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BMS-599626

CAS No. : 714971-09-2

MCE 站：BMS-599626

产品活性：BMS-599626 (AC480) 是一种选择性的口服生物利用度 HER1 和 HER2 抑制剂，其 IC₅₀ 分别为 20 和 30 nM。BMS-599626 对 HER4 的 IC₅₀ 值为 190 nM，对 VEGFR2、c-Kit、Lck、MEK 的抑制强度降低了100倍。BMS-599626抑制肿瘤细胞增殖，并有可能增加肿瘤对放疗的反应。

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

作用靶点：EGFR

In Vitro: BMS-599626 inhibits the proliferation of tumor cells that are dependent on HER1/HER2 signaling. BMS-599626 (0.03-8 μM; 1 huors) results in the inhibition of receptor autophosphorylation, as well as MAPK phosphorylation, with IC₅₀s of 0.3 ａnd 0.22 μM, respectively, in Sal2 cells which express a CD8HER2 fusion protein.
BMS-599626 abrogates HER1 ａnd HER2 signaling ａnd inhibited the proliferation of tumor cell lines that are dependent on these receptors, with IC₅₀ in the range of 0.24 to 1 μM.In GEO cells, HER1 phosphorylation is stimulated by treatment with EGF ａnd is inhibited by BMS-599626 (IC₅₀=0. 75 μM).There is also nearly complete inhibition of EGF-dependent MAPK (0. 8 μM) but only partial inhibition of AKT signaling.The latter likely reflects the activation of AKT by multiple upstream signals.Treatment of N87 cells with BMS-599626 leads to the inhibition of HER2 (0. 38 μM), which is expressed to a high level because of gene amplification, as well as MAPK ａnd AKT phosphorylation (0.35 μM for both).
At the molecular level, in HN-5 cells the agent inhibited the expression of pEGFR, pHER2, cyclins D ａnd E, pRb, pAkt, pMAPK, pCDK1 ａnd 2, CDK 6, ａnd Ku70 proteins. The drug also induced accumulation of cells in the G1 cell cycle phase, inhibited cell growth, enhanced radiosensitivity, ａnd prolonged the presence of γ-H AX foci up to 24 h after radiation.

In Vivo: BMS-599626 (60-240 mg/kg; p.o.; daily for 14 days) results in a dose-dependent inhibition of Sal2 tumor growth.
BMS599626 treatment results in the inhibition of GEO xenograft tumor growth when given once daily for 14 days. In addition to efficacy in the Sal2, GEO, ａnd KPL4 models, BMS-599626 has similar antitumor activity in other HER2 amplified xenograft models including the BT474 breast ａnd N87 gastric tumors, as well as other HER1-overexpressing non-small-cell lung tumors (A549 ａnd L2987).
BMS599626 given before ａnd during irradiation improved the radioresponse of HN5 tumors in vivo.

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