2. Anti-infection Protein Tyrosine Kinase/RTK
  3. VSV TAM Receptor
  4. UNC2881

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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UNC2881

UNC2881 構造式

CAS 番号 : 1493764-08-1

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 89 在庫あり
Solution
10 mM * 1 mL in DMSO USD 89 在庫あり
Solid
5 mg $87 在庫あり
10 mg $140 在庫あり
25 mg $280 在庫あり
50 mg $450 在庫あり
100 mg $750 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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UNC2881 関連抗体

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TAM Receptor アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
Axl Mer Tyro3

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  • 純度とドキュメンテーション

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製品説明

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[1].

IC50 & Target

Axl

 

Mer

 

体外実験

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.

UNC2881 関連抗体

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.
体内実験

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) T1/2 (h) Tmax (h) Cmax (ng/mL) AUClast (ng·h/mL) CLobs (mL/min) Vss (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.
分子量

463.58

分子式

C25H33N7O2
CAS 番号
Appearance

Solid

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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
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
View the Complete Stock Solution Preparation Table

* 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

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

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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
参考文献

Complete Stock Solution Preparation Table

* 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.

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 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

UNC28811493764-08-1UNC 2881UNC-2881VSVTAM ReceptorVesicular Stomatitis VirusTyro3AxlMerorally activephosphorylationplatelet aggregationpathologic thrombosisInhibitorinhibitorinhibit

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製品名:
UNC2881
製品番号:
HY-15798
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