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MRTX1133

Name: MRTX1133
Brand: TargetMol
SKU: T9303
Price: 61 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T9303Cas No. 2621928-55-8

MRTX1133 is a KRAS G12D inhibitor (KD=0.2 pM) that is potent, selective, and non-covalent. MRTX1133 exhibits inhibitory activity against KRAS G12D-mutated tumors, but not against KRAS wild-type tumors.

MRTX1133

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Purity: 99.6%

Catalog No. T9303Cas No. 2621928-55-8

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$61	In Stock	In Stock
5 mg	$156	In Stock	In Stock
10 mg	$219	In Stock	In Stock
25 mg	$393	In Stock	In Stock
50 mg	$592	In Stock	In Stock
100 mg	$937	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$207	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products. If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.

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Batch Information

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Purity:99.6%

Appearance:Solid

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	MRTX1133 is a KRAS G12D inhibitor (KD=0.2 pM) that is potent, selective, and non-covalent. MRTX1133 exhibits inhibitory activity against KRAS G12D-mutated tumors, but not against KRAS wild-type tumors.
Targets&IC50	KRas (G12D):0.2 pM (Kd), KRas (G12D):< 2 nM
In vitro	METHODS: Human gastric cancer cells AGS (KRASG12D) and MKN1 (KRASWT) were treated with MRTX1133 (0-3 μM) for 72 h, and cell viability was measured by CTG method in 2D culture. RESULTS: The IC50 of MRTX1133 on AGS and MKN1 cells was 6 nM and >3000 nM, respectively. [1] METHODS: Human gastric cancer cells AGS (KRASG12D) were treated with MRTX1133 (0-10 μM) for 3-72 h, and the expression levels of target proteins were detected by In-Cell Western method. RESULTS: MRTX1133 inhibited the p-ERK level of AGS with an IC50 of 2 nM. [1] METHODS: Human pancreatic cancer cells SUIT2 (KRASG12D) were treated with MRTX1133 (60 nmol/L) for 24 h, and the expression levels of target proteins were detected by Western Blot. RESULTS: SUIT2 cells treated with MRTX1133 showed a significant decrease in pMEK1/2, a partial decrease in pERK1/2, and an initial decrease in pAKT followed by a recovery at a later time point. The levels of pEGFR and pHER2 decreased and recovered at 72 h. [2]
In vivo	METHODS: To test the antitumor activity in vivo, MRTX1133 (3-30 mg/kg, 10% Captisol in 50 mM citrate buffer pH 5.0) was intraperitoneally injected into nude-Foxn1nu mice bearing human pancreatic adenocarcinoma tumor Panc 04.03 twice daily for seven weeks. RESULTS: MRTX1133 exhibited dose-dependent antitumor activity, with 94% tumor growth inhibition observed at the 3 mg/kg group. Tumor regression of -62% and -73% was observed in the 10 mg/kg and 30 mg/kg groups, respectively. [1] METHODS: To assay antitumor activity in vivo, MRTX1133 (0.5 mg/kg in 12.5% Cremophor+12.5% ethanol+75%, orally once daily) and Cetuximab (50 mg/kg, intraperitoneally once weekly) were administered to BALB/c nude mice harboring human colorectal tumors, LS531 or CACO-2 for twenty-one days. RESULTS: MRTX1133 significantly inhibited tumorigenesis in both in vivo models. The anti-tumor effect was further enhanced when MRTX1133 was combined with Cetuximab. [3]

Chemical Properties

Molecular Weight	600.63
Formula	C₃₃H₃₁F₃N₆O₂
Cas No.	2621928-55-8
Smiles	Oc1cc(-c2ncc3c(nc(OC[C@@]45CCCN4C[C@H](F)C5)nc3c2F)N2C[C@@H]3CC[C@H](C2)N3)c2c(C#C)c(F)ccc2c1
Relative Density.	1.49 g/cm3 (Predicted)

Storage & Solubility Information

Storage

keep away from moisture | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 250 mg/mL (416.23 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 23 mg/mL (38.29 mM), Suspension.

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	1.6649 mL	8.3246 mL	16.6492 mL	83.2459 mL
5 mM	0.3330 mL	1.6649 mL	3.3298 mL	16.6492 mL
10 mM	0.1665 mL	0.8325 mL	1.6649 mL	8.3246 mL
20 mM	0.0832 mL	0.4162 mL	0.8325 mL	4.1623 mL
50 mM	0.0333 mL	0.1665 mL	0.3330 mL	1.6649 mL
100 mM	0.0166 mL	0.0832 mL	0.1665 mL	0.8325 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:

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