| Identification | Back Directory | [Name]
PD 0325901 | [CAS]
391210-10-9 | [Synonyms]
PD325901
PD 0325901
PD-0235901
N-[(2R)-2,3-Dihydroxypropoxy]-3,4-difluoro-2-[(2-fluoro-4-iodophenyl)aMino]be
(R)-N-(2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodophenylamino)benzamide
N-[(R)-2,3-Dihydroxy-propoxy]-3,4-difluoro-2-(2-fluoro-4-iodo-phenylaMino)-benzaMide
N-[(2R)-2,3-DIHYDROXYPROPOXY]-3,4-DIFLUORO-2-[(2-FLUORO-4-IODOPHENYL)AMINO]-BENZAMIDE
PD 0325901
N-[(2R)-2,3-Dihydroxypropoxy]-3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]benzamide
N-[(2R)-2,3-Dihydroxypropoxy]-3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]benzamide PD0325901 | [EINECS(EC#)]
687-152-7 | [Molecular Formula]
C16H14F3IN2O4 | [MDL Number]
MFCD08435926 | [MOL File]
391210-10-9.mol | [Molecular Weight]
482.191 |
| Chemical Properties | Back Directory | [Melting point ]
112-114°C | [density ]
1.817±0.06 g/cm3(Predicted) | [storage temp. ]
Store at-20°C | [solubility ]
DMSO: soluble20mg/mL, clear | [form ]
White to off-white solid | [pka]
13.45±0.20(Predicted) | [color ]
white to off-white | [Optical Rotation]
[α]/D -1.8 to -3.5°, c = 1 mg/mL in methanol | [Stability:]
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months. | [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]
C(NOC[C@H](O)CO)(=O)C1=CC=C(F)C(F)=C1NC1=CC=C(I)C=C1F |
| Hazard Information | Back Directory | [Chemical Properties]
White to Off-White Solid | [Usage]
The mitogenic extracellular kinase 1/2 (MEK1/2) inhibitor | [Description]
PD 325901 (391210-10-9) is a selective non-ATP competitive MEK inhibitor (IC50 = 0.33 nM).1 Inhibits growth and/or proliferation of a variety of cancer cells.2 Enhances self-renewal of embryonic stem cells.3 In combination with vitamin C, synergistically induces hypomethylation of mouse embryonic stem cells.4 In combination with CHIR-99021 and A83-01 induces generation of ground state iPS cells from human and rat somatic cells.5 | [Uses]
PD 0325901 has been used as an inhibitor in extracellular signal-regulated kinase (ERK) inhibition assay in primed induced pluripotent stem cells, RKO colorectal cancer cell line and human embryonic stem cells(hESCs). | [Uses]
The mitogenic extracellular kinase 1/2 (MEK1/2) inhibitor | [Definition]
ChEBI: A hydroxamic acid ester that is benzhydroxamic acid (N-hydroxybenzamide) in which the hydroxamic acid group has been converted to the corresponding 2,3-dihydroxypropyl ester and in which the benzene ring has been substituted at position
by a (2-fluoro-4-iodophenyl)amino group and at positions 3 and 4 by fluorines (the R enantiomer). | [Biochem/physiol Actions]
PD 0325901 is a potent MKK1 (MEK1) and MKK2 (MEK2) inhibitor. The Ki is 1.1 and 0.79 nM for MEK1 and MEK2, respectively. PD 0325901 was inactive against a panel of 27 other kinases. PD 0325901 inhibited C26 tumor pERK by 75% when dosed at 25 mg/kg in mice. | [storage]
-20°C | [References]
1) Sebolt-Leopold et al. (2004), The biological profile of PD0325901: A second generation analog of CI-1040 with improved pharmaceutical potential; Proc. Amer. Assoc. Cancer Res., 45 925
2) Ciuffreda et al. (2009), Growth-inhibitor and antiangiogenic activity of the MEK inhibitor PD0325901 in malignant melanoma with or without BRAF mutations; Neoplasia, 11 720
3) Ai et al. (2016), Maintenance of Self-Renewal and Pluripotency in J1 Mouse Embryonic Stem Cells through Regulating Transcription Factor and MicroRNA Expression Induced by PD0325901; Stem Cells Int., 2016 1792573
4) Li et al. (2016), MEK inhibitor PD0325901 and vitamin C synergistically induce hypomethylation of mouse embryonic stem cells; Oncotarget, 7 39730
5) Li et al. (2009), Generation of rat and human induced pluripotent stem cells by combining genetic reprogramming and chemical inhibitors; Cell Stem Cell, 4 16 |
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