CG428 is a potent CRBN-dependent PROTAC degrader specifically targeting tropomyosin receptor kinase (TRK). It effectively reduces levels of the TPM3-TRKA fusion protein in KM12 colorectal carcinoma cells with a DC50 of 0.36 nM and inhibits downstream PLCγ1 phosphorylation with an IC50 of 0.33 nM. CG428 demonstrates higher binding affinity for TRKA (Kd = 1 nM) compared to TRKB and TRKC, making it a valuable tool for research into colorectal carcinoma.
CG428 is a potent CRBN-dependent PROTAC degrader specifically targeting tropomyosin receptor kinase (TRK). It effectively reduces levels of the TPM3-TRKA fusion protein in KM12 colorectal carcinoma cells with a DC50 of 0.36 nM and inhibits downstream PLCγ1 phosphorylation with an IC50 of 0.33 nM. CG428 demonstrates higher binding affinity for TRKA (Kd = 1 nM) compared to TRKB and TRKC, making it a valuable tool for research into colorectal carcinoma.
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