PROTAC KRAS G12D degrader 1

PROTAC KRAS G12D degrader 1 is a selective PROTAC KRASG12D degrader. PROTAC KRAS G12D degrader 1 inhibits proliferation of KRASG12D-mutant cells and suppresses ERK phosphorylation. PROTAC KRAS G12D degrader 1 inhibits tumor growth in mice bearing AsPC-1 xenografts. PROTAC KRAS G12D degrader 1 can be used for the study of KRASG12D-driven cancers. (Pink: KRAS ligand (HY-175892), Blue: VHL Ligand (HY-112078), Black: Linker, E3 ligase ligand-linker conjugate (HY-175893) ) [1].

Product Specifications

CAS Number

[3033583-54-6]

UNSPSC

12352005

Target

ERK; PROTACs; Ras

Type

Reference compound

Related Pathways

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

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/protac-kras-g12d-degrader-1.html

Purity

98.32

Solubility

DMSO : 10 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

FC1=C(CC)C2=C(C3=NC=C4C(N=C(OC[C@@H]5CCCN5CCCCOCC(N[C@@H](C(C)(C)C)C(N6[C@H](C(N[C@@H](C)C7=CC=C(C8=C(C)N=CS8)C=C7)=O)C[C@@H](O)C6)=O)=O)N=C4N9C[C@H]%10N[C@H](CC%10)C9)=C3F)C=C(O)C=C2C=C1

Molecular Formula

C59H72F2N10O7S

Molecular Weight

1103.33

References & Citations

[1]Zhou C, et al. Design, Synthesis, and Biological Evaluation of Potent and Selective PROTAC Degraders of Oncogenic KRASG12D. J Med Chem. 2024 Jan 10.