Eras-4001

Name: Eras-4001
Brand: TargetMol
SKU: T212829
Rating: 4.5 (1 reviews)

Catalog No. T212829 Copy Product Info

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Eras-4001 is a small-molecule pan-KRAS inhibitor capable of targeting both wild-type KRAS and various mutant forms simultaneously. Eras-4001 inhibits signaling between KRAS and effector proteins such as RAF, thereby blocking the activity of the RAS/MAPK pathway. In preliminary studies, this compound has demonstrated high affinity for KRAS (nano-molar IC₅₀) and induced tumor regression in multiple KRAS-mutant tumor models, indicating potential value for antitumor therapy.

Eras-4001

Copy Product Info

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Catalog No. T212829

Cas No. 3024878-19-8

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Product Introduction

Bioactivity

Description	Eras-4001 is a small-molecule pan-KRAS inhibitor capable of targeting both wild-type KRAS and various mutant forms simultaneously. Eras-4001 inhibits signaling between KRAS and effector proteins such as RAF, thereby blocking the activity of the RAS/MAPK pathway. In preliminary studies, this compound has demonstrated high affinity for KRAS (nano-molar IC₅₀) and induced tumor regression in multiple KRAS-mutant tumor models, indicating potential value for antitumor therapy.
Targets&IC50	H727 cells:3.51 nM, AsPC1 cells:1.78 nM, MKN1 cells:3.6 nM, SW620 cells:12.6 nM, LU99 cells:2.7 nM
In vivo	After 28 days of treatment with Eras-4001 (150 mg/kg, oral, twice daily), tumor volume suppression reached 97.2%, demonstrating a significant inhibitory effect on human colorectal cancer GP2D xenografts in mice.

Chemical Properties

Molecular Weight	743.19
Formula	C₃₆H₃₉ClF₄N₈O₃
Cas No.	3024878-19-8
Smiles	C(OC1=NC(=C2C(=N1)C[C@H](OC2)C3=C(C(F)(F)F)C(C#CC)=CC(N)=C3F)N4CC=5N(CCC4)N=C(C(N(C)C)=O)C5Cl)[C@@]67N(CC(=C)C6)CCC7
Relative Density.	no data available

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

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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:

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 DMSO TargetMol | 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 DMSO TargetMol | reagent stock solution to 400 μL PEG300 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 ddH₂O TargetMol | 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.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

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