:30,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C22H23ClFN5O3/c1-13-11-28(2)7-8-29(13)22(30)32-19-9-14-17(10-18(19)31-3)25-12-26-21(14)27-16-6-4-5-15(23)20(16)24/h4-6,9-10,12-13H,7-8,11H2,1-3H3,(H,25,26,27)/t13-/m1/s1 |
| InChiKey | MXDSJQHFFDGFDK-CYBMUJFWSA-N |
| CID | 78209992 |
| Short Description | EGFR inhibitor |
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