Product Name :
AZ5104
Description:
AZ5104 is a demethylated metabolite of AZD-9291. AZ-5104 was identified to exhibit 5-fold potency compared to AZD-9291, which is currently in clinical trial. AZ5104 is a potent EGFR inhibitor with IC50 of <1 nM, 6 nM, 1 nM, and 25 nM for EGFR (L858R/T790M), EGFR (L858R), EGFR (L861Q), and EGFR (wildtype), respectively.
CAS:
1421373-98-9
Molecular Weight:
485.58
Formula:
C27H31N7O2
Chemical Name:
N-(5-((4-(1H-indol-3-yl)pyrimidin-2-yl)amino)-2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxyphenyl)acrylamide
Smiles :
CN(C)CCN(C)C1=CC(OC)=C(C=C1NC(=O)C=C)NC1=NC(=CC=N1)C1=CNC2=CC=CC=C12
InChiKey:
IQNVEOMHJHBNHC-UHFFFAOYSA-N
InChi :
InChI=1S/C27H31N7O2/c1-6-26(35)30-22-15-23(25(36-5)16-24(22)34(4)14-13-33(2)3)32-27-28-12-11-21(31-27)19-17-29-20-10-8-7-9-18(19)20/h6-12,15-17,29H,1,13-14H2,2-5H3,(H,30,35)(H,28,31,32)
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
AZ5104 is a demethylated metabolite of AZD-9291.{{Trovafloxacin} site|{Trovafloxacin} Bacterial|{Trovafloxacin} Protocol|{Trovafloxacin} In Vitro|{Trovafloxacin} manufacturer|{Trovafloxacin} Epigenetic Reader Domain} AZ-5104 was identified to exhibit 5-fold potency compared to AZD-9291, which is currently in clinical trial.{{Pyrazinamide} MedChemExpress|{Pyrazinamide} Anti-infection|{Pyrazinamide} Technical Information|{Pyrazinamide} In Vivo|{Pyrazinamide} manufacturer|{Pyrazinamide} Autophagy} AZ5104 is a potent EGFR inhibitor with IC50 of Product information|CAS Number: 1421373-98-9|Molecular Weight: 485.PMID:25429455 58|Formula: C27H31N7O2|Synonym:|AZ-5104|metabolite of AZD9291|Demethylated AZ9291|AZ5104|AZ 5104|Chemical Name: N-(5-((4-(1H-indol-3-yl)pyrimidin-2-yl)amino)-2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxyphenyl)acrylamide|Smiles: CN(C)CCN(C)C1=CC(OC)=C(C=C1NC(=O)C=C)NC1=NC(=CC=N1)C1=CNC2=CC=CC=C12|InChiKey: IQNVEOMHJHBNHC-UHFFFAOYSA-N|InChi: InChI=1S/C27H31N7O2/c1-6-26(35)30-22-15-23(25(36-5)16-24(22)34(4)14-13-33(2)3)32-27-28-12-11-21(31-27)19-17-29-20-10-8-7-9-18(19)20/h6-12,15-17,29H,1,13-14H2,2-5H3,(H,30,35)(H,28,31,32)|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: Soluble in DMSO, not in water|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined.|HS Tariff Code: 382200|How to use|In Vitro:|AZ5104 inhibits EGFR phosphorylation with IC50s of 2, 1, 2, 53, and 33 nM in H1975 (EGFRL858R/T790M), PC-9VanR (EGFRExon 19 deletion/T790M), PC-9 (EGFRExon 19 deletion), H2073 (WT), and LOVO (WT), respectively. AZ5104 exhibits a reduced selectivity margin against wild-type EGFR when compared to AZD9291. AZ5104 display minimal off-target activity against other non-HER family kinases, but has the potential to target both HER2 and HER4 kinase activity.|In Vivo:|The metabolite, AZ5104 (5 mg/kg/day), is effective in shrinking tumors in both C/L858R and C/L+T mice.|References:|Liao BC, Lin CC, Yang JC. Second and third-generation epidermal growth factor receptor tyrosine kinase inhibitors in advanced nonsmall cell lung cancer. Curr Opin Oncol. 2015 Jan 21. [Epub ahead of print] PubMed PMID: 25611025.Stinchcombe TE. Recent advances in the treatment of non-small cell and small cell lung cancer. F1000Prime Rep. 2014 Dec 1;6:117. doi: 10.12703/P6-117. eCollection 2014. Review. PubMed PMID: 25580271; PubMed Central PMCID: PMC4251418.Steuer CE, Khuri FR, Ramalingam SS. The next generation of epidermal growth factor receptor tyrosine kinase inhibitors in the treatment of lung cancer. Cancer. 2014 Dec 17. doi: 10.1002/cncr.29139. [Epub ahead of print] PubMed PMID: 25521095.Products are for research use only. Not for human use.|
