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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.

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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539652324673341608
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.

Sigma-Aldrich

324674

EGFR Inhibitor

EGFR/ErbB-2 Inhibitor The EGFR/ErbB-2 Inhibitor, also referenced under CAS 179248-61-4, controls the biological activity of EGFR/ErbB-2. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Sigma-Aldrich

324673

EGFR/ErbB-2 Inhibitor

form

solid

form

solid

form

solid

form

solid

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

color

off-white

color

orange

color

off-white

color

off-white

solubility

ethanol: 25 mg/mL, DMSO: 50 mg/mL

solubility

DMSO: 20 mg/mL

solubility

methanol: 1 mg/mL, DMSO: 25 mg/mL

solubility

DMSO: 10 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 Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


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Articles

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AldeRed™ 588-A is a red fluorescent live cell probe that detects ALDH activity used to identify cancer stem cells and progenitor cells in culture. Cancer stem cells (CSCs) are subpopulations of cancer cells that can self-renew, generate diverse cells in the tumor mass, and sustain tumorigenesis. Some researchers believe that cancer arises from cancer stem cells that originate as a result of mutational hits on normal stem cells.

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