2. PROTAC Neuronal Signaling Protein Tyrosine Kinase/RTK
  3. PROTACs Trk Receptor
  4. CG428

CG428 是一种有效的、选择性的原肌球蛋白受体激酶 (TRK) PROTAC 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)。(Pink: TRK inhibitor (HY-118271); Black: linker (HY-W067489); Blue: CRBN Ligand (HY-41547))

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CG428 Chemical Structure

CG428 Chemical Structure

CAS No. : 2412055-93-5

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CG428 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

查看所有亚型
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

查看 Trk Receptor 亚型特异性产品:

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TrkA TrkB TrkC Trk

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CG428 is a potent and selective tropomyosin receptor kinase (TRK) PROTAC 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].(Pink: TRK inhibitor (HY-118271); Black: linker (HY-W067489); Blue: CRBN Ligand (HY-41547))

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
KM12 IC50
52 nM
Compound: 6; CG428
Antiproliferative activity against human KM12 cells assessed as reduction in cell viability measured after 3 days by Celltiter-Glo assay
Antiproliferative activity against human KM12 cells assessed as reduction in cell viability measured after 3 days by Celltiter-Glo assay
[PMID: 33058680]
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

CG428 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • 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.

Keywords:

CG4282412055-93-5CG 428CG-428PROTACsTrk ReceptorTropomyosin related kinase receptorTPM3-TRKATRK degraderKM12pPLCγ1TRKATRKBTRKCanti-tumorInhibitorinhibitorinhibit

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目录号：
HY-137465
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