Product Description: 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].
Applications: Cancer-Kinase/protease
Formula: C49H52FN11O5
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.
CAS Number: 3053716-98-3
Molecular Weight: 894.01
Compound Purity: 96.36
Research Area: Cancer
Solubility: DMSO : 66.67 mg/mL (ultrasonic)
Target: Apoptosis;CDK;PROTACs
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