产品描述: | Pimasertib (AS703026) is a highly selective, ATP non-competitive allosteric orally available MEK1/2 inhibitor |
靶点: |
MEK1;MEK2;MEK |
体内研究: |
Pimasertib (15, 30 mg/kg) significantly inhibits the growth of tumor in the human H929 MM xenograft model in CB17 SCID mice. Pimasertib (10 mg/kg, p.o.) inhibits tumor growth of cetuximab-resistant tumor attributed by K-ras mutation |
参考文献: |
1. Kim K, et al. Blockade of the MEK/ERK signalling cascade by AS703026, a novel selective MEK1/2 inhibitor, induces pleiotropic anti-myeloma activity in vitro and in vivo. Br J Haematol, 2010, 149(4), 537-549. 2. Park SJ, et al. The MEK1/2 inhibitor AS703026 circumvents resistance to the BRAF inhibitor PLX4032 in human malignant melanoma cells. Am J Med Sci. 2013 Dec;346(6):494-8. 3. Yoon J, et al. MEK1/2 inhibitors AS703026 and AZD6244 may be potential therapies for KRAS mutated colorectal cancer that is resistant to EGFR monoclonal antibody therapy. Cancer Res, 2011, 71(2), 445-453. |
溶解性: |
DMSO : ≥ 100 mg/mL (231.91 mM) |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
2.319 ml |
11.596 ml |
23.191 ml |
5 mM |
0.464 ml |
2.319 ml |
4.638 ml |
10 mM |
0.232 ml |
1.16 ml |
2.319 ml |
50 mM |
0.046 ml |
0.232 ml |
0.464 ml |
|
注意: |
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