PD168393 is an irreversible EGFR inhibitor (IC50: 0.70 nM), irreversibly alkylate Cys-773; inactive against PKC, FGFR, PDGFR, and insulin.

EGFR:0.70 nM

PD 168393与EGFR TK的ATP结合位点对接。在持续暴露的条件下，PD168393彻底抑制了A431细胞中EGF依赖的受体自磷酸化作用，并且在移除化合物后8小时内仍持续抑制。PD168393以IC50为5.7 nM抑制MDA-MB-453细胞中hergulin诱导的酪氨酸磷酸化。对于胰岛素、PDGF和基础的FGFR TKs以及PKC，PD168393无活性。PD168393以IC50为1-6 nM抑制HS-27人类成纤维细胞中EGF介导的酪氨酸磷酸化，但对FGF或PDGF介导的酪氨酸磷酸化影响较小。[1] PD168393在3T3-Her2细胞中快速而有效地抑制Her2诱导的酪氨酸磷酸化，IC50约为100 nM。D168393还抑制了3T3-Her2细胞中PLCγ1/Stat1/Dok1/δ-catenin的磷酸化。[2]

PD 168393在赤裸鼠体内植入的A431人类表皮样癌移植瘤中显示出了115%的肿瘤生长抑制效果，同时EGFR的磷酸酪氨酸含量降低了50%。PD 168393在血浆中的浓度也较低。[1]

The effects of VU0364770 on rat mGlu1 and mGlu5 are assessed by using calcium mobilization and measuring the glutamate concentration-response relationship in the presence and absence of 10 μM VU0364770. Using a double-addition protocol, VU0364770 is added to the cells, followed 2.5 min later by a full concentration-response of glutamate. Shifts of the concentration-response relationship are used to assess potential potentiator (left shift of more than 2-fold) or antagonist (right shift of more than 2-fold or depression of the maximum response by at least 75%) activity of VU0364770. Compounds are further assessed for mGlu5 antagonist activity by performing a full concentration-response curve, starting at 30 μM and serially diluted it by using 1:3 dilutions, in the presence of an EC80 concentration of glutamate[1].