best quality 1626387-80-1 Wholesaler 1626387-80-1 AZD-3759 Best price zorifertinib CAS NO.1626387-80-1

best quality 1626387-80-1 Wholesaler 1626387-80-1 AZD-3759 Best price zorifertinib

ZD 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). 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.

AZD3759 is a n orally available inhibitor of the epidermal growth factor receptor (EGFR), with potential antineoplastic activity. Upon oral administration, AZD3759 binds to and inhibits the activity of EGFR as well as certain mutant forms of EGFR.

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). 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. 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: A crystalline solid. Solubility: DMF: 10 mg/ml, DMSO: 10 mg/ml, Ethanol: 2 mg/ml. lambdamax: 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.