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Cysmethynil

CAS No. : 851636-83-4

MCE 站：Cysmethynil

产品活性：Cysmethynil 是一种 Icmt 抑制剂（IC₅₀ = 2.4 μM）。Cysmethynil 抑制 RAS 膜结合和EGF的信号转导。Cysmethynil 将细胞周期阻滞在 G1 期，诱导细胞自噬。Cysmethynil 抑制 PC3 细胞增殖，与 Paclitaxel (HY-B0015) ａnd Doxorubicin (HY-15142A) 有协同作用。Cysmethynil 具有抗肿瘤作用，可用于实体瘤 (例如前列腺癌等) 研究。

研究领域：Autophagy  |  GPCR/G Protein

作用靶点：Autophagy  |  ICMT

In Vitro: Cysmethynil (15 μM or 20 μM or 30 μM; 6 days) inhibits Icmt^+/+ cells ａnd Icmt^-/-/ICMT cells proliferation, unaffects Icmt^-/-cells growth .
Cysmethynil (20-30 μM; 1-6 days) inhibits PC3 cells proliferation ａnd results in a dose- ａnd time-dependent reduction in the number of viable PC3 cells.

In Vivo: Cysmethynil (100 mg/kg, 200 mg/kg; intraperitoneal injection; every 48 h; 28 day) without adverse effects on mice body weight, significantly impacts on tumor growth, causes both an accumulation of cells in the G1 phase ａnd cell death .
Cysmethynil (20 mg/kg; intraperitoneal injection; three times a week; 2 weeks; alone or combined with Paclitaxel (HY-B0015)/ Doxorubicin (HY-15142A) ) is not toxic to mice ａnd induces only moderate inhibition of tumor growth as single agent, the combination with Paclitaxel(HY-B0015)/ Doxorubicin(HY-15142A) results in significantly greater efficacy in inhibiting tumor growth. Cysmethynil sensitizes cervical cancer cells to chemotherapy agent in xenograft mouse model.

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