Cat. No.: HY-156002

LUNA18

(Synonyms: Paluratide)

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Based on 1 Customer Validation

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.

Purity: 99.76%
CAS No.: 2676177-63-0
Formula: C₇₃H₁₀₅F₅N₁₂O₁₂
Molecular Weight:1437.68

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)

LUNA18 Chemical Structure

CAS No.: 2676177-63-0

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target

IC50: <2 nM (KRAS^G12D-SOS)^[1]
0.043 nM (KRAS^G12D)^[1]

All Ras Isoforms :

All ERK Isoforms :

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.

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)	AUC_inf (ng·h/mL)	CL (mL/min/kg)	V_ss (L/kg)	T_1/2 (h)	C_max (ng/mL)	T_max (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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 2676177-63-0
Appearance Solid
Molecular Weight 1437.68
Formula C₇₃H₁₀₅F₅N₁₂O₁₂
Color White to off-white
Synonyms

Paluratide
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; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

0.6956 mL

3.4778 mL

6.9557 mL

5 mM

0.1391 mL

0.6956 mL

1.3911 mL

10 mM

0.0696 mL

0.3478 mL

0.6956 mL

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.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (1.74 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (1.74 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact

MedChemExpress (MCE) .

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (286 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

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. [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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Macrocyclic Compound Library

Peptide Library

Clinical Compound Library Plus

All Ras Isoforms

All ERK Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

LUNA18

Macrocyclic Compound Library

Peptide Library

Clinical Compound Library Plus

All Ras Isoforms

All ERK Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

LUNA18 Related Classifications

Cat. No.: HY-156002