EGF816 free base · Synonyms: Nazartinib

Nazartinib is a covalent mutant-selective EGFR inhibitor.

For research use only. Not for human or veterinary use.

Target EGFR

Research area Cancer

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Data Sheet SDS COA

EGF816 structure

CAS No.: 1508250-71-2

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
100 mg	USD 400.00	BP-01896-100mg	In stock	Get quote
250 mg	USD 680.00	BP-01896-250mg	In stock	Get quote
500 mg	USD 1,050.00	BP-01896-500mg	In stock	Get quote
1 g	USD 1,650.00	BP-01896-1g	In stock	Get quote
5 g	Inquire	BP-01896-5g	Inquire	Inquire

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Description

Nazartinib (EGF816) is a covalent mutant-selective EGFR inhibitor, with Ki and Kinact of 31 nM and 0.222 min−1 on EGFR(L858R/790M) mutant, respectively.

Biological activity

In Vitro Nazartinib (EGF816) has inhibitory effect on the mutant cell lines with IC50s of 4, 6, 2 nM in H1975, H3255, and HCC827, respectively, and demonstrates improved ADME and PK properties. Nazartinib (EGF816) shows potent inhibition of pEGFR levels in H3255, HCC827, and H1975 cell lines with EC50 values of 5, 1, and 3 nM, respectively. Nazartinib inhibits cell proliferation, with EC50 values of 9, 11, and 25 nM in H3255, HCC827, and H1975, respectively. Nazartinib has an OC50 (compound concentration at 50% occupancy) value of 2 and 5 nM on HCC827 and H1975, respectively. In Vivo In H1975 mouse xenograft model, Nazartinib (EGF816; 50 and 20 mg/kg or 25 mg/kg, p.o.) demonstrates dose-dependent efficacy with near complete tumor cells regression at the highest dose tested (50 mg/kg). In H1975 mouse model, Nazartinib (EGF816; 10 mg/kg, p.o.) induces tumor growth inhibition with a T/C (tumor/control volume) of 29%, and when doses are 30 and 100 mg/kg, tumor regressions are achieved (T/C, -61% and -80%, respectively). In the H3255 xenograft model, Nazartinib (30 mg/kg, p.o.) shows significant antitumor activity. Antiproliferative activity of Nazartinib on 89 lung cancer cell lines indicates that Nazartinib selectively inhibits cell lines containing EGFR with catalytic domain mutations.

Identifiers

SMILES: CN(C)C\C=C\C(=O)N1CCCC[C@H](C1)N1C(NC(=O)C2=CC=NC(C)=C2)=NC2=C1C(Cl)=CC=C2
InChIKey: IOMMMLWIABWRKL-WUTDNEBXSA-N

Specifications

MW (average): 495.0160
Formula: C₂₆H₃₁ClN₆O₂
CAS No.: 1508250-71-2
Physical state: Solid
Color: off-white to yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

References

[1]. Lelais G, et al. Discovery of (R,E)-N-(7-Chloro-1-(1-[4-(dimethylamino)but-2-enoyl]azepan-3-yl)-1H-benzo[d]imidazol-2-yl)-2-methylisonicotinamide (EGF816), a Novel, Potent, and WT Sparing Covalent Inhibitor of Oncogenic (L858R, ex19del) and Resistant (T79

[2]. Jia Y, et al. EGF816 Exerts Anticancer Effects in Non-Small Cell Lung Cancer by Irreversibly and Selectively Targeting Primary and Acquired Activating Mutations in the EGF Receptor. Cancer Res. 2016 Mar 15;76(6):1591-602

Same target

Search EGFR

Same research area

Search Cancer