PD0325901 |
Catalog No.GC10397
One-Click Copy Product Info
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PD0325901 is an orally active, selective and non-ATP-competitive mitogen-activated protein kinase kinase (MEK) inhibitor with an IC50 value of 0.33nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 391210-10-9
Sample solution is provided at 25 µL, 10mM.
PD0325901 is an orally active, selective and non-ATP-competitive mitogen-activated protein kinase kinase (MEK) inhibitor with an IC50 value of 0.33 nM[1]. The Ki value of PD0325901 for activated MEK1 and MEK2 is 1 nM[2]. PD0325901 inhibits the phosphorylation of ERK1/2 and induces cell apoptosis, maintaining stem cell renewal function and anti-cancer activity[3].
In vitro, treatment of papillary thyroid carcinoma (PTC) cell lines (K2 and TPC-1) with PD0325901 (0.1 μM) for 96 h significantly inhibited cell growth and reduced intracellular ERK1/2 phosphorylation[4]. Treatment of bone marrow monocytes/macrophages (BMMs) with PD0325901 (0.32, 0.64, 1.28 nM) for 24-96 h significantly inhibited osteoclast differentiation, inhibited osteoclast-specific gene expression, and inhibited NF-κB signaling pathway activation[5].
In vivo, oral treatment of mice with non-small cell lung cancer (NSCLC) with PD0325901 (20 mg/kg) significantly enhanced the in vivo efficacy of PD-1 antibodies and increased lymphocyte infiltration and function[6]. Treatment of mice with transgenic hepatocyte (TAMH) flank tumors with PD0325901 (20 mg/kg) significantly reduced the activity of MEK in cancer cells and decreased tumor growth rate[7].
References:
[1] You K S, Yi Y W, Cho J, et al. Dual inhibition of AKT and MEK pathways potentiates the anti-cancer effect of gefitinib in triple-negative breast cancer cells[J]. Cancers, 2021, 13(6): 1205.
[2] Brown A P, Carlson T C G, Loi C M, et al. Pharmacodynamic and toxicokinetic evaluation of the novel MEK inhibitor, PD0325901, in the rat following oral and intravenous administration[J]. Cancer chemotherapy and pharmacology, 2007, 59: 671-679.
[3] Chen G, Guo Y, Li C, et al. Small molecules that promote self-renewal of stem cells and somatic cell reprogramming[J]. Stem Cell Reviews and Reports, 2020, 16: 511-523.
[4] Henderson Y C, Chen Y, Frederick M J, et al. MEK inhibitor PD0325901 significantly reduces the growth of papillary thyroid carcinoma cells in vitro and in vivo[J]. Molecular cancer therapeutics, 2010, 9(7): 1968-1976.
[5] Jiang T, Gong Y, Zhang W, et al. PD0325901, an ERK inhibitor, attenuates RANKL‐induced osteoclast formation and mitigates cartilage inflammation by inhibiting the NF-κB and MAPK pathways[J]. Bioorganic Chemistry, 2023, 132: 106321.
[6] Luo M, Xia Y, Wang F, et al. PD0325901, an ERK inhibitor, enhances the efficacy of PD-1 inhibitor in non-small cell lung carcinoma[J]. Acta Pharmaceutica Sinica B, 2021, 11(10): 3120-3133.
[7] Hennig M, Yip‐Schneider M T, Wentz S, et al. Targeting mitogen‐activated protein kinase kinase with the inhibitor PD0325901 decreases hepatocellular carcinoma growth in vitro and in mouse model systems[J]. Hepatology, 2010, 51(4): 1218-1225.
| Cell experiment [1]: | |
Cell lines | PTC cell lines |
Preparation Method | Cells were treated with 0.1μM PD0325901 for 96 hours. |
Reaction Conditions | 0.1μM; 96h |
Applications | PD0325901 significantly inhibits the growth of PTC cells. |
| Animal experiment [2]: | |
Animal models | C57BL/6 mice |
Preparation Method | LLC cells were injected subcutaneously into the flanks of 4-6 week-old female C57BL/6J mice. When the tumors reached approximately 50-100 mm3, the tumor-bearing mice were randomly divided into four groups: control group, PD-1 antibody group, PD0325901 group, and PD0325901+PD-1 antibody group. Control group animals were treated with saline; PD0325901 was orally administered at a dose of 20 mg/kg every other day; PD-1 antibody was injected intraperitoneally once every 4 days (10 mg/kg). |
Dosage form | 20mg/kg; p.o. |
Applications | PD0325901 enhanced the efficacy of PD-1 antibody in vivo, ncreased lymphocytes infiltration and function. |
References: [1] Henderson Y C, Chen Y, Frederick M J, et al. MEK inhibitor PD0325901 significantly reduces the growth of papillary thyroid carcinoma cells in vitro and in vivo[J]. Molecular cancer therapeutics, 2010, 9(7): 1968-1976. [2]Luo M, Xia Y, Wang F, et al. PD0325901, an ERK inhibitor, enhances the efficacy of PD-1 inhibitor in non-small cell lung carcinoma[J]. Acta Pharmaceutica Sinica B, 2021, 11(10): 3120-3133. | |
| Cas No. | 391210-10-9 | SDF | |
| Chemical Name | N-[(2R)-2,3-dihydroxypropoxy]-3,4-difluoro-2-(2-fluoro-4-iodoanilino)benzamide | ||
| Canonical SMILES | C1=CC(=C(C=C1I)F)NC2=C(C=CC(=C2F)F)C(=O)NOCC(CO)O | ||
| Formula | C16H14F3IN2O4 | M.Wt | 482.19 |
| Solubility | ≥ 24.1mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0739 mL | 10.3694 mL | 20.7387 mL |
| 5 mM | 414.8 μL | 2.0739 mL | 4.1477 mL |
| 10 mM | 207.4 μL | 1.0369 mL | 2.0739 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)