2. GPCR/G Protein MAPK/ERK Pathway Stem Cell/Wnt
  3. Ras ERK
  4. 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.

For research use only. We do not sell to patients.

Custom Peptide Synthesis

LUNA18 Chemical Structure

LUNA18 Chemical Structure

CAS No. : 2676177-63-0

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1 mg USD 1450 In-stock
5 mg USD 3980 In-stock
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Based on 1 publication(s) in Google Scholar

LUNA18 Related Antibodies

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K-Ras H-Ras N-Ras Ras

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ERK ERK1 ERK2 ERK5 ERK8

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Description

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].

IC50 & Target

IC50: <2 nM (KRASG12D-SOS)[1]
0.043 nM (KRASG12D)[1]
In Vitro

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

LUNA18 Related Antibodies

Cell Viability Assay[3]

Cell Line: NCI-H2122, MiaPaCa-2, NCI-H441, LS 180, GSU cell lines
Concentration: 0-1000 nM
Incubation Time: 7 days
Result: Inhibited the proliferation of NCI-H2122, MiaPaCa-2, NCI-H441, LS 180, GSU cell lines.

Western Blot Analysis[3]

Cell Line: NCI-H441
Concentration: 0-100 nM
Incubation Time: 4 h
Result: Decreased GTP-KRAS, pERK1/2 and pAKT expression in a concentration-dependent manner in NCI-H441.
In Vivo

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]

Route Dose (mg/kg) AUCinf (ng·h/mL) CL (mL/min/kg) Vss (L/kg) T1/2 (h) Cmax (ng/mL) Tmax (h) F (%)
Mouse IV 1 1700±100 9.8±0.4 2.6±0.5 5.5±0.9 - - -
Mouse PO 10 3600±200 - - 3.5±0.1 780±60 2.0±0 21±1
Rat IV 1 3400±400 5.0±0.7 0.96±0.07 5.2±0.4 - - -
Rat PO 10 7400±3600 - - 3.6±0.5 1800±400 2.0±0 22±11
Dog IV 0.3 4100±1100 1.3±0.4 0.99±0.17 14±3 - - -
Dog PO 0.3 2000±800 - - 15±2 190±60 2.0±0.8 47±9
Monkey IV 0.165 680±1.7 4.2±1.2 1.2±0.4 8.0±1.2 - - -
Monkey PO 3 3400±2300 - - 8.5±0.8 630±450 2.3±1.3 26±19

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: NCI-H441 xenograft mouse model
Dosage: 10 mg/kg
Administration: p.o., once daily for 14 days
Result: Resulted in antitumor activity without any marked body weight loss in NCI-H441 xenograft mouse model.
Molecular Weight

1437.68

Formula

C73H105F5N12O12
CAS No.
Appearance

Solid

Color

White to off-white

Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Sealed storage, away from moisture and light, under nitrogen

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (69.56 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.6956 mL 3.4778 mL 6.9557 mL
5 mM 0.1391 mL 0.6956 mL 1.3911 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.26%

COA (262 KB) RP-HPLC (366 KB) LCMS (108 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 0.6956 mL 3.4778 mL 6.9557 mL 17.3891 mL
5 mM 0.1391 mL 0.6956 mL 1.3911 mL 3.4778 mL
10 mM 0.0696 mL 0.3478 mL 0.6956 mL 1.7389 mL
15 mM 0.0464 mL 0.2319 mL 0.4637 mL 1.1593 mL
20 mM 0.0348 mL 0.1739 mL 0.3478 mL 0.8695 mL
25 mM 0.0278 mL 0.1391 mL 0.2782 mL 0.6956 mL
30 mM 0.0232 mL 0.1159 mL 0.2319 mL 0.5796 mL
40 mM 0.0174 mL 0.0869 mL 0.1739 mL 0.4347 mL
50 mM 0.0139 mL 0.0696 mL 0.1391 mL 0.3478 mL
60 mM 0.0116 mL 0.0580 mL 0.1159 mL 0.2898 mL
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LUNA18 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

LUNA182676177-63-0LUNA 18LUNA-18RasERKExtracellular signal regulated kinasesorally-availableKRASERK and RAS inhibitormouse xenograft modelcolon cancerstomach cancernon-small cell lung cancerpancreaticcancerInhibitorinhibitorinhibit

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