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.

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

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

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] The biological profile of PD0325901: A second generation analog of CI-1040 with improved pharmaceutical potential
[2] LUDOVICA CIUFFREDA . Growth-Inhibitory and Antiangiogenic Activity of the MEK Inhibitor PD0325901 in Malignant Melanoma with or without BRAF Mutations[J]. Neoplasia, 2009, 11 8: Pages 720-731, W1-W6. DOI:10.1593/neo.09398
[3] ZHIYING AI. Maintenance of Self-Renewal and Pluripotency in J1 Mouse Embryonic Stem Cells through Regulating Transcription Factor and MicroRNA Expression Induced by PD0325901[J]. Stem Cells International, 2015, 2016 1. DOI:10.1155/2016/1792573
[4] CUIPING LI. MEK inhibitor PD0325901 and vitamin C synergistically induce hypomethylation of mouse embryonic stem cells.[J]. Oncotarget, 2016: 39730-39739. DOI:10.18632/oncotarget.9452
[5] WENLIN LI. Generation of rat and human induced pluripotent stem cells by combining genetic reprogramming and chemical inhibitors.[J]. Cell stem cell, 2009, 4 1: 16-19. DOI:10.1016/j.stem.2008.11.014

PD 0325901(391210-10-9)Related Product Information

• PD 123319 ditrifluoroacetate
• PD 166285
• PD173955
• PD 166793
• PD 98059
• PD184352
• PD318088
• PRND
• Y27632 (hydrochloride)
• Selumetinib
• MK-2206 2HCl
• SB 431542
• Trametinib
• CHIR-99021
• PD 166866
• PD 173074
• 2-Fluoro-4-iodoaniline
• PD 0325901