| CAS NO: | 945614-12-0 |
| 规格: | ≥98% |
| 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 |
| Molecular Weight (MW) | 556.63 |
|---|---|
| Formula | C31H33FN6O3 |
| 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 | |
| SMILES | O=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 |
| Synonyms | ARRY 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 |
| 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 Vivo | In 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 model | RPMI 8226 xenografts |
| Formulation & Dosage | 25 mg/kg; p.o. |
| References | Clin Cancer Res. 2015 Mar 1;21(5):985-94. |
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. |
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