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UNC2881
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
UNC2881图片
CAS NO:1493764-08-1
规格:≥98%
包装与价格：
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)463.58
FormulaC25H33N7O2
CAS No.1493764-08-1
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 292 mg/mL (198.5 mM)
Water: <1 mg/mL
Ethanol: 5 mg/mL (10.8 mM)
Other info
Chemical Name: N-(4-(1H-imidazol-1-yl)benzyl)-2-(butylamino)-4-(((1r,4r)-4-hydroxycyclohexyl)amino)pyrimidine-5-carboxamide
InChi Key: NPVXOWLPOFYACO-XUTJKUGGSA-N
InChi Code: InChI=1S/C25H33N7O2/c1-2-3-12-27-25-29-16-22(23(31-25)30-19-6-10-21(33)11-7-19)24(34)28-15-18-4-8-20(9-5-18)32-14-13-26-17-32/h4-5,8-9,13-14,16-17,19,21,33H,2-3,6-7,10-12,15H2,1H3,(H,28,34)(H2,27,29,30,31)/t19-,21-
SMILES Code: O=C(C1=CN=C(NCCCC)N=C1N[C@H]2CC[C@H](O)CC2)NCC3=CC=C(N4C=CN=C4)C=C3
SynonymsUNC-2881, UNC 2881, UNC2881,
实验参考方法
In Vitro

In vitro activity: UNC2881 inhibits Mer kinase activity in 697 B-ALL cells with IC50 of 22 nM, and inhibits collagen-stimulated platelet aggregation.

Kinase Assay: UNC2881 is a potent and specific Mer kinase inhibitor; inhibits steady-state Mer kinase phosphorylation with an IC50 value of 22 nM.

Cell Assay: In 697 B-ALL cells, UNC2881 inhibited Mer phosphorylation with IC50 value of 22 nM. Also, UNC2881 inhibited ligand-dependent phosphorylation of a chimeric protein consisting of the intracellular domain of Mer and the extracellular domain of the epidermal growth factor receptor (EGFR). In human platelet-rich plasma, UNC2881 inhibited platelet aggregation induced by fibrillar Type I equine collagen by greater than 25%. UNC2881 also inhibited ATP release, a marker of platelet activation.

In VivoUNC2881 have high systemic clearance (94.5 mL/min/kg) and 14% oral bioavailability in mice.
Animal modelMouse model
Formulation & Dosage94.5 mL/min/kg; oral
ReferencesJ Med Chem. 2013 Dec 12;56(23):9693-700.