LUNA18 |
Catalog No.GC73607
One-Click Copy Product Info
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LUNA18 is an orally-available cyclic peptide KRAS and ERK inhibitor.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2676177-63-0
Sample solution is provided at 25 µL, 10mM.
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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.
LUNA18 (2 μmol/L, 36 h) robustly inhibits proliferation of NCI-H2122, MiaPaCa-2, NCI-H441, LS 180, GSU cell lines, which is a selective RAS inhibitor[3].LUNA18 (0-100 nM, 4 h) decreases GTP-KRAS, pERK1/2 and pAKT expression in a concentration-dependent manner in NCI-H441 cell lines[3].
LUNA18 (10 mg/kg, p.o., once daily for 14 days) results in dose-dependent antitumor activity without any marked body weight loss in NCI-H441 xenograft mouse model[3].PK parameters of LUNA18[3]
References:
[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.
| Cas No. | 2676177-63-0 | SDF | |
| Formula | C73H105F5N12O12 | M.Wt | 1437.68 |
| Solubility | DMSO : ≥ 100 mg/mL (69.56 mM) | Storage | Sealed storage, away from moisture and light, under nitrogen |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 695.6 μL | 3.4778 mL | 6.9557 mL |
| 5 mM | 139.1 μL | 695.6 μL | 1.3911 mL |
| 10 mM | 69.6 μL | 347.8 μL | 695.6 μL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >96.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)