Nazartinib (EGF816)

Nazartinib (EGF816, NVS-816) is a covalent, irreversible, mutant-selective EGFR inhibitor that has nanomolar inhibitory potency against activating mt (L858R, ex19del) and T790M mt, with up to 60-fold selectivity over wild type (wt) EGFR in vitro.

Product information

CAS Number: 1508250-71-2

Molecular Weight: 495.02

Formula: C26H31ClN6O2

Chemical Name: N-(7-chloro-1-{1-[4-(dimethylamino)but-2-enoyl]azepan-3-yl}-1H-1,3-benzodiazol-2-yl)-2-methylpyridine-4-carboxamide

Smiles: CN(C)CC=CC(=O)N1CC(CCCC1)N1C(NC(=O)C2=CC(C)=NC=C2)=NC2C=CC=C(Cl)C1=2

InChiKey: IOMMMLWIABWRKL-YRNVUSSQSA-N

InChi: InChI=1S/C26H31ClN6O2/c1-18-16-19(12-13-28-18)25(35)30-26-29-22-10-6-9-21(27)24(22)33(26)20-8-4-5-15-32(17-20)23(34)11-7-14-31(2)3/h6-7,9-13,16,20H,4-5,8,14-15,17H2,1-3H3,(H,29,30,35)/b11-7+

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Solubility (25°C). 99 mg/mL(199.99 mM). Insoluble.

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:

Nazartinib (EGF816, NVS-816) is a covalent, irreversible, mutant-selective EGFR inhibitor that has nanomolar inhibitory potency against activating mt (L858R, ex19del) and T790M mt, with up to 60-fold selectivity over wild type (wt) EGFR in vitro.

In Vivo:

EGF816 is well tolerated and possesses favorable physicochemical properties and good oral bioavailability in mice. It shows moderate volume of distribution and low to moderate clearance in rodents (30% and 35% of rat and mouse liver blood flow, respectively). In the dog, EGF816 shows high clearance and high volume of distribution. EGF816 also demonstrates antitumor activity in an exon 20 insertion mutant model. At levels above efficacious doses, EGF816 treatment leads to minimal inhibition of WT EGFR and is well tolerated. In single-dose studies, EGF816 provides sustained inhibition of EGFR phosphorylation, consistent with its ability for irreversible binding. EGF816 has a longer half-life in human than mouse and is currently being evaluated in phase I/II clinical trials in patients harboring EGFR mutations, including T790M.

Products are for research use only. Not for human use.