SIAIS178

SIAIS178 is a potent and selective BCR-ABL degrader based on PROTAC technology with an IC50 of 24 nM. SIAIS178 causes effective degradation of BCR-ABL protein by recruiting Von Hippel-Lindau (VHL) E3 ubiquitin ligase. SIAIS178 has anticancer activity[1].

Product Specifications

CAS Number

[2376047-73-1]

UNSPSC

12352005

Target

Bcr-Abl; 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/siais178.html

Purity

99.36

Solubility

DMSO : 300 mg/mL (ultrasonic)

Smiles

O=C(N1CCN(C2=NC(C)=NC(NC3=NC=C(C(NC4=C(C=CC=C4Cl)C)=O)S3)=C2)CC1)CCCCCCC(N[C@@H](C(C)(C)C)C(N5[C@@H](C[C@@H](O)C5)C(NCC6=CC=C(C7=C(N=CS7)C)C=C6)=O)=O)=O

Molecular Formula

C50H62ClN11O6S2

Molecular Weight

1012.68

References & Citations

[1]Zhao Q, et al. Discovery of SIAIS178 as an Effective BCR-ABL Degrader by Recruiting Von Hippel-Lindau (VHL) E3 Ubiquitin Ligase. J Med Chem. 2019 Oct 24;62 (20) :9281-9298.