PROTAC SOS1 degrader-10

PROTAC SOS1 degrader-10 (Compound 11o) is a degrader for son of sevenless 1 (SOS1) in a CRBN and proteasome dependent manner. PROTAC SOS1 degrader-10 degrades SOS1 in KRAS mutant cancer cells SW620, A549 and DLD-1, with DC50s of 2.23, 1.85 and 7.53 nM, respectively. PROTAC SOS1 degrader-10 inhibits the proliferations of cells SW620, A549 and DLD-1, with IC50s of 36.7, 52.2 and 107 nM, respectively. PROTAC SOS1 degrader-10 inhibits phosphorylation of ERK. (Pink: SOS1 ligand (HY-161655) ; Black: linker (HY-161656) ; Blue: E3 ligase ligand (HY-W249500) ) [1]

Product Specifications

CAS Number

[3043923-74-3]

UNSPSC

12352005

Target

PROTACs; Ras; SOS1

Type

Reference compound

Related Pathways

GPCR/G Protein; MAPK/ERK Pathway; PROTAC

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/protac-sos1-degrader-10.html

Solubility

10 mM in DMSO

Smiles

NC1=CC(C(F)(F)F)=CC([C@@H](C)NC2=C3C(N(C)C(C([C@H]4CC[C@H](C(N5CCN(CC6CCC7(CCN(C(C8=CC=C(OC)C(N9CCC(NC9=O)=O)=C8)=O)CC7)CC6)CC5)=O)CC4)=C3)=O)=NC=N2)=C1

Molecular Formula

C51H63F3N10O6

Molecular Weight

969.10

References & Citations

[1]Wang, K, et al. “Design, synthesis, and bioevaluation of SOS1 PROTACs derived from pyrido[2,3-d]pyrimidin-7-one-based SOS1 inhibitor.” Bioorganic & medicinal chemistry letters vol. 107 (2024) : 129780.