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Pexmetinib(ARRY-614)
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。
Pexmetinib(ARRY-614)图片
CAS NO:945614-12-0
规格:≥98%
包装与价格:
包装价格(元)
1mg电议
2mg电议
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)556.63
FormulaC31H33FN6O3
CAS No.945614-12-0
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 100 mg/mL (179.6 mM)
Water: <1 mg/mL
Ethanol: N/A
SMILESO=C(NCC1=CC(F)=CC=C1OC2=CC3=C(N(CCO)N=C3)C=C2)NC4=CC(C(C)(C)C)=NN4C5=CC=C(C)C=C5
SynonymsARRY 614; ARRY614; ARRY-614; 1-(3-(tert-butyl)-1-(p-tolyl)-1H-pyrazol-5-yl)-3-(5-fluoro-2-((1-(2-hydroxyethyl)-1H-indazol-5-yl)oxy)benzyl)urea
实验参考方法
In Vitro

In vitro activity: In HeLa cells, Pexmetinib inhibits phospho-HSP27 with IC50 of 2 nM. In isolated PBMCs and human whole blood cells, Pexmetinib inhibits LPS-Induced TNFα with IC50 of 4.5 nM and 313 nM, respectively.


Kinase Assay: Pexmetinib (ARRY-614) is a potent inhibitor of cytokine synthesis, via the dual inhibition of p38 mitogen-activated protein kinase (MAPK), and Tie2/Tek receptor tyrosine kinase. The in vitro IC50 values of ARR Y-614 for both Tie2 and p38 mitogen-activated protein kinase are 1000 ng/mL and 100 ng/mL, respectively.


Cell Assay: In primary human bone marrow stromal cells, ARRY-614 inhibited basal cytokines with an IC50 value ranging from 50-100 nM.

In VivoIn male Swiss Webster mice, Pexmetinib (30 mg/kg, p.o.) inhibits the production of the proinflammatory cytokines TNFα and IL6 in response to lipopolysaccharide (LPS) or staphyloccus enterotoxin A. In established RPMI 8226 xenografts, ARRY-614 (25 mg/kg, p.o.) inhibits tumor growth and shows additive activity when combines with thalidomide. In ovarian carcinoma A2780 xenografts, ARRY-614 (30 mg/kg, p.o.) also shows additive tumor growth inhibition activity when combines with Taxol.
Animal modelRPMI 8226 xenografts
Formulation & Dosage25 mg/kg; p.o.
References

Clin Cancer Res. 2015 Mar 1;21(5):985-94.

生物活性


Bone marrow levels of p-p38 and CC3. Clin Cancer Res. 2015 Mar 1; 21(5): 985–994.


ARRY-614 Plasma Concentration-Time Profiles. Clin Cancer Res. 2015 Mar 1;21(5):985-94.