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Merck
CN

513033

PD 168393

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

别名:

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

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关于此项目

经验公式(希尔记法):
C17H13BrN4O
化学文摘社编号:
分子量:
369.22
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
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Quality Segment

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

SMILES string

Brc1cc(ccc1)Nc2ncnc3c2cc(cc3)NC(=O)C=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.

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

Preparation Note

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

Disclaimer

Toxicity: Standard Handling (A)


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存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



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