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My Cart> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > MAPK > CI-1040CAS：212631-79-3
Molecular Formula：C17H14ClF2IN2O2
Molecular Weight：478.66
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥99%
Appearance：White to off-white Solid
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| CAS | 212631-79-3 |
| Name | CI-1040 |
| Molecular Formula | C17H14ClF2IN2O2 |
| Molecular Weight | 478.66 |
| Solubility | Soluble in DMSO |
| Purity | ≥99% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD02683961 |
| SMILES | O=C(C1=CC=C(C(F)=C1NC2=CC=C(I)C=C2Cl)F)NOCC3CC3 |
| Target Point | MEK |
| Passage | MAPK |
| Background | It is a highly specific small molecule inhibitor of MEK. |
| Biological Activity | CI-1040 是有口服活性，高度特异的MEK小分子抑制剂，对MEK1的IC50值为17 nM [1-3]。 |
| IC50 | MEK1:17nM[1-3] |
| In Vitro | CI-1040以剂量和时间依赖性方式诱导U-937细胞凋亡并抑制增殖。 CI-1040诱导PUMA mRNA和蛋白水平显著增加[2]。CI-1040直接抑制MEK1，IC50为17 nM。它还被证明对一组相关激酶的活性很小，其IC50值高出2.5个数量级以上。用CI-1040处理全细胞完全抑制有丝分裂原刺激的ERK磷酸化。发现浓度为1μM的CI-1040在MDA-MB-231乳腺癌细胞中分别抑制ERK1和ERK2的磷酸化99％和92％[1]。 |
| In Vivo | 全身施用MEK抑制剂CI-1040将腺瘤形成减少至第三并且显著恢复肺结构。 CL-1040处理的小鼠肺细胞增殖率降低，对肺细胞分化无明显影响[3]。 |
| Cell Experiment | 将MEK抑制剂CI-1040作为10mM储备溶液溶解在DMSO中，并以50mg/mL的终浓度用于细胞培养。将U-937细胞用5和20uM CI-1040预处理24小时，然后用wt-p53 siRNA或PUMA siRNA转染48小时。然后向每个孔中加入20mL MTT溶液并进一步温育2小时。终止后，吸出上清液，将代谢活细胞形成的MTT甲and溶解于100mL异丙醇中。将板在旋转振荡器上混合30分钟，并使用读板器在595nm处测量吸光度[2]。 |
| Animal Experiment | 小鼠：通过将组成型活性C-Raf激酶靶向肺来产生肺癌小鼠模型。 BAY43-9006或CI-1040每天腹膜内注射剂量为100mg/kg，从4个月龄开始，持续21天。在治疗期结束时分离并分析肺[3]。 |
| Data Literature Source | [1]. Allen LF，et al. CI-1040 (PD184352)，a targeted signal transduction inhibitor of MEK (MAPKK). Semin Oncol. 2003 Oct;30(5 Suppl 16):105-16. [2]. Wei CR，et al. MEK inhibitor CI-1040 induces apoptosis in acute myeloid leukemia cells in vitro. Eur Rev Med Pharmacol Sci. 2016 May;20(10):1961-8. [3]. Kramer BW，et al. Use of mitogenic cascade blockers for treatment of C-Raf induced lung adenoma in vivo: CI-1040strongly reduces growth and improves lung structure. BMC Cancer. 2004 Jun 1;4:24. |
| Unit | Bottle |
| Specification | 5mg 10mg 25mg |
是高度特异的MEK小分子抑制剂 。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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