CAS 2378258-52-5

PROTAC K-Ras Degrader-1

CAS: 2378258-52-5

PROTAC K-Ras Degrader-1 is a PROTAC degrader based on the Cereblon E3 ligase ligand, capable of degrading K-Ras.

Formula: C₅₃H₆₂N₁₀O₁₀

Purezza: 98.05%

Colore e forma: Solid

Peso molecolare: 999.12

Ref: TM-T13844

Protac K-ras degrader-1

CAS: 2378258-52-5

PROTAC K-RAS degrader-1, a proteolysis-targeting chimera (PROTAC), is a potent and selective proteolysis-targeting chimera (PROTAC) designed to degrade the K-RAS G12C mutant protein. This heterobifunctional small molecule is composed of a cereblon (CRBN) E3 ligand that binds to the CRBN E3 ubiquitin ligase complex, a linker region, and a K-RAS-binding moiety that selectively recognizes and binds to the K-RAS G12C mutant protein. Upon binding to CRBN and K-RAS G12C, PROTAC K-RAS degrader-1 acts as a molecular glue, bringing the E3 ligase close to K-RAS, leading to its ubiquitination and subsequent proteasomal degradation. Preclinical studies have demonstrated its potent degradation efficacy in K-RAS G12C-driven cancer cell lines, leading to inhibition of cell proliferation and tumor regression in xenograft models, offering a promising therapeutic approach for the treatment of K-RAS-driven cancers by directly degrading the oncogenic driver K-RAS(G12C) protein.

Formula: C₅₃H₆₂N₁₀O₁₀

Purezza: Min. 95%

Peso molecolare: 999.1 g/mol

Ref: 3D-DVD25852