HJM-561

HJM-561 is a selective and effective orally active EGFR PROTAC degrader. HJM-561 is able to overcome the triple EGFR mutations that are resistant to Osimertinib (HY-15772) . HJM-561 exhibits potent degradation of EGFR Del19/T790M/C797S (DC50: 9.2 nM) and L858R/T790M/C797S (DC50: 5.8 nM), and has anti-tumor activity (pink: EGFR ligand (HY-12857) ; blue: CRBN ligand (HY-A0003) ; black: linker) [1].

Product Specifications

CAS Number

[2570251-68-0]

UNSPSC

12352005

Target

EGFR; PROTACs

Type

Reference compound

Related Pathways

JAK/STAT Signaling; PROTAC; Protein Tyrosine Kinase/RTK

Applications

COVID-19-immunoregulation

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/hjm-561.html

Purity

99.26

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C1C2=C(CN1C3C(NC(CC3)=O)=O)C(C#CCCN4CCN(C5CCN(CC5)C6=CC=C(C(OC)=C6)NC7=NC=C(C(NC8=C(P(C)(C)=O)C=CC=C8)=N7)Cl)CC4)=CC=C2

Molecular Formula

C45H51ClN9O5P

Molecular Weight

864.37

References & Citations

[1]Du Y, et al. HJM-561, a Potent, Selective, and Orally Bioavailable EGFR PROTAC that Overcomes Osimertinib-Resistant EGFR Triple Mutations. Mol Cancer Ther. 2022 Jul 5;21 (7) :1060-1066.