EGF816 (mesylate)

Product Name: EGF816 (mesylate)
CAS No.: 1508250-72-3
Chemical Name: EGF816 (mesylate)
Synonyms: CS-2105;EGF816 (mesylate);Nazartinib mesylate);Nazartinib mesylate (EGF81);Nazartinib trifluoroacetate salt;EGF816 mesylate (EGF-816 mesylate;EGF-816 MESYLATE;NAZARTINIB MESYLATE;N-[7-chloro-1-[(3R)-1-[(E)-4-(dimethylamino)but-2-enoyl]azepan-3-yl]benzimidazol-2-yl]-2-methylpyridine-4-carboxamide
CBNumber: CB83041404
Molecular Formula: C27H35ClN6O5S
Formula Weight: 591.12
MOL File: 1508250-72-3.mol

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EGF816 (mesylate) Property

storage temp.: Store at -20°C
solubility: Soluble in DMSO

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Biorbyt Ltd

Product number: orb611621
Product name: EGF816 mesylate
Packaging: 100mg
Price: $912.9
Updated: 2021/12/16

Biorbyt Ltd

Product number: orb611621
Product name: EGF816 mesylate
Packaging: 250mg
Price: $1802
Updated: 2021/12/16

DC Chemicals

Product number: DC23179
Product name: EGF816mesylate
Purity: >98%
Packaging: 1g
Price: $2400
Updated: 2021/12/16

Crysdot

Product number: CD31003328
Product name: EGF816mesylate
Purity: 98+%
Packaging: 5mg
Price: $243
Updated: 2021/12/16

Crysdot

Product number: CD31003328
Product name: EGF816mesylate
Purity: 98+%
Packaging: 10mg
Price: $347
Updated: 2021/12/16

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EGF816 (mesylate) Chemical Properties,Usage,Production

Uses

Nazartinib mesylate (EGF816 mesylate) is a novel, covalent mutant-selective EGFR inhibitor, with Ki and Kinact of 31 nM and 0.222 min?1 on EGFR(L858R/790M) mutant, 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)^[1]. 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^[2].

IC 50

EGFR^L858R/T790M: 31 nM (Ki)

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 DOI:10.1021/acs.jmedchem.5b01985
[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 DOI:10.1158/0008-5472.CAN-15-2581

EGF816 (mesylate) Preparation Products And Raw materials

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EGF816 (mesylate) Suppliers

China 13 India 1 United States 7 Global 21

SPIRO PHARMA

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ShangHai Biochempartner Co.,Ltd

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TargetMol Chemicals Inc.

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InvivoChem

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Cckinase, Inc.

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Absin Bioscience Inc.

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1508250-72-3, EGF816 (mesylate)Related Search:

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EGF816 (mesylate)

CS-2105

EGF816 mesylate (EGF-816 mesylate

Nazartinib mesylate)

EGF-816 MESYLATE;NAZARTINIB MESYLATE

N-[7-chloro-1-[(3R)-1-[(E)-4-(dimethylamino)but-2-enoyl]azepan-3-yl]benzimidazol-2-yl]-2-methylpyridine-4-carboxamide

Nazartinib trifluoroacetate salt

Nazartinib mesylate (EGF81)

1508250-72-3

C27H35ClN6O5S