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My CartCAS：1236699-92-5
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：Light yellow to brown Solid
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| CAS | 1236699-92-5 |
| Name | Pimasertib |
| Molecular Formula | C15H15FIN3O3 |
| Molecular Weight | 431.2 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | Light yellow to brown Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD00015027 |
| SMILES | FC1=C(C=CC(I)=C1)NC2=CN=CC=C2C(NC[C@@H](CO)O)=O |
| Target Point | MEK |
| Passage | MAPK |
| Background | Pimasertib/AS-703026 is a potent, selective, and ATP-noncompetitive allosteric inhibitor of MEK1/2, primarily for cancer research. |
| Biological Activity | Pimasertib (AS703026) 是一种高效，具有选择性，ATP 非竞争性的 MEK1/2 别构抑制剂，主要用于癌症研究。[1-3] |
| In Vitro | Pimasertib与PLX4032组合显著诱导RPMI-7951细胞的凋亡，而单独使用的每种药物则不会。 Pimasertib与小干扰RNA介导的BRAF下调协同作用，产生与PLX4032和Pimasertib联合治疗相似的结果[3]。Pimasertib(5，0.5和0.1μM)特异性阻断MM细胞中的ERK1/2活化，单独培养或与BMSC一起培养。 Pimasertib以剂量依赖性方式抑制MM细胞系的生长，IC50范围为0.005至2μM。 Pimasertib对INA-6，U266，H929细胞的IC50分别为10nM，5nM，200nM。 Pimasertib诱导细胞凋亡并调节细胞周期特征。 Pimasertib靶向BM微环境中的MM细胞[1]。 Pimasertib(10μmol/ L)抑制西妥昔单抗抗性D-MUT细胞中的ERK通路，增殖和转化[2]。 |
| In Vivo | Pimasertib(15，30 mg/kg)显著抑制CB17 SCID小鼠人H929 MM异种移植模型中肿瘤的生长[1]。 Pimasertib(10 mg/kg，po)抑制由K-ras突变引起的西妥昔单抗抗性肿瘤的肿瘤生长[2]。 |
| Animal Experiment | 在100μLRPMI-1640培养基中用H929(4×106)细胞皮下接种CB17严重联合免疫缺陷(SCID)小鼠。小鼠在细胞注射后约3周产生可触知的肿瘤(约130mm 3)并随机接受每日两次口服Pimasertib(15或30mg/kg)或单独的对照载体。使用卡尺每隔一天在2个维度上测量肿瘤大小，并计算肿瘤体积。当它们的肿瘤体积达到2立方厘米时，当它们垂死或显示麻痹或其生活质量发生重大损害时，对动物实施安乐死。 |
| Data Literature Source | [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]. 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. [3]. 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. |
| Unit | Bottle |
| Specification | 5mg 10mg 50mg |
是一种高效，具有选择性，ATP 非竞争性的 MEK1/2 别构抑制剂，主要用于癌症研究。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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1. The products are all for scientific research use only. Do not use it for medical, clinical diagnosis or treatment, food and cosmetics, etc. Do not store them in ordinary residential areas.
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