PD158780

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PD 158780 可逆地抑制 ErbB 受体超家族所有四个成员的自身磷酸化和转磷酸化：EGFR、ErbB2、ErbB3 和 ErbB4（细胞测定中 IC50 值：8μM、49 nM、52 nM 和 52 nM）。

PD 158780 reversibly inhibits auto and transphosphorylation of all four members of the ErbB receptor superfamily: EGFR ErbB2 ErbB3 and ErbB4 (IC50s: 8μM 49 nM 52 nM and 52 nM in cell assay).

PD158780 inhibits EGF receptor autophosphorylation in A431 human epidermoid carcinoma with IC50 value of 13 nM. PD158780 is highly specific for the EGF receptor in Swiss 3T3 fibroblasts, inhibiting EGF-dependent receptor autophosphorylation and thymidine incorporation at low nanomolar concentrations while requiring micromolar levels for platelet-derived growth factor- and basic fibroblast growth factordependent processes. PD158780 inhibits heregulin-stimulated phosphorylation in the SK-BR-3 and MDAMB-453 breast carcinomas with IC50 values of 49 and 52 nM, respectively, suggesting that the compound is active against other members of the EGF receptor family.

PD158780 is active against clone formation in several breast tumors having different expression patterns of the ErbB family. PD158780 shows good therapeutic effect against the A431 epidermoid carcinoma when administered either intraperitoneally or orally. PD158780 produces measurable, significant effects against a mouse fibroblast transfected with human EGFR. PD158780 produces a significant therapeutic effect against the estrogendependent MCF-7 breast carcinoma at equitoxic dose levels.

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Angiogenesis

EGFR

EGFR| ErbB2| ErbB3| ErbB4

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171179-06-9

330.19

C14H12BrN5

>98% (HPLC)

DMSO: 30 mg/mL (90.86 mM); Ethanol: 8 mg/mL (24.23 mM)

CNc1cc2c(Nc3cccc(Br)c3)ncnc2cn1

4-N-(3-bromophenyl)-6-N-methylpyrido[34-d]pyrimidine-46-diamine

(-20℃)

With Ice Pack

≥ 2 years