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BAY-293 is a potent inhibitor of Son of Sevenless 1 (SOS1) and blocks RAS activation via disruption of the KRAS-SOS1 interaction with an IC50 of 21 nM.
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GMB-475 is a PROTAC BCR-ABL1 degrader, overcomes BCR-ABL1-dependent drug resistance, targets BCR-ABL1 protein and recruits the E3 ligase Von Hippel Lindau.
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ARV-825 is a PROTAC, and acts as a potent BRD4 degrader, with Kds of 90 and 28 nM for BRD4 BD1 and BRD4 BD2, respectively.
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RG7112 is a potent, selective, first clinical and orally active MDM2-p53 inhibitor, with a KD of 11 nM for binding to MDM2.
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AMG 232 is a potent, selective and orally available inhibitor of p53-MDM2 interaction, with an IC50 of 0.6 nM. AMG 232 binds to MDM2 with a Kd of 0.045 nM.
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AAPK-25 is a potent and selective Aurora kinases and Polo-like Kinases (PLK) dual inhibitor, which shows anti-tumor activity.
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CP-10 is a PROTAC with highly selective, specific, and remarkable CDK6 degradation (DC50=2.1 nM), which has anti-cancer activity.
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MS31 is a highly selective spindlin 1 inhibitor, which inhibits the interactions between SPIN1 and H3K4me3. MS31 is not toxic to nontumorigenic cells.
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BI-4924 is a lipophilic and highly plasma protein bound selective phosphoglycerate dehydrogenase (PHGDH) inhibitor (IC50=3 nM) with excellent microsomal.
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BI-2852 is a potent KRAS inhibitor with nanomolar affinity and reduces pERK and pAKT levels in a dose-dependent manner in a KRAS mutant cell line NCI-H358.
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