A MEK inhibitor that sustains stem cell renewal
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PD 0325901

Item No. 13034

Technical Information
Formal Name
N-[(2R)-2,3-dihydroxypropoxy]-3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-benzamide
CAS Number
391210-10-9
Synonyms
  • Mirdametinib
Molecular Formula
C16H14F3IN2O4
Formula Weight
Purity
≥90%
A crystalline solid
DMF: 25 mg/mlDMSO: 25 mg/mlEthanol: 20 mg/ml
λmax
238, 276, 313 nm
SMILES
FC1=C(F)C(NC2=CC=C(I)C=C2F)=C(C(NOC[C@H](O)CO)=O)C=C1
InChi Code
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
InChi Key
SUDAHWBOROXANE-SECBINFHSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    The dual specific threonine/tyrosine kinase MEK is a key component of the RAS/RAF/MEK/ERK signaling pathway that is frequently activated in human tumors.1,2 PD 0325901 is a potent MEK inhibitor that suppresses phosphorylation of ERK in mouse colon 26 tumors with an IC50 value of 0.33 nM.3 Suppression of ERK activation with 1 µM PD 0325901 combined with 3 µM CHIR99021 (a glycogen synthase kinase 3 inhibitor) prevents cell differentiation and sustains self renewal of mouse embryonic stem cells for at least eight passages.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Vojtek, A.B., and Der, C.J. Increasing complexity of the Ras signaling pathway. The Journal of Biological Chemisty 273, 19925-19928 (1998).

    2. Dorsam, R.T., and Gutkind, J.S. G-protein-coupled receptors and cancer. Nat. Rev. Cancer 7(2), 79-94 (2007).

    3. Barret, S.D., Bridges, A.J., Dudley, D.T., et alThe discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901. Bioorg. Med. Chem. Lett. 18, 6501-6504 (2008).

    4. Ying, Q.L., Wray, J., Nichols, J., et alThe ground state of embryonic stem cell self-renewal. Nature 453(7194), 519-524 (2008).

    Product Citations

    Ioannou, Y.A. The structure and function of the niemann-pick C1 protein. Mol. Genet. Metab. 71(1-2), 175-181 (2000).

    Wang, Q., Geng, Z., Gong, Y., et alWDR68 is essential for the transcriptional activation of the PRC1-AUTS2 complex and neuronal differentiation of mouse embryonic stem cells. Stem Cell Res. 33, 206-214 (2018).