A brain penetrant inhibitor of EGFR
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AZD 3759

Item No. 19931

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2R)-2,4-dimethyl-1-piperazinecarboxylic acid, 4-[(3-chloro-2-fluorophenyl)amino]-7-methoxy-6-quinazolinyl ester
CAS Number
1626387-80-1
Molecular Formula
C22H23ClFN5O3
Formula Weight
459.9
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 10 mg/mlEthanol: 2 mg/ml
λmax
205, 224, 253 nm
SMILES
ClC1=C(F)C(NC2=NC=NC3=C2C=C(OC(N4[C@H](C)CN(C)CC4)=O)C(OC)=C3)=CC=C1
InChi Code
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
InChi Key
MXDSJQHFFDGFDK-CYBMUJFWSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    10 mg

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    Product Description

    AZD 3759 is a brain penetrant inhibitor of wild-type and constitutively active mutant EGF receptors (EGFRs; IC50s = 0.3, 0.2, and 0.2 nM for wild-type, L858R-mutant, and exon 19 deletion-containing EGFRs, respectively).1 It is selective for EGFR over 115 other kinases, exhibiting <50% inhibition at a concentration of 1 μM. AZD 3579 reduces EGFR phosphorylation and cellular proliferation in L858R-mutant and exon 19 deletion-containing H3255 and PC-9 cells (GI50s = 7.7 and 7.0 nM, respectively) but has no effect on H838 cells that express wild-type EGFR (GI50 = 21,556 nM). AZD 3759 inhibits tumor growth by 78% and induces tumor regression at doses of 7.5 and 15 mg/kg, p.o., respectively in a PC-9 mouse model of non-small cell lung cancer (NSCLC) brain metastasis.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Zeng, Q., Wang, J., Cheng, Z., et al. Discovery and evaluation of clinical candidate AZD3759, a potent, oral active, central nervous system-penetrant, epidermal growth factor receptor tyrosine kinase inhibitor. J. Med. Chem. 58(20), 8200-8215 (2015).