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RMC5127

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Catalog No. T204085Cas No. 3056146-38-1
Alias RMC-5127, RMC 5127

RMC5127 is an orally available, mutation-selective RAS G12V inhibitor exhibiting central nervous system (CNS) and brain permeability. It suppresses the RAS pathway and induces apoptosis in KRAS G12V mutant cancer cells, demonstrating antitumour activity.

RMC5127

RMC5127

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Purity: 99.96%
Catalog No. T204085Alias RMC-5127, RMC 5127Cas No. 3056146-38-1
RMC5127 is an orally available, mutation-selective RAS G12V inhibitor exhibiting central nervous system (CNS) and brain permeability. It suppresses the RAS pathway and induces apoptosis in KRAS G12V mutant cancer cells, demonstrating antitumour activity.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$396-In Stock
5 mg$993-In Stock
10 mg$1,590-In Stock
25 mg$3,360-In Stock
50 mg$4,970-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.96%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
RMC5127 is an orally available, mutation-selective RAS G12V inhibitor exhibiting central nervous system (CNS) and brain permeability. It suppresses the RAS pathway and induces apoptosis in KRAS G12V mutant cancer cells, demonstrating antitumour activity.
In vitro
In a panel of human cancer cell lines harboring the KRASG12V mutation, RMC5127 significantly suppressed RAS pathway activity, inhibited cell proliferation, and induced cell apoptosis; however, in a panel of K/N/HRAS wild-type cancer cell lines, this drug only exerted a submaximal inhibitory effect [1].
In vivo
Following repeated oral administration of RMC5127 to subcutaneous cell line-derived xenograft (CDX) models and patient-derived xenograft (PDX) models of non-small cell lung cancer (NSCLC), pancreatic ductal adenocarcinoma (PDAC), and colorectal cancer (CRC) harboring the KRASG12V mutation, significant and durable antitumor activity was observed. In the whole brain tissues of naïve mice (tumor-free mice), dose-dependent exposure of RMC5127 was detected, indicating that this compound possesses blood-brain barrier penetration ability [1].
SynonymsRMC-5127, RMC 5127
Chemical Properties
Molecular Weight1062.32
FormulaC57H75N9O9S
Cas No.3056146-38-1
SmilesC[C@H](OC)C(N=C1)=[C@@]([C@@]2=C(CC(C)(C)COC([C@H]3NN(C([C@@H](NC([C@H]4OC[C@@H]4C)=O)[C@H]5N6CC7(COC7)C6)=O)C8CC3C8)=O)C9=C(C=CC(C%10=CSC5=N%10)=C9)N2CCOC%11CCOCC%11)C=C1N%12CCN(C%13CC%13)CC%12
Relative Density.no data available
Storage & Solubility Information
StorageIn solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 100 mg/mL (94.13 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM0.9413 mL4.7067 mL9.4134 mL47.0668 mL
5 mM0.1883 mL0.9413 mL1.8827 mL9.4134 mL
10 mM0.0941 mL0.4707 mL0.9413 mL4.7067 mL
20 mM0.0471 mL0.2353 mL0.4707 mL2.3533 mL
50 mM0.0188 mL0.0941 mL0.1883 mL0.9413 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
% DMSO
%
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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