CG 428

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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)。

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).

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Tyrosine Kinase

Trk Receptor

Trk receptor

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2412055-93-5

814.86

C43H43FN10O6

>98% (HPLC)

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O=C1C=2C(C(=O)N1C3C(=O)NC(=O)CC3)=CC=CC2NCCOCCC(=O)N4CCN(CC4)C=5N=C(C=CC5)C=6N7C(=NC6)C=CC(=N7)N8[C@H](CCC8)C9=CC(F)=CC=C9

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(-20℃)

With Ice Pack

≥ 2 years