Pexmetinib
作者：齐岳
发布时间：2023-09-13
17:38:45
点击数：
产品名称：Pexmetinib
产品描述：
| 产品描述 | Pexmetinib (ARRY-614) is a potent, orally bioavailable, dual p38 MAPK/Tie-2 inhibitor with IC50 of 4 nM/18 nM in a HEK-293 cell line. Phase 1. |
| 靶点活性 | p38 MAPK:4 nM, Tie-2:18 nM |
| 体外活性 | 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. [1] |
| 体内活性 | In male Swiss Webster mice, Pexmetinib (30 mg/kg, p.o.) inhibits the production of the proin? ammatory 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. [1] |
| 别名 | ARRY-614 |
| 分子量 | 556.63 |
| 分子式 | C31H33FN6O3 |
| CAS No. | 945614-12-0 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
H2O: <1 mg/mL
DMSO: 93 mg/mL (167.1 mM)
Ethanol: 93 mg/mL (167.1 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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