2676177-63-0
Chemical Structure
LUNA18
Synonym(s): Paluratide
- CAS No.: 2676177-63-0
- Formula:C73H105F5N12O12
- Molecular Weight:1437.68
InChIKey: ZQVKVYRBKAEFPD-DEBTURSASA-N
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
Biological Activity: 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].
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LUNA18 | 99.76% | 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. | ||||||||||||||||||||
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- [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. [Content Brief]
- [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. [Content Brief]
Keywords
