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PD0325901
- Mirdametinib
- Optical Purity: Optically pure
- Soluble in DMSO
- MF: C16H14F3IN2O4
- MW: 482.19
Description
PD0325901 (Mirdametinib) is a potent, highly selective and non-ATP-competitive MEK (MAP2K) inhibitor with high affinities at both MEK1 and MEK2 receptors. Developed as an optimized derivative of PD184352 (CI-1040, Axon 1368), PD0325901 exhibits improved bioavailability and effectively suppresses MEK-dependent phosphorylation of ERK1/2, resulting in inhibition of MAPK/ERK signaling.
The MEK/ERK pathway is a central regulator of cell proliferation, differentiation, survival, and developmental signaling and is frequently dysregulated in cancer and RAS/MAPK pathway disorders. PD0325901 is widely used as a research tool in oncology, signal transduction, developmental biology, and stem cell research. Together with CHIR99021 (Axon 1386), PD0325901 forms the classic 2i culture system (Axon 2128), which supports maintenance of naïve pluripotency and self-renewal in embryonic stem cells and induced pluripotent stem cells. PD0325901 is also the core component of several widely used stem cell Inhibitor Set(s).
Key Features
- Potent and highly selective non-ATP-competitive MEK inhibitor
- Suppresses ERK1/2 phosphorylation and MAPK signaling
- Improved bioavailability compared to PD184352 (CI-1040)
- Core component of the widely used 2i and other stem cell culture systems
- Clinically developed as Mirdametinib for RAS/MAPK pathway disorders
Applications
- MEK/ERK and MAPK signaling research
- Cancer and RAS pathway studies
- Embryonic stem cell and iPSC culture
- Naïve pluripotency and cellular reprogramming research
- Developmental biology and regenerative medicine studies
*Promotion: CHIR99021 is also part of Inhibitor Set(s):
| Stem Cell 2i inhibitor Set (Axon 2128) |
| Stem Cell 4i inhibitor Set (Axon 5009) |
| Naive Stem Cell NHSM inhibitor Set (Axon 5010) |
| Naive Stem Cell 5i inhibitor Set (Axon 5011) |
Prime Source Information:
PD0325901 from Axon Medchem has been procured by many labs as drug standard for generating reliable and reproducible biological data, evidenced by many recent publications.
More Information
| Parent CAS No. | 391210-10-9 |
|---|---|
| Chemical Name | N-((R)-2,3-Dihydroxy[propoxy)-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide |
| extra_info | . |
| SMILES | C([C@@H](CO)O)ONC(=O)C1=C(NC2C(F)=CC(I)=CC=2)C(F)=C(F)C=C1 |&1:1,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C16H14F3IN2O4/c17-11-3-2-10(16(25)22-26-7-9(24)6-23)15(14(11)19)21-13-4-1-8(20)5-12(13)18/h1-5,9,21,23-24H,6-7H2,(H,22,25)/t9-/m1/s1 |
| InChiKey | SUDAHWBOROXANE-SECBINFHSA-N |
| CID | 9826528 |
| Short Description | MEK1 inhibitor |
References
- J Bain et al. The selectivity of protein kinase inhibitors: a further update.Biochem J. 2007, 408(Pt 3), 297–315.
- QL Ying et al. The ground state of embryonic stem cell self-renewal. Nature, 2008, 453, 519-523.
- SD Barrett et al. The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901. Bioorg. Med. Chem. Lett. 2008, 18, 6501-6504.
- C Frémin and S Meloche. From basic research to clinical development of MEK1/2 inhibitors for cancer therapy. J. Hematol. Oncol. 2010, 3, 8.
- List of publications using PD0325901 (Axon 1408) purchased from Axon Medchem
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