UNC2881

SKU: orb1223282

Description

UNC2881 is a potent Mer kinase inhibitor. UNC2281 inhibits steady-state Mer kinase phosphorylation with an IC50 value of 22 nM. Treatment with UNC2281 is also sufficient to block EGF-mediated stimulation of a chimeric receptor containing the intracellular domain of Mer fused to the extracellular domain of EGFR. In addition, UNC2881 potently inhibits collagen-induced platelet aggregation, suggesting that this class of inhibitors may have utility for prevention and/or treatment of pathologic thrombosis.

Images & Validation

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Key Properties

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CAS Number	1493764-08-1
MW	463.58
Purity	>98% (HPLC)
Formula	C₂₅H₃₃N₇O₂
SMILES	CCCCNc1ncc(c(N[C@@H]2CC[C@H](CC2)O)n1)C(=O)NCc1ccc(n2ccnc2)cc1
Target	AChR
Solubility	DMSO : ≥ 44 mg/mL; 94.91 mM

Bioactivity

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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. 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. Pharmacokinetics of UNC2881 in mice. Animal model: C57BL/6 mice (7-10 weeks old). 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.

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. 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. Western blot analysis. 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.

Storage & Handling

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Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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UNC2881, UNC-2881, UNC 2881

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AChR

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UNC2881 (orb1223282)

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Purity:	99.72%
CAS Number:	1493764-08-1
MW:	463.58
Formula:	C₂₅H₃₃N₇O₂

UNC2881

Description

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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