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513033

Sigma-Aldrich

PD 168393

A potent, cell-permeable, irreversible, ATP-competitive and selective inhibitor of EGF receptor (EGFR) tyrosine kinase activity (IC₅₀ = 700 pM).

Synonym(s):

PD 168393, 4-[(3-Bromophenyl)amino]-6-acrylamidoquinazoline

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About This Item

Empirical Formula (Hill Notation):
C17H13BrN4O
CAS Number:
194423-15-9
Molecular Weight:
369.22
MDL number:
MFCD02179207
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

100

Assay

≥98% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

yellow

solubility

DMSO: 200 mg/mL

shipped in

ambient

storage temp.

−20°C

InChI

1S/C17H13BrN4O/c1-2-16(23)21-13-6-7-15-14(9-13)17(20-10-19-15)22-12-5-3-4-11(18)8-12/h2-10H,1H2,(H,21,23)(H,19,20,22)

InChI key

HTUBKQUPEREOGA-UHFFFAOYSA-N

General description

A potent, cell-permeable, irreversible, ATP-competitive and selective inhibitor of EGF receptor (EGFR) tyrosine kinase activity (IC50 = 0.70 nM). Does not inhibit other protein kinases. Acts by binding to the catalytic domain of the EGFR with a 1:1 stoichiometry and alkylating Cys773. Excellent antitumor agent in vivo.
A potent, cell-permeable, irreversible, ATP-competitive and selective inhibitor of EGF receptor (EGFR) tyrosine kinase activity (IC50 = 700 pM). Does not inhibit other protein kinases. Acts by binding to the catalytic domain of the EGFR with a 1:1 stoichiometry and alkylating Cys773. Excellent antitumor agent in vivo.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
EGFR
Product competes with ATP.
Reversible: no
Target IC50: 700 pM against EGFR

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C. Avoid freeze/thaw cycles of solutions.

Other Notes

Fry, D.W., et al. 1998. Proc. Natl. Acad. Sci USA 95, 12022.

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

Regulatory Listings

Regulatory Listings are mainly provided for chemical products. Only limited information can be provided here for non-chemical products. No entry means none of the components are listed. It is the user’s obligation to ensure the safe and legal use of the product.

JAN Code

513033-15MG:
513033-VMG:
513033-1MG:

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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