YJ1206
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 , a linker (HY-W004328), and a VHL E3 ubiquitin ligase (HY-W453548). (Pink: Navitoclax; Blue: VHL ligand; Black: linker).
Product Specifications
CAS Number
3053716-98-3
UNSPSC
12352211
Target
Apoptosis; CDK; PROTACs
Type
Reference compound
Related Pathways
Apoptosis; Cell Cycle/DNA Damage; PROTAC
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/yj1206.html
Purity
96.92
Solubility
DMSO : 66.67 mg/mL (ultrasonic)
Smiles
O=C(NCC1=CC=CC=C1)N(C2=CN=C(N3CCN(C4CCN(C5=C(F)C=C(C(N(C6CCC(NC6=O)=O)C7=O)=O)C7=C5)CC4)CC3)C=C2)[C@H](CC8)CC[C@@H]8NC9=NC=C%10C(C=CC=C%10)=N9
Molecular Formula
C49H52FN11O5
Molecular Weight
894.01
References & Citations
Shipping Conditions
Blue Ice
Storage Conditions
-20°C, 3 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
CDK12; CDK13
Available Sizes
Frequently Asked Questions
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