| Hazard Information | Back Directory | [Uses]
YJ1206 is an orally active, selective CDK12/CDK13 PROTAC degrader with an IC50 of 12.55 nM for in VCaP cells. YJ1206 increases DNA damage, induces apoptosis, and promotes tumor regression in orthotopic WA74 patient-derived xenograft (PDX) mice models of resistant prostate cancer. YJ1206 suppresses tumor growth in vivo in conjunction with AKT pathway inhibitors. YJ1206 is composed of the CDK12/CDK13 degradation agent (HY-168658), a linker (HY-W004328), and a VHL E3 ubiquitin ligase (HY-W453548). (Pink: Navitoclax; Blue: VHL ligand; Black: linker)[1]. | [IC 50]
CDK12; CDK13 | [References]
[1] Yu Chang, et al. Development of an orally bioavailable CDK12/13 degrader and induction of synthetic lethality with AKT pathway inhibition. Cell Rep Med. 2024 Oct 15;5(10):101752. DOI:10.1016/j.xcrm.2024.101752 |
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| Company Name: |
Biorbyt Ltd.
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+44 (0)1223 859 353 |
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http://www.biorbyt.com |
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