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SIAIS562055

SIAIS562055 is a potent cereblon-based SOS1 PROTAC with a Kd of 95.9 nM. SIAIS562055 exhibits sustained degradation of SOS1 and inhibition of downstream ERK pathways. SIAIS562055 effectively blocked the binding of KRASG12C or KRASG12D to SOS1, with the IC50 values of 95.7 nM and 134.5 nM, respectively. SIAIS562055 exhibits potent anticancer activity. (Pink: SOS1 ligand (HY-168638) ; Black: linker (HY-W539874) ; Blue: E3 ligase ligand (HY-W076696) ) [1].

Product Specifications

UNSPSC

12352211

Target

PROTACs; Ras; SOS1

Type

Reference compound

Related Pathways

GPCR/G Protein; MAPK/ERK Pathway; PROTAC

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/siais562055.html

Smiles

COC1=CC2=C(C(N[C@@H](C3=CC(N)=CC(C(F)(F)F)=C3)C)=NC(C)=N2)C=C1OC4CCN(CC4)CCCCCCCCCCCCSC5=C6C(C(N(C6)C7C(NC(CC7)=O)=O)=O)=CC=C5

Molecular Formula

C49H62F3N7O5S

Molecular Weight

918.12

References & Citations

[1]Ziwei Luo, et al. Targeted Degradation of SOS1 Exhibits Potent Anticancer Activity and Overcomes Resistance in KRAS-Mutant Tumors and BCR-ABL-Positive Leukemia. Cancer Res. 2024 Oct 22.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

Cereblon; K-Ras

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