Shopping Cart

Your shopping cart is currently empty

MRTX-1257

Name: MRTX-1257
Brand: TargetMol
SKU: T16143
Price: 58 USD
Availability: InStock
Rating: 5 (10 reviews)

😃Good

Catalog No. T16143Cas No. 2206736-04-9

MRTX-1257 is a selective, irreversible, and covalent inhibitor of KRAS G12C with an IC50 of 900 pM for KRAS-dependent ERK phosphorylation in H358 cells. MRTX-1257 demonstrated 31% bioavailability in the mouse, with free fraction exposures well above cellular potency, and 77% target engagement in a PK/PD experiment.

MRTX-1257

😃Good

Purity: 99.07%

Catalog No. T16143Cas No. 2206736-04-9

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$58	In Stock	In Stock
2 mg	$82	In Stock	In Stock
5 mg	$133	In Stock	In Stock
10 mg	$217	In Stock	In Stock
25 mg	$391	In Stock	In Stock
50 mg	$569	In Stock	In Stock
100 mg	$826	-	In Stock
200 mg	$1,090	-	In Stock
1 mL x 10 mM (in DMSO)	$178	In Stock	In Stock

Add to Cart

Add to Quotation

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.

Questions

Batch Information

Select Batch

Purity:99.07%

Appearance:Solid

Color:White to Yellow

Resource Download

COA HNMR HPLC

Product Introduction

Bioactivity

Description	MRTX-1257 is a selective, irreversible, and covalent inhibitor of KRAS G12C with an IC50 of 900 pM for KRAS-dependent ERK phosphorylation in H358 cells. MRTX-1257 demonstrated 31% bioavailability in the mouse, with free fraction exposures well above cellular potency, and 77% target engagement in a PK/PD experiment.
In vivo	MRTX-1257 shows sustained regression at 3,10, 30, and 100 mg/kg dose groups. MRTX-1257 dosed of 100 mg/kg daily causes complete responses that are maintained >70 days after cessation of treatment. MRTX-1257 (1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg and 100 mg/kg, orally, daily for 30 days) displays rapid tumor growth inhibition at all dose groups in MIA PaCa-2 G12C Xenograft model in mice .

Chemical Properties

Molecular Weight	565.71
Formula	C₃₃H₃₉N₇O₂
Cas No.	2206736-04-9
Smiles	CN1CCC[C@H]1COc1nc2CN(CCc2c(n1)N1CCN([C@@H](CC#N)C1)C(=O)C=C)c1cccc2cccc(C)c12
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.

Solubility Information

DMSO: 35 mg/mL (61.87 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.54 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.7677 mL	8.8385 mL	17.6769 mL	88.3845 mL
5 mM	0.3535 mL	1.7677 mL	3.5354 mL	17.6769 mL
10 mM	0.1768 mL	0.8838 mL	1.7677 mL	8.8385 mL
20 mM	0.0884 mL	0.4419 mL	0.8838 mL	4.4192 mL
50 mM	0.0354 mL	0.1768 mL	0.3535 mL	1.7677 mL

Calculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Molecular Weight Calculator

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