[CAS NO. 1493764-08-1] UNC2881

Name: UNC2881
Brand: Arctom Scientific
SKU: HY-15798

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PRODUCTS SPECIFICATIONS [1493764-08-1]

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Catalog

HY-15798

Brand

MCE

CAS

1493764-08-1

DESCRIPTION [1493764-08-1]

Overview

MDL	MFCD28142814
Molecular Weight	463.58
Molecular Formula	C25H33N7O2
SMILES	CCCCNC1=NC(N[C@H]2CC[C@H](O)CC2)=C(C(NCC3=CC=C(N4C=NC=C4)C=C3)=O)C=N1

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

Summary

UNC2881 is an orally active and specific Mer kinase inhibitor, inhibits steady-state Mer kinase phosphorylation with an IC ₅₀ value of 22 nM. UNC2881 shows additional inhibition against Axl and Tyro with IC ₅₀ s 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)	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

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 2×10 ⁸ PFU vesicular stomatitis virus (VSV) (i.v.) on days -3, -2, -1, and 0
Result:	Reduced VSV replication in spleen, liver, kidney, lung.

Appearance

Solid

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.