PD158780

그림문자(GHS)

• 그림문자(GHS)

  

• 신호 어

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PD158780 화학적 특성, 용도, 생산

• 용도

  PD 158780 is a potent tyrosine kinase inhibitor of the epidermal growth factor receptor and has been shown to delay substantial growth of tumors in vivo tumor models.

• 일반 설명

  A potent inhibitor of the EGFR tyrosine kinase activity (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 NIH3T3 cells.

• 생물학적 활성

  Potent inhibitor of ErbB receptor family tyrosine kinases (IC 50 values are 0.008, 49 and 52 nM for EGFR, ErbB2 and ErbB2/ErbB4 respectively) that does not inhibit FGF or PDGF-mediated tyrosine phosphorylation. Induces G 1 cell cycle arrest in MCF10A cells and is antiproliferative in A431 human epidermal carcinoma cells.

PD158780 공급 업체

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