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UNC2250
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。
UNC2250图片
CAS NO:1493694-70-4
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)440.58
FormulaC24H36N6O2
CAS No.1493694-70-4
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 2 mg/mL (4.5 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Other infoChemical Name: (1r,4r)-4-((2-(butylamino)-5-(5-(morpholinomethyl)pyridin-2-yl)pyrimidin-4-yl)amino)cyclohexanol
InChi Key: HSYSSKFCQHXOBP-MXVIHJGJSA-N
InChi Code: InChI=1S/C24H36N6O2/c1-2-3-10-25-24-27-16-21(23(29-24)28-19-5-7-20(31)8-6-19)22-9-4-18(15-26-22)17-30-11-13-32-14-12-30/h4,9,15-16,19-20,31H,2-3,5-8,10-14,17H2,1H3,(H2,25,27,28,29)/t19-,20-
SMILES Code: O[C@H]1CC[C@H](NC2=NC(NCCCC)=NC=C2C3=NC=C(CN4CCOCC4)C=C3)CC1
SynonymsUNC-2250, UNC 2250, UNC2250,
实验参考方法
In Vitro

In vitro activity: UNC2250 efficiently inhibits Mer phosphorylation in 697 B-ALL cells and Colo699 NSCLC cells. Moreover, UNC2250 also displays functional antitumor activity by reducing colony-forming potential in both rhabdoid tumor cells and NSCLC cells.


Kinase Assay: Activity assays are performed in a 384-well, polypropylene microplate in a final volume of 50 μL of 50 mM Hepes, pH 7.4, containing 10 mM MgCl2, 1.0 mM DTT, 0.01% Triton X-100, 0.1% bovine serum albumin (BSA), containing 1.0 μM fluorescent substrate and ATP at the Km for each enzyme. All reactions are terminated by addition of 20 μL of 70 mM EDTA. After an 180 min incubation, phosphorylated and unphosphorylated substrate peptides are separated in buffer supplemented with 1× CR-8 on a LabChip EZ Reader equipped with a 12-sipper chip. Data are analyzed using EZ Reader software.


Cell Assay: BT-12 rhabdoid tumor cells (10 000 cells) are cultured in 2.0 mL of 0.35% soft agar containing 0.5× RPMI medium, 7.5% FBS, and the indicated concentrations of 10 or DMSO vehicle only and overlaid with 0.5 mL of 1× RPMI medium containing 15% FBS and 10 or DMSO vehicle only. Medium and 10 or vehicle are refreshed 2 times per week. Colonies were stained with thiazolyl blue tetrazolium bromide and counted after 3 weeks. Colo699 NSCLC cells (15 000 cells) are cultured in 1.5 mL of 0.35% soft agar containing 1× RPMI medium and 10% FBS and overlaid with 2.0 mL of 1× RPMI medium containing 10% FBS and the indicated concentrations of 10 or DMSO vehicle only. Medium and 10 or vehicle are refreshed 3 times per week. Colonies are stained with nitrotetrazolium blue chloride and counted after 2 weeks.

In VivoAccording to in vivo PK experiment, UNC2250 has a moderate half-life, clearance, and volume of distribution as well as reasonable oral bioavailability and good solubility.
Animal modelMice or rat
Formulation & DosageN/A
References

J Med Chem. 2013 Dec 12;56(23):9683-92.