LUNA18

LUNA18 is an orally-available cyclic peptide KRAS and ERK inhibitor. LUNA18 phosphorylates ERK and AKT and decreases cell proliferation in RAS-mutated cancer cells. LUNA18 exhibits RAS signal inhibition and potent anti-cancer activities through inhibiting interaction between RAS and guanine nucleotide exchange factors (GEFs) in a mouse xenograft model. LUNA18 shows significant cellular efficacy against cell lines with KRAS genetic alterations, such as colon cancer, stomach cancer, non-small cell lung cancer and pancreaticcancer[1][2][3].

Product Specifications

CAS Number

[2676177-63-0]

Product Name Alternative

Paluratide

UNSPSC

12352209

Target

ERK; Ras

Type

Reference compound

Related Pathways

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

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/luna18.html

Purity

99.76

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

CC1=CC=C(C[C@@H](C(N(CC(N[C@H](C(N2CCC[C@H]2C(NC3(CCCC3)C(N(C)[C@H](C(N4C)=O)C5CCCC5)=O)=O)=O)CCC6=CC(F)=C(C(F)=C6)C(F)(F)F)=O)C)=O)N(C([C@@H]7CCN7C([C@H](C)N(C)C([C@H]([C@@H](C)CC)NC([C@H](CC(C)C)N(C)C(C[C@H]4C(N(C)C)=O)=O)=O)=O)=O)=O)CC)C=C1

Molecular Formula

C73H105F5N12O12

Molecular Weight

1437.68

References & Citations

[1]Tanada M, et al. Development of Orally Bioavailable Peptides Targeting an Intracellular Protein: From a Hit to a Clinical KRAS Inhibitor. J Am Chem Soc. 2023 Aug 2;145 (30) :16610-16620.|[2]Sase H, et al. Anti-tumor activity of orally-available cyclic peptide LUNA18 through direct RAS inhibition in RAS-altered tumors[J]. Cancer Research, 2024, 84 (6_Supplement) : 1654-1654.|[3]Ohta A, et al. Validation of a New Methodology to Create Oral Drugs beyond the Rule of 5 for Intracellular Tough Targets[J]. J Am Chem Soc. 2023 Nov 8;145 (44) :24035-24051.