{{cart_num}}
My Cart> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > MAPK > PD0325901CAS：391210-10-9
Molecular Formula：C16H14F3IN2O4
Molecular Weight：482.19
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to off-white Solid
Qty：
Size：
| CAS | 391210-10-9 |
| Name | PD0325901 |
| Molecular Formula | C16H14F3IN2O4 |
| Molecular Weight | 482.19 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 687-152-7 |
| MDL | MFCD08435926 |
| SMILES | O=C(C1=CC=C(C(F)=C1NC2=CC=C(I)C=C2F)F)NOC[C@H](O)CO |
| Target Point | MEK |
| Passage | MAPK |
| Background | PD0325901 is a selective MEK inhibitor. |
| Biological Activity | PD0325901是选择性，可渗透细胞的 MEK 抑制剂， IC50为0.33 nM。[1-2] |
| IC50 | MEK1:0.33nM |
| In Vitro | PD0325901对于纯化的MEK具有极好的特异性和高效性，显示出针对活化的MEK1和MEK2的1nM的Kiapp。就其对ERK1和ERK2的磷酸化的细胞作用而言，PD0325901的效力比CI-1040大约高500倍，显示亚纳摩尔活性。 PD0325901可防止黑素瘤细胞系的生长。 PD0325901抑制TPC-1细胞和K2细胞的生长，GC50分别为11 nM和6.3 nM。 PD0325901显著阻止具有极低浓度(10nM)的BRAF突变的PTC细胞的生长，并且仅在相同浓度下适度增加携带RET/PTC1重排的PTC细胞的生长。 PD0325901有效抑制多个PTC细胞系中ERK1/2的磷酸化[2]。 |
| In Vivo | PD0325901(25mg/kg，po)在给药后24小时抑制ERK的磷酸化超过50％。产生70％完全肿瘤反应(C26模型)所需的剂量为25mg/kg /天，而PD0325901和CI-1040分别为900mg/kg /天。已经证明PD 0325901的抗癌活性用于广谱的人肿瘤异种移植物。在小鼠中处理PD0325901(20-25mg/kg /天，po)，显示没有接种具有BRAF突变的PTC细胞的肿瘤生长。对于具有RET/PTC1重排的PTC，与对照相比，原位肿瘤的平均肿瘤体积减少了58％。携带BRAF突变的PTC细胞对PD0325901的敏感性高于携带RET/PTC1重排的PTC细胞[2]。 |
| Cell Experiment | 将PTC细胞(1×104)接种在含有1mL培养基的24孔板中，在37℃培养箱中培养4天。在第0天将不同浓度的MEK抑制剂PD0325901一式三份加入细胞中。在第2天将溶于0.8％NaCl溶液中的5mg/mL MTT加入到每个孔(0.2mL)中以测试GC50或每天用于细胞生长曲线。 |
| Animal Experiment | 将用表达荧光素酶的逆转录病毒(5μLRPMI1640培养基中的5×10 5个细胞)稳定感染的K2和TPC-1细胞接种到甲状腺中，并使用Living Image 3.0软件每周监测小鼠的Xenogen肿瘤生长。接种一周后，通过超声处理将PD0325901溶解于80mM柠檬酸缓冲液(pH7)中，并通过口服强饲法(20-25mg/kg)每天给予小鼠3周(连续5天/周)。对照小鼠单独给予80mM柠檬酸缓冲液(pH 7)。所有体内实验至少进行两次。 |
| Kinase Experiment | 在含有p44MAP激酶(GST-MAPK)的谷胱甘肽S-转移酶融合蛋白和含有p45MEK(GST-MEK)的谷胱甘肽S-转移酶蛋白的存在下测定32P掺入髓鞘碱性蛋白(MBP)。该测定溶液含有20mM HEPES，pH 7.4，10mM MgCl 2，1mM MnCl 2，1mM EGTA，50mM [γ-32P] ATP，10mg GST-MEK，0.5mg GST-MAPK和40mg MBP。体积为100毫升。 20分钟后，通过加入三氯乙酸终止反应，并通过GF/C过滤垫过滤。保留在过滤垫上的32P使用1205 Betaplate测定。在各种剂量范围评估PD0325901以确定剂量反应曲线。 |
| Data Literature Source | [1]. Barrett SD，et al. The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901. Bioorg Med Chem Lett. 2008 Dec 15;18(24):6501-4. [2]. Henderson YC，et al. MEK inhibitor PD0325901 significantly reduces the growth of papillary thyroid carcinoma cells in vitro and in vivo. Mol Cancer Ther. 2010 Jul;9(7):1968-76. |
| Unit | Bottle |
| Specification | 10mg 50mg 100mg |
PD0325901是选择性的 MEK 抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
Note：
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.
2. For your safety and health, please wear laboratory clothes, disposable gloves and masks.
3. The experimental results may be affected by many factors, after-sale service is limited to the product itself and does not involve other compensation.
Sorry, there is no more information.
Sorry, there is no more information.
Sorry, there is no more information.
Manual Download
