Art. -Nr.: HY-107620

PD 198306

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PD 198306 is a selective MAPK/ERK-kinase (MEK) inhibitor. PD 198306 results in an observable reduction in the Streptozocin induced increase in the level of active ERK1 and 2. Antihyperalgesic effects.

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Reinheit: 99.75%
CAS. Nr.: 212631-61-3
Formel: C₁₈H₁₆F₃IN₂O₂
Molecular Weight:476.23

Speicherung:

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

PD 198306 Chemical Structure

CAS. Nr.: 212631-61-3

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

MEK

Alle MEK Isoform-spezifische Produkte anzeigen :

In Vitro

PD198306 significantly inhibits Tha-GFP replication by 25% at 10 μM, after 36 h^[2].
PD198306 (5 μM) reduces Tha-Crimson replication significantly by 20% at 18 h but such a result could not be confirmed at 36 h^[2].

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

Cell Cycle Analysis^[2]

Cell Line:

Human induced pluripotent stem cells (iPSC)
Concentration:

10 μM
Incubation Time:

6 hours
Result:

Inhibited Tha-Crimson replication at 10 μM, reducing it by 30% at 18 h and 50% at 36 h.

In Vivo

Intrathecal administration of PD 198306 (1-30 μg per 10 μL) dose-dependently (1-30 μg) blocks static allodynia in both the streptozocin and the chronic constriction injury (CCI) models of neuropathic pain^[1].

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

Animal Model:

Male Sprague Dawley rats (250-300 g) bearing neuropathic pain^[1]
Dosage:

1-30 μg per 10 μL and 3 mg per 100 μL (PD 198306 is suspended in cremophor:ethanol:water, 1 : 1 : 8.)
Administration:

Single doses of intrathecal (i.t.) or intraplantar (ipl) of PD 198306 (1-30 μg per 10 μL and 3 mg per 100 μL respectively
Result:

Intrathecal administration dose-dependently (1-30 μg) blocked static allodynia the streptozocin model of neuropathic pain.
The minimum effective doses (MED) of 3 μg significantly blocked static allodynia 30 min after treatment.
Both 10 μg and the highest dose used (30 μg) totally blocked the maintenance of static allodynia, for up to 1 h.

Chemical Information

CAS. Nr. 212631-61-3
Appearance Solid
Molecular Weight 476.23
Formel C₁₈H₁₆F₃IN₂O₂
Color White to off-white
SMILES

O=C(NOCC1CC1)C(C=C(F)C(F)=C2F)=C2NC3=C(C=C(I)C=C3)C
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 : 200 mg/mL (419.97 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

2.0998 mL

10.4991 mL

20.9983 mL

5 mM

0.4200 mL

2.0998 mL

4.1997 mL

10 mM

0.2100 mL

1.0499 mL

2.0998 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)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 5 mg/mL (10.50 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 5 mg/mL (10.50 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
SDS (544 KB)
- English - EN (544 KB)
- Français - FR (544 KB)
- Deutsch - DE (544 KB)
- Norwegian - NO (544 KB)
- Español - ES (544 KB)
- Swedish - SV (544 KB)
- Italian - IT (544 KB)
- Korean - KR (544 KB)
- Portuguese - PT (544 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]. A Ciruela, et al. Identification of MEK1 as a novel target for the treatment of neuropathic pain. Br J Pharmacol. 2003 Mar;138(5):751-6. [Content Brief]

[2]. Benoit Besson, et al. Kinome-Wide RNA Interference Screening Identifies Mitogen-Activated Protein Kinases and Phosphatidylinositol Metabolism as Key Factors for Rabies Virus Infection. mSphere. 2019 May 22;4(3):e00047-19. [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	2.0998 mL	10.4991 mL	20.9983 mL	52.4956 mL
	5 mM	0.4200 mL	2.0998 mL	4.1997 mL	10.4991 mL
	10 mM	0.2100 mL	1.0499 mL	2.0998 mL	5.2496 mL
	15 mM	0.1400 mL	0.6999 mL	1.3999 mL	3.4997 mL
	20 mM	0.1050 mL	0.5250 mL	1.0499 mL	2.6248 mL
	25 mM	0.0840 mL	0.4200 mL	0.8399 mL	2.0998 mL
	30 mM	0.0700 mL	0.3500 mL	0.6999 mL	1.7499 mL
	40 mM	0.0525 mL	0.2625 mL	0.5250 mL	1.3124 mL
	50 mM	0.0420 mL	0.2100 mL	0.4200 mL	1.0499 mL
	60 mM	0.0350 mL	0.1750 mL	0.3500 mL	0.8749 mL
	80 mM	0.0262 mL	0.1312 mL	0.2625 mL	0.6562 mL
	100 mM	0.0210 mL	0.1050 mL	0.2100 mL	0.5250 mL

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PD 198306

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Ferroptosis Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Pain-Related Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Alle MEK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PD 198306

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Ferroptosis Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Pain-Related Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Alle MEK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PD 198306 Related Classifications

HY-107620 Related Classifications