Pimasertib
Based on 10 publication(s) in Google Scholar
Pimasertib (AS703026) is a highly selective, ATP non-competitive allosteric orally available MEK1/2 inhibitor.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.60%
- CAS No.: 1236699-92-5
- Formule: C15H15FIN3O3
- Masse moléculaire:431.20
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
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Publications Citing Use of MedChemExpress (MCE) Pimasertib
More- Cell. 2023 Jun 22;186(13):2929-2949.e20. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Sci Adv. 2023 Mar 22;9(12):eadd5028. [Abstract]
- Sci Data. 2024 Sep 19;11(1):1024. [Abstract]
- Oncogenesis. 2019 Nov 4;8(11):65. [Abstract]
- Int Immunopharmacol. 2026 Apr 29:181:116734. [Abstract]
- Hong Kong Polytechnic University. 2025.
- Res Sq. 2025 Apr 14.
- Oncotarget. 2020 Nov 3;11(44):3921-3932. [Abstract]
- ACS Comb Sci. 2019 Dec 9;21(12):805-816. [Abstract]
Voir tous les produits spécifiques à Isoform MEK
More
Activité biologique
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MEK1 |
MEK2 |
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Cell Line
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Type | Value | Description | References |
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| COLO 205 | IC50 |
1.81 nM
Compound: AS-703026
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Inhibition of MEK1 in human COLO205 cells
Inhibition of MEK1 in human COLO205 cells
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[PMID: 24755426] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pimasertib (10 mg/kg, p.o.) inhibits tumor growth of cetuximab-resistant tumor attributed by K-ras mutation[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1236699-92-5
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Appearance Solid
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Masse moléculaire 431.20
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Formule C15H15FIN3O3
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Color Light yellow to khaki
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SMILES
FC1=C(C=CC(I)=C1)NC2=CN=CC=C2C(NC[C@@H](CO)O)=O
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Synonyms
AS703026; MSC1936369B
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (10)
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Journal Impact Factor
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Most Recent
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Cell
Distinct longevity mechanisms across and within species and their association with aging. [Abstract]2023 Jun 22;186(13):2929-2949.e20. PMID: 37269831 -
Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Sci Adv
Breast tumors interfere with endothelial TRAIL at the premetastatic niche to promote cancer cell seeding. [Abstract]2023 Mar 22;9(12):eadd5028. PMID: 36947620 -
Sci Data
High-throughput drug screening identifies novel therapeutics for Low Grade Serous Ovarian Carcinoma. [Abstract]2024 Sep 19;11(1):1024. PMID: 39300112 -
Oncogenesis
A novel small-molecule inhibitor of trefoil factor 3 (TFF3) potentiates MEK1/2 inhibition in lung adenocarcinoma. [Abstract]2019 Nov 4;8(11):65. PMID: 31685806 -
Int Immunopharmacol
The role and significance of YKL-40 in mucopathological remodeling in eosinophilic chronic rhinosinusitis. [Abstract]2026 Apr 29:181:116734. PMID: 42061140 -
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Oncotarget
2020 Nov 3;11(44):3921-3932. PMID: 33216841 -
ACS Comb Sci
Benzimidazolyl-pyrazolo[3,4- b]pyridinones, Selective Inhibitors of MOLT-4 Leukemia Cell Growth and Sea Urchin Embryo Spiculogenesis: Target Quest. [Abstract]2019 Dec 9;21(12):805-816. PMID: 31689077
Solvant et solubilité
DMSO : ≥ 100 mg/mL (231.91 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.80 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.80 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (282 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3191 mL | 11.5955 mL | 23.1911 mL | 57.9777 mL |
| 5 mM | 0.4638 mL | 2.3191 mL | 4.6382 mL | 11.5955 mL | |
| 10 mM | 0.2319 mL | 1.1596 mL | 2.3191 mL | 5.7978 mL | |
| 15 mM | 0.1546 mL | 0.7730 mL | 1.5461 mL | 3.8652 mL | |
| 20 mM | 0.1160 mL | 0.5798 mL | 1.1596 mL | 2.8989 mL | |
| 25 mM | 0.0928 mL | 0.4638 mL | 0.9276 mL | 2.3191 mL | |
| 30 mM | 0.0773 mL | 0.3865 mL | 0.7730 mL | 1.9326 mL | |
| 40 mM | 0.0580 mL | 0.2899 mL | 0.5798 mL | 1.4494 mL | |
| 50 mM | 0.0464 mL | 0.2319 mL | 0.4638 mL | 1.1596 mL | |
| 60 mM | 0.0387 mL | 0.1933 mL | 0.3865 mL | 0.9663 mL | |
| 80 mM | 0.0290 mL | 0.1449 mL | 0.2899 mL | 0.7247 mL | |
| 100 mM | 0.0232 mL | 0.1160 mL | 0.2319 mL | 0.5798 mL |
Pimasertib Related Classifications
HY-12042 Related Classifications
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