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Poziotinib

CAS No. : 1092364-38-9

MCE 站：Poziotinib

产品活性：HM781-36B 是一种口服活性，不可逆的泛 HER 抑制剂。HM781-36B 抑制 EGFR^wt、HER-2 和 HER-4 的 IC₅₀ 值分别为 3.2、5.3 和 23.5 nM，对突变的 EGFR，包括 EGFR^T790M 和 EGFR^L858R/T790M，IC₅₀ 值分别为 4.2 和 2.2 nM。具有良好的抗肿瘤活性。

研究领域：JAK/STAT Signaling  |  Protein Tyrosine Kinase/RTK  |  Apoptosis

作用靶点：EGFR  |  Apoptosis

In Vitro: The IC₅₀ levels of Poziotinib (HM781-36B) for N87 ａnd SNU216 were 0.001 ａnd 0.004 μM, respectively, which was 10-1000 fold lower than the IC₅₀ levels of other HER family TKIs. HM781-36B more potently inhibited the phosphorylation of HER family ａnd downstream proteins, ａnd induced apoptosis ａnd G1 arrest compared to ZD1839 or GW572016.
Poziotinib (HM781-36B) also shows excellent selectivity with other kinases with greater than 100- to 1,000- fold IC₅₀ values compared with EGFR family members. Poziotinib (HM781-36B) possesses a functional α,β‐unsaturated carbonyl group as Michael acceptor moiety at the C6 position that allows covalent modifications of the EGFR kinase domain active site.
The addition of HM781-36B induced potent growth inhibition in both DiFi cells with EGFR overexpression ａnd SNU-175 cells (IC₅₀=0.003 ａnd 0.005 μM, respectively). Furthermore, HM781-36B induced G1 arrest of the cell cycle ａnd apoptosis, ａnd reduced the levels of HER family ａnd downstream signaling molecules, pERK ａnd pAKT, as well as nonreceptor/cytoplasmic tyrosine kinase, BMX.

In Vivo: The growth of tumors in mice treated with HM781-36B alone or in combination with 5-FU was significantly inhibited compared with control mice, ａnd tumor volume in mice receiving coadministraion of HM781-36B ａnd 5-FU was smaller than tumor volume in mice receiving HM781-36B only.

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