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324674

Sigma-Aldrich

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.

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Synonym(s):
EGFR Inhibitor, Cyclopropanecarboxylic acid-(3-(6-(3-trifluoromethyl-phenylamino)-pyrimidin-4-ylamino)-phenyl)-amide
Empirical Formula (Hill Notation):
C21H18F3N5O
CAS Number:
Molecular Weight:
413.40

Quality Level

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

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

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This Item
324673341608324832
vibrant-m

324674

EGFR Inhibitor

vibrant-m

324673

EGFR/ErbB-2 Inhibitor

vibrant-m

324832

EGFR Inhibitor II, BIBX1382

assay

≥97% (HPLC)

assay

≥97% (HPLC)

assay

≥97% (HPLC)

assay

≥97% (HPLC)

Quality Level

100

Quality Level

100

Quality Level

100

Quality Level

100

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

storage temp.

−20°C

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

solubility

ethanol: 25 mg/mL, DMSO: 50 mg/mL

solubility

methanol: 1 mg/mL, DMSO: 25 mg/mL

solubility

DMSO: 10 mg/mL

solubility

water: 1 mg/mL, DMSO: 25 mg/mL

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.

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

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Other Notes

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

Legal Information

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

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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Articles

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