Art. -Nr.: HY-15798

UNC2881

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UNC2881 is an orally active and specific Mer kinase inhibitor, inhibits steady-state Mer kinase phosphorylation with an IC₅₀ value of 22 nM. UNC2881 shows additional inhibition against Axl and Tyro with IC₅₀s of 360 nM and 250 nM, respectively. UNC2881 potently inhibits collagen-induced platelet aggregation, can be used for pathologic thrombosis research.

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Reinheit: 99.79%
CAS. Nr.: 1493764-08-1
Formel: C₂₅H₃₃N₇O₂
Molecular Weight:463.58

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

UNC2881 Chemical Structure

CAS. Nr.: 1493764-08-1

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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

Axl

Mer

Alle TAM Receptor Isoform-spezifische Produkte anzeigen :

In Vitro

UNC2881 (compound 23) (0-1000 nM; 1 h) block ligand-stimulated activation of a chimeric EGFR-MerTK. UNC2881 also inhibits endogenous Mer tyrosine kinase activation in acute lymphoblastic leukemia cells^[1].
UNC2881 (3 μM; 1 h) suppresses platelet aggregation by greater than 25% in human platelet-rich plasma in response to stimulation with fibrillar type I equine collagen^[1].

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

Western Blot Analysis^[1]

Cell Line:

32D cells
Concentration:

0, 10, 30, 100, 300, 1000 nM
Incubation Time:

1 hour; prior to stimulation with 100 ng/mL EGF ligand for 15 min
Result:

Reduced the phospho-tyrosine level in a dose-dependent manner.

In Vivo

UNC2881 (3 mg/kg; p.o.; single dose) has high systemic clearance (94.5 mL/min/kg) and 14% oral bioavailability, displays terminal half-life of 0.80 h^[1].
UNC2881 (3 mg/kg; i.v.; injected with VSV on days -3, -2, -1, and 0) limits Mertk signaling, and promotes the antiviral immune response, reducing the viral replication of vesicular stomatitis virus (VSV) in infected mice^[2].
Pharmacokinetics of UNC2881 in mice^[1]

Route	Dose (mg/kg)	T_1/2 (h)	T_max (h)	C_max (ng/mL)	AUC_last (ng·h/mL)	CL_obs (mL/min)	V_ss (L/kg)	F (%)
IV	3	0.8		2609	527	94.5	1.65
PO	3		0.30	90.0	71.7			14

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

Animal Model:

C57BL/6 mice (7-10 weeks old)^[2]
Dosage:

3 mg/kg
Administration:

Intravenous injection; infected with 2×10⁸ PFU vesicular stomatitis virus (VSV) (i.v.) on days -3, -2, -1, and 0
Result:

Reduced VSV replication in spleen, liver, kidney, lung.

Chemical Information

CAS. Nr. 1493764-08-1
Appearance Solid
Molecular Weight 463.58
Formel C₂₅H₃₃N₇O₂
Color White to off-white
SMILES

CCCCNC1=NC(N[C@H]2CC[C@H](O)CC2)=C(C(NCC3=CC=C(N4C=NC=C4)C=C3)=O)C=N1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (107.86 mM; ultrasonic and warming and heat to 60°C; 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

2.1571 mL

10.7856 mL

21.5713 mL

5 mM

0.4314 mL

2.1571 mL

4.3142 mL

10 mM

0.2157 mL

1.0786 mL

2.1571 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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: ≥ 2.5 mg/mL (5.39 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.39 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.39 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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 (275 KB)
SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 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]. Zhang W, et al. Discovery of Mer specific tyrosine kinase inhibitors for the treatment and prevention of thrombosis. J Med Chem. 2013 Dec 12;56(23):9693-700. [Content Brief]

[2]. Tom Adomati, et al. Dead Cells Induce Innate Anergy Via Mertk after Acute Viral Infection. Cell Reports. 2020. 30(11):3671-3681.

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1571 mL	10.7856 mL	21.5713 mL	53.9281 mL
	5 mM	0.4314 mL	2.1571 mL	4.3143 mL	10.7856 mL
	10 mM	0.2157 mL	1.0786 mL	2.1571 mL	5.3928 mL
	15 mM	0.1438 mL	0.7190 mL	1.4381 mL	3.5952 mL
	20 mM	0.1079 mL	0.5393 mL	1.0786 mL	2.6964 mL
	25 mM	0.0863 mL	0.4314 mL	0.8629 mL	2.1571 mL
	30 mM	0.0719 mL	0.3595 mL	0.7190 mL	1.7976 mL
	40 mM	0.0539 mL	0.2696 mL	0.5393 mL	1.3482 mL
	50 mM	0.0431 mL	0.2157 mL	0.4314 mL	1.0786 mL
	60 mM	0.0360 mL	0.1798 mL	0.3595 mL	0.8988 mL
	80 mM	0.0270 mL	0.1348 mL	0.2696 mL	0.6741 mL
	100 mM	0.0216 mL	0.1079 mL	0.2157 mL	0.5393 mL

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UNC2881

Anti-Infection Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Antiviral Compound Library

Anti-Cardiovascular Disease Compound Library

Orally Active Compound Library

Anti-Blood Cancer Compound Library

Targeted Diversity Library

Coagulation and Anti-coagulation Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Alle TAM Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

UNC2881

Anti-Infection Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Antiviral Compound Library

Anti-Cardiovascular Disease Compound Library

Orally Active Compound Library

Anti-Blood Cancer Compound Library

Targeted Diversity Library

Coagulation and Anti-coagulation Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Alle TAM Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

UNC2881 Related Classifications

HY-15798 Related Classifications