Art. -Nr.: HY-131341

Syk-IN-4

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Syk-IN-4 is a potent, selective and orally bioavailable SYK inhibitor with an IC₅₀ of 0.31 nM. SYK has emerged as a potential target for autoimmunity and hematological cancers.

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Reinheit: 98.0%
CAS. Nr.: 2932264-95-2
Formel: C₂₁H₂₅N₉O
Molecular Weight:419.48

Speicherung:

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

Syk-IN-4 Chemical Structure

CAS. Nr.: 2932264-95-2

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

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

Biologische Aktivität

Beschreibung

Syk-IN-4 is a potent, selective and orally bioavailable SYK inhibitor with an IC₅₀ of 0.31 nM. SYK has emerged as a potential target for autoimmunity and hematological cancers^[1].

IC₅₀ & Target

IC50: 0.31 nM (SYK)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
SUD4	GI₅₀	0.24 μM Compound: 1a	Growth inhibition of human SU-DHL-4 cells after 72 hrs Growth inhibition of human SU-DHL-4 cells after 72 hrs	[PMID: 32877741]
SUD4	IC₅₀	0.24 μM Compound: 4	Cytotoxicity against human SU-DHL-4 cells assessed as reduction in cell viability Cytotoxicity against human SU-DHL-4 cells assessed as reduction in cell viability	[PMID: 37270074]
SU-DHL-2	GI₅₀	0.24 μM Compound: 17	Growth inhibition of human SUDHL-4 cells Growth inhibition of human SUDHL-4 cells	[PMID: 32717371]
T-cell	GI₅₀	2.6 μM Compound: 17	Growth inhibition of T-cells (unknown origin) Growth inhibition of T-cells (unknown origin)	[PMID: 32717371]

In Vitro

Syk-IN-4 is a potent inhibitor of hERG with an IC₅₀ of 3.0 μM^[1].
Syk-IN-4 inhibits SUDHL-4 and T cell proliferation with GI₅₀s of 0.24 and 2.6 μM, respectively^[1].

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

In Vivo

Syk-IN-4 exhibits moderate oral bioavailability (60%) following oral administration (1 mg/kg) in male Hans Wistar rats^[1].
Syk-IN-4 exhibits high plasma clearance (151 mL/min/kg) combined with large volumes of distribution (1.0 L/kg respectively) following i.v. administration (0.5 mg/kg) in male Hans Wistar rats^[1].

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

Chemical Information

CAS. Nr. 2932264-95-2
Appearance Solid
Molecular Weight 419.48
Formel C₂₁H₂₅N₉O
Color White to off-white
SMILES

CC1=NN(C=C1CN(C)C)C2=NC(NC3=CC=C(N(C)N=C4C(NC)=O)C4=C3)=NC=C2
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 : 62.5 mg/mL (148.99 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

2.3839 mL

11.9195 mL

23.8390 mL

5 mM

0.4768 mL

2.3839 mL

4.7678 mL

10 mM

0.2384 mL

1.1920 mL

2.3839 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: ≥ 2.08 mg/mL (4.96 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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% (20% SBE-β-CD in Saline)

Solubility: 2.08 mg/mL (4.96 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: ≥ 2.08 mg/mL (4.96 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 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 (279 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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]. Neil P Grimster, et al. Optimization of a Series of Potent, Selective and Orally Bioavailable SYK Inhibitors. Bioorg Med Chem Lett. 2020 Jul 24;127433. [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	2.3839 mL	11.9195 mL	23.8390 mL	59.5976 mL
	5 mM	0.4768 mL	2.3839 mL	4.7678 mL	11.9195 mL
	10 mM	0.2384 mL	1.1920 mL	2.3839 mL	5.9598 mL
	15 mM	0.1589 mL	0.7946 mL	1.5893 mL	3.9732 mL
	20 mM	0.1192 mL	0.5960 mL	1.1920 mL	2.9799 mL
	25 mM	0.0954 mL	0.4768 mL	0.9536 mL	2.3839 mL
	30 mM	0.0795 mL	0.3973 mL	0.7946 mL	1.9866 mL
	40 mM	0.0596 mL	0.2980 mL	0.5960 mL	1.4899 mL
	50 mM	0.0477 mL	0.2384 mL	0.4768 mL	1.1920 mL
	60 mM	0.0397 mL	0.1987 mL	0.3973 mL	0.9933 mL
	80 mM	0.0298 mL	0.1490 mL	0.2980 mL	0.7450 mL
	100 mM	0.0238 mL	0.1192 mL	0.2384 mL	0.5960 mL

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Syk-IN-4

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Orally Active Compound Library

Targeted Diversity Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Syk-IN-4

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Orally Active Compound Library

Targeted Diversity Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Syk-IN-4 Related Classifications

HY-131341 Related Classifications