1. Protein Tyrosine Kinase/RTK
  2. TAM Receptor
  3. UNC2881

UNC2881 

Cat. No.: HY-15798 Purity: 99.91%
COA Handling Instructions

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.

For research use only. We do not sell to patients.

UNC2881 Chemical Structure

UNC2881 Chemical Structure

CAS No. : 1493764-08-1

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 154 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 154 In-stock
Estimated Time of Arrival: December 31
Solid
10 mg USD 140 In-stock
Estimated Time of Arrival: December 31
50 mg USD 450 In-stock
Estimated Time of Arrival: December 31
100 mg USD 750 In-stock
Estimated Time of Arrival: December 31
500 mg USD 2250 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

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

IC50: 4.3 nM (Mer), 360 nM (Axl), 250 nM (Tyro)[1]

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].

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) 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

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.
Molecular Weight

463.58

Formula

C25H33N7O2

CAS No.
SMILES

CCCCNC1=NC(N[[email protected]]2CC[[email protected]](O)CC2)=C(C(NCC3=CC=C(N4C=NC=C4)C=C3)=O)C=N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 44 mg/mL (94.91 mM)

*"≥" means soluble, but saturation unknown.

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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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.

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UNC2881
Cat. No.:
HY-15798
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