LUNA18

SKU: orb2277774

Description

Paluratide (LUNA18) is an orally bioavailable, cell-permeable cyclic peptide that reversibly inhibits KRAS. It functions by blocking the RAS-GEF interaction and reducing ERK and AKT phosphorylation, thereby suppressing the proliferation of KRAS-mutant cancer cells in both in vitro and in vivo research models.

Research Area

Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 2676177-63-0
• MW: 1437.68
• Formula: C₇₃H₁₀₅F₅N₁₂O₁₂
• SMILES: O=C1C2(NC(=O)C3(N(C(=O)[C@H](CCC4=CC(F)=C(C(F)(F)F)C(F)=C4)NC(=O)CN(C)C(=O)[C@H](CC5=CC=C(C)C=C5)N(CC)C(=O)C6(N(C(=O)[C@H](C)N(C)C(=O)[C@]([C@H](CC)C)(NC(=O)[C@H](CC(C)C)N(C)C(=O)C[C@@H](C(N(C)C)=O)N(C)C(=O)[C@@H](N1C)C7CCCC7)[H])CC6)[H])CCC3)[H])CCCC2
• Target: Ras
• Solubility: DMSO:80 mg/mL (55.65 mM);10% DMSO+40% PEG300+5% Tween-80+45% Saline:3.3 mg/mL (2.3 mM)

Bioactivity

• Target IC50:
  KRAS-mutant cell proliferation:0.17-2.9 nM|KRAS-SOS1:~0.5 nM
• In Vivo:
  Paluratide shows 21% oral bioavailability in mice and, at 10 mg/kg daily, significantly suppresses tumor growth in KRAS-G12V xenograft models while reducing KRAS pathway activity, with no notable toxicity observed .
  Read more...
• In Vitro:
  Paluratide is a high-affinity cyclic peptide KRAS inhibitor that blocks KRAS/SOS1 interaction (IC₅₀ ≈ 0.5 nM). Paluratide inhibits proliferation in various KRAS-mutant cells (IC₅₀ = 0.17-2.9 nM) and reduces GTP-KRAS, pERK1/2, and pAKT levels significantly at 100 nM.
  Read more...

Storage & Handling

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

Alternative Names

LUNA 18, LUNA18

Compound Identifiers

PubChem CID

166509683