EGF816

ChemicalBook > CAS DataBase List > EGF816

Product Name: EGF816
CAS No.: 1508250-71-2
Chemical Name: EGF816
Synonyms: EGF816;CS-1646;NVS-816;Nazartinib;EGF-816;EGF 816;EGF816 Nazartinib;Nazartinib (EGF816);Nazartinib (EGF816, NVS-816);EGF816, 98%, a novel EGFR inhibitor;(R,E)-N-(7-chloro-1-(1-(4-(dimethylamino)but-2-enoyl)azepan-3-yl)-1H-benzo[d]imidazol-2-yl)-2-methylisonicotinamide
CBNumber: CB33040785
Molecular Formula: C26H31ClN6O2
Formula Weight: 495.02
MOL File: 1508250-71-2.mol

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EGF816 Property

Density: 1.28±0.1 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: Soluble in DMSO
form: Powder
pka: 11.38±0.43(Predicted)

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 22409
Product name: Nazartinib
Purity: ≥98%
Packaging: 1mg
Price: $37
Updated: 2024/03/01

Cayman Chemical

Product number: 22409
Product name: Nazartinib
Purity: ≥98%
Packaging: 5mg
Price: $161
Updated: 2024/03/01

Cayman Chemical

Product number: 22409
Product name: Nazartinib
Purity: ≥98%
Packaging: 10mg
Price: $283
Updated: 2024/03/01

Cayman Chemical

Product number: 22409
Product name: Nazartinib
Purity: ≥98%
Packaging: 25mg
Price: $599
Updated: 2024/03/01

ChemScene

Product number: CS-4325
Product name: Nazartinib
Purity: 99.57%
Packaging: 50mg
Price: $650
Updated: 2021/12/16

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EGF816 Chemical Properties,Usage,Production

Description

Nazartinib is an irreversible inhibitor of mutant EGF receptors (EGFRs). It is selective for EGFR mutant cell lines, including H3255 and HCC827 lung adenocarcinoma cells (IC₅₀s = 6.11 and 1.52 nM, respectively) and resistant H1975 non-small cell lung cancer cells (NSCLC; IC₅₀ = 4.18 nM), over cells expressing wild-type EGFRs (IC₅₀ = 160.6 nM for HaCaT keratinocytes). Nazartinib decreases phosphorylation of EGFR in H3255, HCC827, and H1975 cells (EC₅₀s = 5, 1, and 3 nM, respectively) and inhibits cell proliferation (EC₅₀s = 9, 11, and 25 nM, respectively) but does not affect cell proliferation in cell lines containing wild-type EGFR. It reduces tumor growth in an HCC827 lung adenocarcinoma mouse xenograft model when administered at doses ranging from 3 to 100 mg/kg per day for 21 days.

in vitro

egf816 showed sustained inhibition of pegfr, which is consistent with the irreversible binding mechanism of egf816. egf816 also performs exceptionally well in long term dosing studies providing durable responses in the preclinical models [1].

in vivo

egf816 demonstrated strong in vivo tumor regressions in several egfr activating and resistant tumor models. in all of the models egf816 inhibited tumor growth dose-dependently and achieved regressions of established tumors at well tolerated doses [1].

References

[1] shailaja kasibhatla, jie li, celin tompkins, mei-ting vaillancourt, jennifer anderson, annemarie culazzo pferdekamper, chun li, oliver long, mathew mcneill, robert epple, debbie liao, eric murphy, steve bender, yong jia, gerald lelais. egf816, a novel covalent inhibitor of mutant-selective epidermal growth factor receptor, overcomes t790m-mediated resistance in nsclc. [abstract]. in: proceedings of the 105th annual meeting of the american association for cancer research; 2014 apr 5-9; san diego, ca. philadelphia (pa): aacr; cancer res 2014;74(19 suppl):abstract nr 1733. doi:10.1158/1538-7445.am2014-1733

EGF816 Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from EGF816 manufacturers

Career Henan Chemical Co

Product: EGF816 1508250-71-2
Price: US $9.80/KG
Min. Order: 1g
Purity: ≥99%
Supply Ability: 100kg
Release date: 2020-01-08

1508250-71-2, EGF816Related Search:

EGF816 (S-enantiomer) Olmutinib XL-647 Genistein AZD 3759 AG 1478 HYDROCHLORIDE OSI-420 Anlotinib Tucatinib Neratinib Poziotinib (HM781-36B) CO-1686 Dacomitinib (PF299804) AZD-9291

Nazartinib (EGF816)

EGF816, 98%, a novel EGFR inhibitor

EGF816

Nazartinib

NVS-816

Nazartinib (EGF816, NVS-816)

(R,E)-N-(7-chloro-1-(1-(4-(dimethylamino)but-2-enoyl)azepan-3-yl)-1H-benzo[d]imidazol-2-yl)-2-methylisonicotinamide

EGF816 Nazartinib

CS-1646

EGF-816;EGF 816

N-[7-Chloro-1-[(3R)-1-[(2E)-4-(dimethylamino)-1-oxo-2-buten-1-yl]hexahydro-1H-azepin-3-yl]-1H-benzimidazol-2-yl]-2-methyl-4-pyridinecarboxamide

4-Pyridinecarboxamide, N-[7-chloro-1-[(3R)-1-[(2E)-4-(dimethylamino)-1-oxo-2-buten-1-yl]hexahydro-1H-azepin-3-yl]-1H-benzimidazol-2-yl]-2-methyl-

1508250-71-2