Product Name

PD0325901

General description

PD0325901 is an orally bioavailable, synthetic organic molecule targeting mitogen-activated protein kinase kinase with potential antineoplastic activity.

Synonym

N-[(2R)-2,3-dihydroxypropoxy]-3,4-difluoro-2-(2-fluoro-4-iodoanilino)benzamide

Purity

≥98.0%(HPLC)

CAS Number

391210-10-9

Formula

C¹⁶H¹⁴F³IN²O⁴

Molecular Weight

482.19

Suitability

BioReagent, suitable for cell culture, etc.

l  Physical and Chemical Information

Appearance

Solid

Solubility(25℃)

DMSO

≥50mg/mL

Ethanol

≥35mg/mL

Water

Insoluble

l  Biological Information

Biochem/Physiol  Actions

PD0325901 is an orally bioavailable, synthetic organic molecule targeting mitogen-activated protein kinase kinase (MAPK/ERK kinase or MEK) with potential antineoplastic activity. MEK inhibitor PD325901, a derivative of MEK inhibitor CI 1040, selectively binds to and inhibits MEK, which may result in the inhibition of the  phosphorylation and activation of MAPK/ERK and the inhibition of tumor cell proliferation. 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.

PD0325901 is a selective and non ATP-competitive MEK inhibitor with IC50 of 0.33 nM in cell-free assays, roughly 500-fold more potent than CI-1040 on phosphorylation of ERK1 and ERK2.

l  Storage

Storage temp.

-20℃

l  Precautions and Disclaimer

This product is for R&D use only, not for drug, household, or other uses.

l  References

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.    https://www.ncbi.nlm.nih.gov