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391210-10-9-PD-0325901 PD-0325901

PD-0325901

For research use only. Not for therapeutic Use.

  • CAT Number: I003435
  • CAS Number: 391210-10-9
  • Molecular Formula: C₁₆H₁₄F₃IN₂O₄
  • Molecular Weight: 482.20
  • Purity: ≥95%
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PD-0325901（Cat No.:I003435）is a highly selective and potent inhibitor of MEK1 and MEK2, essential components of the MAPK/ERK signaling pathway that regulate cell growth, differentiation, and survival. By blocking MEK1/2, PD-0325901 prevents ERK phosphorylation and activation, disrupting downstream signaling involved in tumor cell proliferation. It has been widely studied for its potential in treating cancers, particularly those with RAS and RAF mutations, such as melanoma and colorectal cancer. PD-0325901 is a valuable tool in cancer research and drug development, exploring targeted therapies that inhibit aberrant MAPK/ERK signaling.


Catalog Number I003435
CAS Number 391210-10-9
Synonyms

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

Molecular Formula C₁₆H₁₄F₃IN₂O₄
Purity ≥95%
Target MEK1/2
Solubility DMSO: ≥ 20 mg/mL, H2O: ＜ 1 mg/mL
Storage 3 years -20C powder
IUPAC Name N-[(2R)-2,3-dihydroxypropoxy]-3,4-difluoro-2-(2-fluoro-4-iodoanilino)benzamide
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
SMILES C1=CC(=C(C=C1I)F)NC2=C(C=CC(=C2F)F)C(=O)NOC[C@@H](CO)O
Reference

1: Shannon S, Jia D, Entersz I, Beelen P, Yu M, Carcione C, Carcione J, Mahtabfar
A, Vaca C, Weaver M, Shreiber D, Zahn JD, Liu L, Lin H, Foty RA. Inhibition of
glioblastoma dispersal by the MEK inhibitor PD0325901. BMC Cancer. 2017 Feb
10;17(1):121. doi: 10.1186/s12885-017-3107-x. PubMed PMID: 28187762; PubMed
Central PMCID: PMC5303286.

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2: Paulo JA, McAllister FE, Everley RA, Beausoleil SA, Banks AS, Gygi SP. Effects
of MEK inhibitors GSK1120212 and PD0325901 in vivo using 10-plex quantitative
proteomics and phosphoproteomics. Proteomics. 2015 Jan;15(2-3):462-73. doi:
10.1002/pmic.201400154. Epub 2014 Oct 18. PubMed PMID: 25195567; PubMed Central
PMCID: PMC4515953.
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3: Sheth PR, Liu Y, Hesson T, Zhao J, Vilenchik L, Liu YH, Mayhood TW, Le HV.
Fully activated MEK1 exhibits compromised affinity for binding of allosteric
inhibitors U0126 and PD0325901. Biochemistry. 2011 Sep 20;50(37):7964-76. doi:
10.1021/bi200542r. Epub 2011 Aug 26. PubMed PMID: 21793567.
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4: Henderson YC, Chen Y, Frederick MJ, Lai SY, Clayman GL. MEK inhibitor
PD0325901 significantly reduces the growth of papillary thyroid carcinoma cells
in vitro and in vivo. Mol Cancer Ther. 2010 Jul;9(7):1968-76. doi:
10.1158/1535-7163.MCT-10-0062. Epub 2010 Jun 29. PubMed PMID: 20587665; PubMed
Central PMCID: PMC2935263.

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5: Brown AP, Carlson TC, Loi CM, Graziano MJ. Pharmacodynamic and toxicokinetic
evaluation of the novel MEK inhibitor, PD0325901, in the rat following oral and
intravenous administration. Cancer Chemother Pharmacol. 2007 Apr;59(5):671-9.
Epub 2006 Aug 31. PubMed PMID: 16944149.

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6: Huang W, Yang AH, Matsumoto D, Collette W, Marroquin L, Ko M, Aguirre S,
Younis HS. PD0325901, a mitogen-activated protein kinase kinase inhibitor,
produces ocular toxicity in a rabbit animal model of retinal vein occlusion. J
Ocul Pharmacol Ther. 2009 Dec;25(6):519-30. doi: 10.1089/jop.2009.0060. PubMed
PMID: 19929595.

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