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513035

PD 158780

Name: PD 158780
Brand: MM

A potent, cell-permeable, reversible, ATP-competitive inhibitor of the EGFR tyrosine kinase activity (IC₅₀ = 8 pM).

别名:

PD 158780, 4-[(3-Bromophenyl)amino]-6-(methylamino)-pyrido[3,4-d]pyridimine

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关于此项目

经验公式（希尔记法）:

C₁₄H₁₂BrN₅

化学文摘社编号:

171179-06-9

分子量:

330.18

UNSPSC Code:

12352200

NACRES:

NA.77

MDL number:

MFCD00942160

Assay:

≥95% (HPLC)

Form:

solid

Quality level:

100

Storage condition:

OK to freeze, protect from light

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属性

Quality Level

100

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem^®

storage condition

OK to freeze, protect from light

color

yellow

solubility

DMSO: 5 mg/mL

shipped in

ambient

storage temp.

−20°C

SMILES string

Brc1cc(ccc1)Nc2ncnc3c2cc(nc3)NC

InChI

1S/C14H12BrN5/c1-16-13-6-11-12(7-17-13)18-8-19-14(11)20-10-4-2-3-9(15)5-10/h2-8H,1H3,(H,16,17)(H,18,19,20)

InChI key

KFHMLBXBRCITHF-UHFFFAOYSA-N

说明

General description

A potent, cell-permeable, reversible, ATP-competitive inhibitor of the EGFR tyrosine kinase activity (IC₅₀ = 8 pM). Also inhibits heregulin-stimulated autophosphorylation in SK-BR-3 (IC₅₀ = 49 nM) and MDA-MB-453 (IC₅₀ = 52 nM) breast carcinomas. The inhibition is competitive and results from binding of the inhibitor at the ATP site of the enzymes. Inhibits the LPA-stimulated MAP kinase kinase 1/2 (MKK1/2) activation and EGFR tyrosine phosphorylation in HeLa and NIH 3T3 cells. A 10 mM (500 µg/151 µl) solution of PD 158780 (Cat. No. 513036) in DMSO is also available.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
EGFR tyrosine kinase

Product competes with ATP.

Reversible: yes

Target IC₅₀: 8 pM against EGFR tyrosine kinase activity; 49 nM, 52 nm, against heregulin-stimulated autophosphorylation in SK-BR-3 and MDA-MB-453 breast carcinomas, respectively

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze at -20°C. Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Cunnick, J.M., et al. 1998. J. Biol. Chem. 273, 14468.
Rewcastle, G.W., et al. 1998. J. Med. Chem.41, 742.

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

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全球贸易项目编号

货号	GTIN
513035-500UG	04055977198645