2. GPCR/G Protein MAPK/ERK Pathway Stem Cell/Wnt
  3. Ras ERK
  4. LUNA18

LUNA18  (Synonyms: Paluratide)

製品番号: HY-156002 純度: 99.76%
COA 取扱説明書 Technical Support

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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LUNA18

LUNA18 構造式

CAS 番号 : 2676177-63-0

容量 価格（税別） 在庫状況 数量
1 mg $1450 在庫あり
5 mg $3980 在庫あり
10 mg $5970 在庫あり
50 mg   お問い合わせ  
100 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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LUNA18 関連抗体

Top Publications Citing Use of Products

Ras アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
K-Ras H-Ras N-Ras Ras

ERK アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
ERK ERK1 ERK2 ERK5 ERK8

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  • 純度とドキュメンテーション

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製品説明

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]
体外実験

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 関連抗体

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.
体内実験

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.
臨床実験
分子量

1437.68

分子式

C73H105F5N12O12
CAS 番号
Appearance

Solid

Color

White to off-white

輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

polypeptide, sealed storage, away from moisture and light, under nitrogen

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

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)

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
10 mM 0.0696 mL 0.3478 mL 0.6956 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

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

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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション

純度: 99.76%

COA (262 KB) LCMS (95 KB) Elemental Analysis Report (119 KB)

取扱説明書 (2659 KB)
参考文献

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

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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:

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

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