PTD10

PTD10 is a highly potent PROTAC BTK degrader (DC50: 0.5 nM, KD: 2.28 nM) . PTD10 degrades BTK in Ramos and JeKo-1 cells with DC50s of 0.5 and 0.6 nM respectively. PTD10 inhibits cell growth, and induces cell apoptosis via activation of the caspase-dependent pathway and mitochondrial pathway. PTD10 can be used for research of B-cell dysregulation. (Pink: Btk ligand (HY-19834) ; Blue: E3 ligase ligand (HY-14658) ; Black: linker (HY-Y0966) ; E3 ligase ligand + linker (HY-131717) ) [1].

Product Specifications

CAS Number

[2642231-19-2]

UNSPSC

12352005

Target

Btk; PROTACs

Type

Reference compound

Related Pathways

PROTAC; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/ptd10.html

Purity

97.38

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

O=C1N(C=C(C=C1NC2=NC=C(N3CCN(C[C@@H]3C)C(CNC4=CC=CC5=C4C(N(C5=O)C6CCC(NC6=O)=O)=O)=O)C=C2)C7=CC=NC(N8CCN9C(C8=O)=CC%10=C9CC(C)(C%10)C)=C7CO)C

Molecular Formula

C49H51N11O8

Molecular Weight

922.00

References & Citations

[1]Li YQ, et al. Discovery of Novel Bruton's Tyrosine Kinase PROTACs with Enhanced Selectivity and Cellular Efficacy. J Med Chem. 2023 Jun 8;66 (11) :7454-7474.