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Paluratide (LUNA18) is a reversible cyclic peptide KRAS inhibitor with the advantages of oral availability and cell permeability for the treatment of kras-mutant cancers, which inhibits cancer cell proliferation by phosphorylating ERK and AKT, and also inhibits the interaction of RAS with guanine nucleotide exchange factors (GEFs).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $1,180 | In Stock | |
5 mg | $3,280 | In Stock | |
10 mg | $4,450 | In Stock | |
25 mg | $6,620 | In Stock | |
50 mg | $8,930 | In Stock |
Description | Paluratide (LUNA18) is a reversible cyclic peptide KRAS inhibitor with the advantages of oral availability and cell permeability for the treatment of kras-mutant cancers, which inhibits cancer cell proliferation by phosphorylating ERK and AKT, and also inhibits the interaction of RAS with guanine nucleotide exchange factors (GEFs). |
Targets&IC50 | KRAS-mutant cell proliferation:0.17-2.9 nM, KRAS-SOS1:~0.5 nM |
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[1]. |
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 [1]. |
Alias | LUNA18, LUNA 18 |
Molecular Weight | 1437.68 |
Formula | C73H105F5N12O12 |
Cas No. | 2676177-63-0 |
Smiles | O=C1C2(NC(=O)[C@]3(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)[C@]6(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 |
Storage | keep away from moisture,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 80 mg/mL (55.65 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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