1. Neuronal Signaling Protein Tyrosine Kinase/RTK
  2. Trk Receptor
  3. CG428

CG428 是一种有效的、选择性的原肌球蛋白受体激酶 (TRK) 降解剂,具有抗肿瘤活性。CG428 降低 KM12 结直肠癌细胞中原肌球蛋白 3 (TPM3)-TRKA 融合蛋白的水平 (DC50 = 0.36 nM),并抑制下游 PLCγ1 磷酸化 (IC50 = 0.33 nM)。CG428 对 TRKA 的结合亲和力高于 TRKB 和 TRKC(Kd 分别为 1 nM、28 nM 和 4.2 nM)。此外,CG428 能有效抑制 KM12 细胞生长 (IC50 = 2.9 nM)。

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CG428 Chemical Structure

CG428 Chemical Structure

CAS No. : 2412055-93-5

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生物活性

CG428 is a potent and selective tropomyosin receptor kinase (TRK) degrader that has anti-tumor activity. CG428 reduces levels of the tropomyosin 3 (TPM3)-TRKA fusion protein in KM12 colorectal carcinoma cells (DC50 = 0.36 nM) and inhibits downstream PLCγ1phosphorylation (IC50 = 0.33 nM). CG428 has a higher binding affinity for TRKA than TRKB and TRKC (Kd = 1 nM, 28 nM and 4.2 nM, respectively). In addition, CG428 effectively inhibits KM12 cell growth (IC50 = 2.9 nM)[1].

分子量

814.86

Formula

C43H43FN10O6

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.

纯度 & 产品资料
参考文献
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  • 稀释计算器

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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:
CG428
目录号:
HY-137465
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