Shopping Cart

Your shopping cart is currently empty

Darizmetinib

Name: Darizmetinib
Brand: TargetMol
SKU: T72956
Price: 66 USD
Availability: InStock
Rating: 5 (10 reviews)

(Synonyms: HRX215, HRX-0215) Copy Product Info

🥰Excellent

Synonyms: HRX215, HRX-0215

Catalog No. T72956 Copy Product Info

Purity: 99.57%

🥰Excellent

Darizmetinib (HRX215, HRX-0215) is a small-molecule inhibitor and an MKK4-targeted inhibitor with potent, selective, and oral activity. By enhancing MKK7 and JNK1 signaling pathways, activating ATF2 and ELK1, Darizmetinib promotes hepatocyte proliferation and regeneration, used for preventing liver failure after extensive hepatectomy or small-for-size liver transplantation.

Cas No. 2369583-33-3

Customer service consultation

Pack Size	Price	USA Stock	Global Stock
1 mg	$66	In Stock	In Stock
2 mg	$96	In Stock	In Stock
5 mg	$158	In Stock	In Stock
10 mg	$248	In Stock	In Stock
25 mg	$360	In Stock	In Stock
50 mg	$445	In Stock	In Stock
100 mg	$652	-	In Stock
1 mL x 10 mM (in DMSO)	$159	In Stock	In Stock

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

Add to Cart

Add to Quotation

With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.

For research use only—not for human use. No sales to individuals. Use as intended only.

Questions

Batch Information

Select Batch

Purity:99.57%

Appearance:Solid

Color:White to Yellow

Resource Download

COA HPLC HNMR

Product Introduction

Bioactivity

Description	Darizmetinib (HRX215, HRX-0215) is a small-molecule inhibitor and an MKK4-targeted inhibitor with potent, selective, and oral activity. By enhancing MKK7 and JNK1 signaling pathways, activating ATF2 and ELK1, Darizmetinib promotes hepatocyte proliferation and regeneration, used for preventing liver failure after extensive hepatectomy or small-for-size liver transplantation.
Targets & IC50	MAP2K4:< 500 nM, MKK4:0.02 µM
In vitro	Methods:Peripheral blood mononuclear cells (PBMCs) induced with exogenous lipopolysaccharide (LPS) were treated with Darizmetinib (0.3, 1, 3 μM) for 2 hours, and pMKK4 protein levels were detected. Results: Darizmetinib reduced LPS-induced pMKK4 levels in PBMCs. [1]
In vivo	Methods: In a fibrotic mouse liver partial hepatectomy model, a single oral dose of Darizmetinib (30 mg/kg) was administered for 15 minutes to 24 hours to assess hepatocyte proliferation; in a hepatectomy mouse model, a single oral dose of Darizmetinib (10 mg/kg) was administered at 2 and 9 hours to detect changes in MKK7, JNK1, ATF2, ELK1, p38, p53, NF-κB signaling pathway-related molecules, and anti-apoptotic protein Bcl-XL; in a pig hepatectomy model, Darizmetinib (5 mg/kg) was administered intravenously every 12 hours starting 24 hours before surgery to assess hepatocyte regeneration. Results: Darizmetinib increased hepatocyte proliferation in fibrotic mouse livers; in hepatectomized mice, activated MKK7 and JNK1 signaling pathways, downstream activation of transcription factors ATF2 and ELK1, reduced p38 and p53 activation, activated NF-κB signaling pathway, and upregulated Bcl-XL; increased hepatocyte regeneration in the pig hepatectomy model. [1]
Synonyms	HRX215, HRX-0215

Chemical Properties

Molecular Weight	457.45
Formula	C₂₁H₁₇F₂N₅O₃S
Cas No.	2369583-33-3
Smiles	O=C(C1=NNC2=NC=C(C=C21)C=3C=CN=CC3)C4=CC=C(F)C(NS(=O)(=O)CCC)=C4F

Storage & Solubility Information

Storage

Keep away from direct sunlight,Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 180 mg/mL (393.49 mM), Sonication is recommended.

H2O: < 1 mg/mL (insoluble or slightly soluble)

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.1860 mL	10.9302 mL	21.8603 mL	109.3016 mL
5 mM	0.4372 mL	2.1860 mL	4.3721 mL	21.8603 mL
10 mM	0.2186 mL	1.0930 mL	2.1860 mL	10.9302 mL
20 mM	0.1093 mL	0.5465 mL	1.0930 mL	5.4651 mL
50 mM	0.0437 mL	0.2186 mL	0.4372 mL	2.1860 mL
100 mM	0.0219 mL	0.1093 mL	0.2186 mL	1.0930 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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.