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Merck
CN

324674

EGFR Inhibitor

The EGFR Inhibitor, also referenced under CAS 879127-07-8, controls the biological activity of EGFR. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

别名:

EGFR Inhibitor, Cyclopropanecarboxylic acid-(3-(6-(3-trifluoromethyl-phenylamino)-pyrimidin-4-ylamino)-phenyl)-amide

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关于此项目

经验公式（希尔记法）:
C21H18F3N5O
化学文摘社编号:
879127-07-8
分子量:
413.40
MDL number:
MFCD13191284
UNSPSC Code:
12352200
NACRES:
NA.77

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产品名称

EGFR Inhibitor, The EGFR Inhibitor, also referenced under CAS 879127-07-8, controls the biological activity of EGFR. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

SMILES string

FC(F)(F)c1cc(ccc1)Nc2ncnc(c2)Nc3cc(ccc3)NC(=O)C4CC4

InChI

1S/C21H18F3N5O/c22-21(23,24)14-3-1-4-15(9-14)27-18-11-19(26-12-25-18)28-16-5-2-6-17(10-16)29-20(30)13-7-8-13/h1-6,9-13H,7-8H2,(H,29,30)(H2,25,26,27,28)

InChI key

YOHYSYJDKVYCJI-UHFFFAOYSA-N

assay

≥97% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

off-white

solubility

ethanol: 25 mg/mL
DMSO: 50 mg/mL

shipped in

ambient

storage temp.

−20°C

Quality Level

100

相关类别

Biochem/physiol Actions

Cell permeable: yes
Product competes with ATP.
Reversible: no
Target IC50: 21 nM, 63 nM, and 4 nM for EGFRwt, EGFRL858R and EGFRL861Q, respectively

Disclaimer

Toxicity: Standard Handling (A)

General description

A cell-permeable 4,6-dianilinopyrimidine compound that acts as a potent, ATP-competitive, and highly selective inhibitor of EGFR and some EGFR mutants (IC50 = 21 nM, 63 nM, and 4 nM for EGFRwt, EGFRL858R and EGFRL861Q, respectively) vs. erbB4/Her4 (IC50 = 7.64 µM) and a panel of 55 other kinases. Shown to completely block EGF-induced EGFR autophosphorylation in U-2OS cells at 10 µM.

Other Notes

Zhang, Q., et al. 2006. J. Am. Chem. Soc.128, 2182

Packaging

Packaged under inert gas

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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相关内容

Human Kinome & InhibitorSelect™ Libraries

Human Kinome Poster: The InhibitorSelect™ Protein Kinase Inhibitor Libraries provide broad coverage of the human kinome as shown here. The depicted human kinome dendrogram of 518 kinases are classified into five broad groups, 90 families, and 145 subfamilies. Inhibitor coverage was assigned based upon published data related to potency (IC50, EC50, Kd, etc.) for individual kinases harvested from the literature. Colored dots denote which library contains an inhibitor with demonstrated potent activity against the designated kinase and do not necessarily reflect known specificity of the inhibitor. Coverage of lipid and atypical kinases are depicted as a separate dendrogram. As shown, Calbiochem® Protein Kinase Inhibitor Libraries cover all major kinase families including TK, CMGC, CAMK, AGC, CK1, STE, TKL, as well as Lipid or Atypical kinase families.

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