AZD 3759

AZD 3759

CAT N°: 19931
Price:

From 48.00 40.80

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).{41251} It is selective for EGFR over 115 other kinases, exhibiting 50s = 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.

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