Home Angiogenesis EGFR inhibitor Nazartinib (EGF816)

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Nazartinib (EGF816) EGFR inhibitor

Cat.No.S7824

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

Chemical Structure

Molecular Weight: 495.02

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Quality Control

Batch: Purity: 99.66%
99.66

Solubility

In vitro
Batch:

DMSO : 99 mg/mL (199.99 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 99 mg/mL

Water : Insoluble

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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 495.02 Formula

C26H31ClN6O2

 Storage (From the date of receipt)
CAS No. 1508250-71-2 Download SDF Storage of Stock Solutions

Synonyms NVS-816 SMILES CC1=NC=CC(=C1)C(=O)NC2=NC3=C(N2C4CCCCN(C4)C(=O)C=CCN(C)C)C(=CC=C3)Cl

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Mechanism of Action

Targets/IC50/Ki
mutant EGFR
0.031 μM(Ki)
In vitro
Nazartinib (EGF816) is a novel, covalent, mutant-selective EGFR inhibitor with nearly equipotent activity on both oncogenic (L858R and ex19del) and T790M-resistant mutations and good selectivity over WT EGFR. It potently inhibits the most common EGFR mutations L858R, Ex19del, and T790M in vitro. The cellular activity of this compound on EGFR mutants are assessed using three well-characterized cell lines, H3255, HCC827, and H1975, which harbor the L858R, Ex19del, and L858R/T790M mutations, respectively. After incubation with cells for 3 hours, it shows potent inhibition of pEGFR levels in H3255, HCC827, and H1975 with EC50 values of 5, 1, and 3 nmol/L, respectively. Cellular-based assays shows that EGF816 is selective toward mutant over WT EGFR.
In vivo
Nazartinib (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, this compound shows high clearance and high volume of distribution. It also demonstrates antitumor activity in an exon 20 insertion mutant model. At levels above efficacious doses, its treatment leads to minimal inhibition of WT EGFR and is well tolerated. In single-dose studies, it provides sustained inhibition of EGFR phosphorylation, consistent with its ability for irreversible binding. This compound 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.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-06-11)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03040973 ACTIVE_NOT_RECRUITING
Advanced Solid Tumors Which Are cMET-dependent
Novartis Pharmaceuticals
 2017-08-23 PHASE2
NCT03333343 ACTIVE_NOT_RECRUITING
EGFR-mutant Non-small Cell Lung Cancer
Novartis Pharmaceuticals
 2018-01-29 PHASE1
NCT03114319 TERMINATED
Advanced EGFR Mutant Non Small Cell LungCancer (NSCLC); KRAS G12-mutant NSCLC; Esophageal Squamous Cell Cancer (SCC); Head/Neck SCC; Melanoma; Advanced Gastrointestinal Stromal Tumors (GIST); Advanced NRAS/BRAFT wt Cutaneous Melanoma
Novartis Pharmaceuticals
 2017-05-26 PHASE1
NCT03516214 COMPLETED
Bronchial Neoplasms
University of Cologne
 2018-04-25 PHASE1
NCT03292133 TERMINATED
Lung Cancer
Massachusetts General Hospital
 2017-10-31 PHASE2
NCT02900664 COMPLETED
Colorectal Cancer, Triple Negative Breast Cancer, NSCLC - Adenocarcinoma
Novartis Pharmaceuticals
 2016-08-23 PHASE1

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