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 (HY-168658), a linker (HY-W004328), and a VHL E3 ubiquitin ligase (HY-W453548) . (Pink: Navitoclax; Blue: VHL ligand; Black: linker) [1].

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

[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.