PD0325901 --- MEK Inhibitor


Catalog No. size PriceQuantity
M60018-2D 10 mM in DMSO (0.415 mL) $79
M60018-2S 2 mg solid $79
M60018-25S 25mg solid $350

Description

PD0325901 is a highly potent and selective inhibitor of MEK with an IC50 of 0.33 nM. Its potency, selectivity, and solubility are all better than many other MEK inhibitors (e.g., CI-1040). It can potently inhibit the phosphorylation and activation of MAPK/ERK and tumor cell proliferation. In combination with CHIR99021, PD0325901 has been shown to promote mouse ES cell self-renewal and iPSC generation.

Product information

CAS Number: 391210-10-9

Molecular Weight: 482.19

Formula: C16H14F3IN2O4

Synonym:

Mirdametinib

Chemical Name: N-[(2R)-2,3-Dihydroxypropoxy]-3,4-difluoro-2[(2-fluoro-4-iodophenyl)amino]-benzamide

Smiles: OC[C@@H](O)CONC(=O)C1=CC=C(F)C(F)=C1NC1=CC=C(I)C=C1F

InChiKey: SUDAHWBOROXANE-SECBINFHSA-N

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

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 100 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

PD0325901 was used at 0.01-0.5 µM in vitro and in cellular assays.

In Vivo:

PD0325901 was orally administrated to mice at 25 mg/kg once per day.

References:

  1. Barrett SD, et al. The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901. (2008) Bioorg. Med. Chem. Lett. 18: 6501-6504.
  2. Lin T, et al. A chemical platform for improved induction of human iPSCs. (2009) Nature Methods 6, 805-808.
  3. Henderson YC, et al. MEK inhibitor PD0325901 significantly reduces the growth of papillary thyroid carcinoma cells in vitro and in vivo. (2010) Mol Cancer Ther. 9(7):1968-76.

Products are for research use only. Not for human use.


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