1. Protein Tyrosine Kinase/RTK PI3K/Akt/mTOR Apoptosis
  2. IGF-1R Insulin Receptor Akt Apoptosis
  3. GTx-134

GTx-134 是一种双胰岛素样生长因子 1 受体/胰岛素受体 (IGF-1R/IR) 抑制剂,其对 IGF-1R 和 IR 的 IC50 分别为 97 和 187 nM。GTx-134通过抑制 IGF-1R 的自磷酸化及其下游信号通路 (Akt),阻断肿瘤细胞的增殖与存活信号。GTx-134 对多发性骨髓瘤细胞系具有广谱抑制活性,并且可诱发敏感细胞凋亡 (apoptosis)。GTx-134 在 MM1.S 细胞移植的小鼠中显著抑制了肿瘤生长。GTx-134 与现有疗法 (如蛋白酶体制剂、免疫调节剂) 协同。GTx-134 可用于高危骨髓瘤研究。

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GTx-134

GTx-134 Chemical Structure

CAS No. : 1008448-19-8

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生物活性

GTx-134 is a dual insulin-like growth factor 1 receptor/insulin receptor (IGF-1R/IR) inhibitor with an IC50 values for IGF-1R and IR of 97 and 187 nM respectively. GTx-134 inhibits the autophosphorylation of IGF-1R and its downstream signaling pathway (Akt), thereby blocking the proliferation and survival signals of tumor cells. GTx-134 has broad-spectrum inhibitory activity against multiple myeloma cell lines and can induce apoptosis in sensitive cells. GTx-134 significantly inhibits tumor growth in mice with MM1.S cell transplantation. GTx-134 works in synergy with existing therapies (such as protease preparations, immunomodulators). GTx-134 can be used in high-risk myeloma research[1].

分子量

648.77

Formula

C33H40N6O6S

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
GTx-134
目录号:
HY-13312A
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