Setidegrasib

Setidegrasib (KRAS G12D inhibitor 17, ASP3082) is a PROTAC KRAS degrader (DC50: 37 nM) . Setidegrasib induces the degradation of G12D-mutation KRAS protein. Setidegrasib suppresses p-ERK, p-AKT, p-S6 levels in AsPC-1 cells. Setidegrasib exhibits anti-tumor activity in various cancer xenograft models in mice. Setidegrasib can be used for the study of KRAS (G12D) -mutated solid tumors. (Blue: VHL ligase ligand (HY-168699) ; Black: linker (HY-168698) ; Pink: G12D ligand (HY-168700) ) [1][2].

Product Specifications

CAS Number

[2821793-99-9]

Product Name Alternative

ASP-3082; KRAS G12D inhibitor 17

UNSPSC

12352005

Target

Akt; ERK; PROTACs; Ras

Type

Reference compound

Related Pathways

GPCR/G Protein; MAPK/ERK Pathway; PI3K/Akt/mTOR; PROTAC; Stem Cell/Wnt

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

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

Purity

99.65

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

CC1=C(SC=N1)C2=CC=C(C=C2)[C@@H](NC([C@@H]3C[C@H](CN3C([C@H](C(C)C)N4C=C(N=N4)C5=CC=C(C=C5)COC6=[C@]([C@]7=C(C(F)=CC8=C7C=NN8)C)C(C9CC9)=CC%10=C6N=C(N=C%10N%11C[C@@H]%12C[C@H]%11CN%12)OC%13CCOCC%13)=O)O)=O)CO

Molecular Formula

C60H65FN12O7S

Molecular Weight

1117.30

References & Citations

[1]Yoshinari, et al. Preparation of quinazoline-linked (4R) -4-hydroxy-L-prolinamide compounds for inducing degradation of G12D-mutation KRAS protein: World Intellectual Property Organization, WO2022173032[P]. 2022-08-18.|[2]Yoshinari T, et al. Discovery of KRAS (G12D) selective degrader ASP3082. Commun Chem. 2025 Aug 23;8 (1) :254.