Pimasertib (Synonyms: AS703026; MSC1936369B) 纯度: 99.70%
Pimasertib (AS703026) 是一种高效,具有选择性,口服活性的、ATP 非竞争性的 MEK1/2 别构抑制剂,主要用于癌症研究。
Pimasertib Chemical Structure
CAS No. : 1236699-92-5
规格 | 价格 | 是否有货 | 数量 |
---|---|---|---|
Free Sample (0.1-0.5 mg) | Apply now | ||
10 mM * 1 mL in DMSO | ¥550 | In-stock | |
5 mg | ¥500 | In-stock | |
10 mg | ¥650 | In-stock | |
50 mg | ¥1800 | In-stock | |
100 mg | ¥2800 | In-stock | |
200 mg | 询价 | ||
500 mg | 询价 |
* Please select Quantity before adding items.
Pimasertib 相关产品
•相关化合物库:
- Drug Repurposing Compound Library Plus
- Clinical Compound Library Plus
- Bioactive Compound Library Plus
- Immunology/Inflammation Compound Library
- Kinase Inhibitor Library
- MAPK Compound Library
- Anti-Cancer Compound Library
- Clinical Compound Library
- Drug Repurposing Compound Library
- Reprogramming Compound Library
- Oxygen Sensing Compound Library
- Ferroptosis Compound Library
- Anti-COVID-19 Compound Library
- Orally Active Compound Library
- Glutamine Metabolism Compound Library
- Anti-Pancreatic Cancer Compound Library
- Angiogenesis Related Compound Library
- Targeted Diversity Library
- Anti-Liver Cancer Compound Library
- Rare Diseases Drug Library
- Anti-Colorectal Cancer Compound Library
生物活性 |
Pimasertib (AS703026) is a highly selective, ATP non-competitive allosteric orally available MEK1/2 inhibitor[1][2]. |
||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
IC50 & Target[1] |
|
||||||||||||||||
体外研究 (In Vitro) |
Pimasertib (5, 0.5, and 0.1 μM) specifically blocks ERK1/2 activation in MM cells, cultured alone or with BMSCs. Pimasertib inhibits the growth of MM cell lines in a dose-dependent manner, with IC50s ranging from 0.005 to 2 μM. The IC50s of Pimasertib against INA-6, U266, H929 cells are 10 nM, 5 nM, 200 nM respectively. Pimasertib induces apoptosis and modulates the cell cycle profile. Pimasertib targets MM cells in the BM microenvironment[1]. Pimasertib (10 μmol/L) inhibits ERK pathway, proliferation, and transformation in cetuximab-resistant D-MUT cells[2]. Pimasertib in combination with PLX4032 significantly induces apoptosis of RPMI-7951 cells, whereas each drug used alone does not. Pimasertib synergizes with small interfering RNA-mediated downregulation of BRAF to produce results similar to those of combined treatment with PLX4032 and Pimasertib[3]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
||||||||||||||||
体内研究 (In Vivo) |
Pimasertib (15, 30 mg/kg) significantly inhibits the growth of tumor in the human H929 MM xenograft model in CB17 SCID mice[1]. Pimasertib (10 mg/kg, p.o.) inhibits tumor growth of cetuximab-resistant tumor attributed by K-ras mutation[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
||||||||||||||||
Clinical Trial |
|
||||||||||||||||
分子量 |
431.20 |
||||||||||||||||
Formula |
C15H15FIN3O3 |
||||||||||||||||
CAS 号 |
1236699-92-5 |
||||||||||||||||
运输条件 |
Room temperature in continental US; may vary elsewhere. |
||||||||||||||||
储存方式 |
|
||||||||||||||||
溶解性数据 |
In Vitro:
DMSO : ≥ 100 mg/mL (231.91 mM) * “≥” means soluble, but saturation unknown. 配制储备液
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
|
||||||||||||||||
参考文献 |
|
Cell Assay [1] |
The inhibitory effects of study compounds on MM cell growth and survival are assessed by both [3H]thymidine incorporation and by measuring MTT dye absorbance. Cells (104/well for MM cell line, in triplicates and 2-5×105/well for patient MM cells) are cultured in 96-well plates for 3 days (MM cell lines) or 5-days (patient MM cells). For the [3H]thymidine incorporation assay, cells are pulsed with 0.5 μCi (0.0185 MBq)/well [3H]thymidine for 6 h (cell lines), harvested onto glass fiber filters, and counted in a β-scintillation counter. Due to low DNA synthesis of patient MM cells, they are pulsed with 2 μCi/well [3H]thymidine and measured during the last 36 h of culture. MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
---|---|
Animal Administration [1] |
CB17 severe combined immunodeficiency (SCID) mice are subcutaneously inoculated with H929 (4×106) cells in 100 μL RPMI-1640 medium. Mice developed palpable tumors (appr 130 mm3) approximately 3 weeks after cell injection and are randomized to receive orally twice daily either Pimasertib (15 or 30 mg/kg) or control vehicle alone. Tumor size is measured every other day in 2 dimensions using calipers, and tumor volume is calculated. Animals are euthanized when their tumors reach 2 cm3 in volume, when they are moribund or show paralysis or major compromise in their quality of life occurs. Tumor formation changes in mice treated with control vehicle vs. Pimasertib are plotted using the GraphPad Prism version 4.03 for Windows. Tumors are subjected to immunoblotting and immunochemistry analyses using specific monoclonal (m)Abs. Images are examined with a Leica DM LB research microscope, captured using Leica IM50 Image Manager, and processed using Adobe Photoshop Software version 7.0. MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
参考文献 |
|
所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务