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SCH772984 HCl

Name: SCH772984 HCl
Brand: TargetMol
SKU: T23337
Rating: 4.5 (1 reviews)

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Catalog No. T23337

SCH772984 HCl is a selective inhibitor of ERK1/2 that displays behaviors of both type I and type II kinase inhibitors, with IC50s of 4 and 1 nM, respectively. SCH772984 HCl has nanomolar cellular potency in tumor cells with mutations in BRAF, NRAS, or KRA

SCH772984 HCl

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Catalog No. T23337

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$95	Inquiry	Inquiry
5 mg	$135	Inquiry	Inquiry
10 mg	$198	Inquiry	Inquiry

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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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Product Introduction

Bioactivity

Description	SCH772984 HCl is a selective inhibitor of ERK1/2 that displays behaviors of both type I and type II kinase inhibitors, with IC50s of 4 and 1 nM, respectively. SCH772984 HCl has nanomolar cellular potency in tumor cells with mutations in BRAF, NRAS, or KRA
Targets&IC50	ERK1:4 nM, ERK2:1 nM
In vitro	In LOX BRAFV600E melanoma cells, SCH772984 HCl (3, 10, 30, 100, 300 nM; 24 hours) inhibited ERK and RSK phosphorylation. SCH772984 HCl showed EC50 values less than 500 nM in approximately 88% and 49% of BRAF-mutant (n=25) or RAS-mutant (n=35) tumor lines, respectively. In SCH772984 HCl-sensitive melanoma cells, SCH772984 HCl (300 nM; 24-48hours) resulted in a G1 arrest[1].
In vivo	In female nude mice bearing human LOX BRAFV600E tumors, SCH772984 HCl (12.5, 25, 50 mg/kg; i.p. twice daily for 14 days) lead to 98% tumor regression at all doses. Dose-dependent antitumor activity is also observed in the KRAS-mutant pancreatic MiaPaCa model, with 36% regression at 50 mg/kg twice daily. Importantly, tumor regression is accompanied by robust inhibition of ERK phosphorylation in tumor tissue[1].

Chemical Properties

Molecular Weight	624.14
Formula	C₃₃H₃₄ClN₉O₂
Smiles	O=C(NC1=CC2=C(NN=C2C3=CC=NC=C3)C=C1)[C@H]4CN(CC(N5CCN(C6=CC=C(C7=NC=CC=N7)C=C6)CC5)=O)CC4.[H]Cl
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

H2O: 23.5 mg/mL (37.65 mM), Sonication is recommended.

Solution Preparation Table

H2O

	1mg	5mg	10mg	50mg
1 mM	1.6022 mL	8.0110 mL	16.0220 mL	80.1102 mL
5 mM	0.3204 mL	1.6022 mL	3.2044 mL	16.0220 mL
10 mM	0.1602 mL	0.8011 mL	1.6022 mL	8.0110 mL
20 mM	0.0801 mL	0.4006 mL	0.8011 mL	4.0055 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