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PD 0325901

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PD 0325901 Basic information

Product Name:
PD 0325901
Synonyms:
  • N-[(2R)-2,3-DIHYDROXYPROPOXY]-3,4-DIFLUORO-2-[(2-FLUORO-4-IODOPHENYL)AMINO]-BENZAMIDE
  • PD 0325901
  • (R)-N-(2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodophenylamino)benzamide
  • PD-0235901
  • N-[(2R)-2,3-Dihydroxypropoxy]-3,4-difluoro-2-[(2-fluoro-4-iodophenyl)aMino]be
  • PD325901
  • 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 PD0325901
CAS:
391210-10-9
MF:
C16H14F3IN2O4
MW:
482.19
EINECS:
687-152-7
Product Categories:
  • MAPK
  • Inhibitor
  • Aromatics
  • Chiral Reagents
  • Intermediates & Fine Chemicals
  • Inhibitors
  • API
  • Pharmaceuticals
Mol File:
391210-10-9.mol
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PD 0325901 Chemical Properties

Melting point:
112-114°C
Density 
1.817±0.06 g/cm3(Predicted)
storage temp. 
2-8°C
solubility 
DMSO: soluble20mg/mL, clear
form 
White to off-white solid
pka
13.45±0.20(Predicted)
color 
white to off-white
optical activity
[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.
InChIKey
SUDAHWBOROXANE-SECBINFHSA-N
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Safety Information

Hazard Codes 
T,N
Risk Statements 
25-48-50
Safety Statements 
22-36/37/39-61
RIDADR 
UN 2811 6.1 / PGIII
WGK Germany 
3
HazardClass 
IRRITANT
HS Code 
29242990
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PD 0325901 Usage And Synthesis

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

Chemical Properties

White to Off-White Solid

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

PD 0325901Supplier

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