PROTAC K-Ras Degrader-4

SKU: orb3029073

Description

PROTAC K-Ras Degrader-4 (Compound 4) is a proteolysis-targeting chimera (PROTAC) molecule designed to selectively degrade oncogenic mutants of K-Ras, effectively degrading KRASG12D in the GP5d cell line and KRASG12V in SW620 cells with DC50 of 1 nM and 13 nM, respectively; it concomitantly inhibits the downstream MAPK signaling pathway and represents a novel therapeutic strategy for cancer research targeting previously undruggable Ras mutations.

Research Area

Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 2938169-99-2
• MW: 989.22
• Purity: 99.30% (May vary between batches)
• Formula: C₅₀H₆₀N₁₂O₆S₂
• SMILES: C[C@]1(C2=C(SC(N)=C2C#N)CCC1)C3=NC(=NO3)C4=NC(=NC=C4)N5[C@@H](C)CN(CCCCOC=6C=C([C@H](C(=O)N7[C@H](C(NCC8=CC=C(C=C8)C9=C(C)N=CS9)=O)C[C@@H](O)C7)C(C)C)ON6)CCC5
• Target: Ras,Kras,PROTACs
• Solubility: DMSO:80 mg/mL (80.87 mM)

Bioactivity

• In Vitro:
  PROTAC K-Ras Degrader-4 (0-1 μM, 5 days) was used to treat GP2d cell lines and was found to inhibit the expression of DUSP6 and the proliferation of GP2d cells with KRASG12D mutation.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PROTACKRasDegrader4

Quick Database Links

Gene Symbol

Ras,Kras,PROTACs