Art. -Nr.: HY-152860

Darizmetinib

(Synonyms: HRX-0215)

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Darizmetinib (HRX-0215) is an orally active, potent and selective inhibitor of mitogen-activated protein kinase kinase 4 (MKK4). Darizmetinib leads to enhancement of the MKK7 and JNK1 signaling pathways, thereby activating the transcription factors ATF2 and ELK1, promoting cell proliferation and liver regeneration. Darizmetinib is promising for research of preventing liver failure after extensive oncological liver resections or transplantation of small liver grafts.

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Reinheit: 99.94%
CAS. Nr.: 2369583-33-3
Formel: C₂₁H₁₇F₂N₅O₃S
Molecular Weight:457.45

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Darizmetinib Chemical Structure

CAS. Nr.: 2369583-33-3

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle p38 MAPK Isoform-spezifische Produkte anzeigen :

Alle JNK Isoform-spezifische Produkte anzeigen :

Alle NF-κB Isoform-spezifische Produkte anzeigen :

In Vitro

Darizmetinib (0.3, 1,3 μM, 2 h) reduces lipopolysaccharide (LPS) (HY-D1056)-induced pMKK4 levels in peripheral blood mononuclear cells (PBMCs)^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[3]

Cell Line:

PBMCs
Concentration:

0.3, 1,3 μM
Incubation Time:

2 h
Result:

Reduced pMKK4 levels in a potent and dose-dependent manner in PBMCs, confirming cell membrane permeability.

In Vivo

Darizmetinib (30 mg/kg, p.o., a single dose for 15 min-24 h) increases the number of proliferating hepatocytes upon partial hepatectomy in fibrotic mouse livers ^[3].
Darizmetinib (10 mg/kg, p.o., a single dose for 2 h and 9 h) activates pro-regenerative program by increaseing MKK7 and JNK1 signaling with a downstream activation of the transcription factors ATF2 and ELK1, reduces p38- and p53 activation, activates nuclear factor κB (NF-κB) signaling, and upregulates the anti-apoptotic protein Bcl-XL in hepatectomized mice^[3].
Darizmetinib (5 mg/kg, i.v., every 12 h, starting 24 h before surgery)--mediated suppression of MKK4 increases hepatocyte regeneration in a pig hepatectomy model^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

partial hepatectomy in fibrotic mouse livers^[2]
Dosage:

30 mg/kg
Administration:

p.o., a single dose for 15 min-24 h
Result:

Enhanced hepatocyte proliferation in partial hepatectomy in fibrotic mouse livers, suggesting that the presence of fibrosis per se does not interfere with the Darizmetinib-mediated pro-regenerative mechanism.

Chemical Information

CAS. Nr. 2369583-33-3
Appearance Solid
Molecular Weight 457.45
Formel C₂₁H₁₇F₂N₅O₃S
Color White to off-white
SMILES

O=C(C1=CC=C(C(NS(=O)(CCC)=O)=C1F)F)C2=NNC3=NC=C(C4=CC=NC=C4)C=C32
Synonyms

HRX-0215
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 175 mg/mL (382.56 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1860 mL

10.9302 mL

21.8603 mL

5 mM

0.4372 mL

2.1860 mL

4.3721 mL

10 mM

0.2186 mL

1.0930 mL

2.1860 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Praefke B, et al. Preparation of pyrazolopyridines as protein kinase MKK4 inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death: World Intellectual Property Organization, WO2019149738. 2019-08-08.

[2]. WHO Drug Information-World Health Organization (WHO).

[3]. Zwirner S, et al. First-in-class MKK4 inhibitors enhance liver regeneration and prevent liver failure. Cell. 2024 Mar 28;187(7):1666-1684.e26. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1860 mL	10.9302 mL	21.8603 mL	54.6508 mL
	5 mM	0.4372 mL	2.1860 mL	4.3721 mL	10.9302 mL
	10 mM	0.2186 mL	1.0930 mL	2.1860 mL	5.4651 mL
	15 mM	0.1457 mL	0.7287 mL	1.4574 mL	3.6434 mL
	20 mM	0.1093 mL	0.5465 mL	1.0930 mL	2.7325 mL
	25 mM	0.0874 mL	0.4372 mL	0.8744 mL	2.1860 mL
	30 mM	0.0729 mL	0.3643 mL	0.7287 mL	1.8217 mL
	40 mM	0.0547 mL	0.2733 mL	0.5465 mL	1.3663 mL
	50 mM	0.0437 mL	0.2186 mL	0.4372 mL	1.0930 mL
	60 mM	0.0364 mL	0.1822 mL	0.3643 mL	0.9108 mL
	80 mM	0.0273 mL	0.1366 mL	0.2733 mL	0.6831 mL
	100 mM	0.0219 mL	0.1093 mL	0.2186 mL	0.5465 mL

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Darizmetinib

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Apoptosis Compound Library

Immunology/Inflammation Compound Library

Alle p38 MAPK Isoform-spezifische Produkte anzeigen

Alle JNK Isoform-spezifische Produkte anzeigen

Alle NF-κB Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Darizmetinib Related Classifications

HY-152860 Related Classifications