PD 0325901

Synonym(s):InSolution MEK1/2 Inhibitor III, PD0325901 - CAS 391210-10-9 - Calbiochem;MEK1/2 Inhibitor III - CAS 391210-10-9 - Calbiochem;N-[(2R)-2,3-Dihydroxypropoxy]-3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-benzamide;PD 0325901, N-((2R)-2,3-Dihyroxypropoxy)-3,4-difluoro-2-((2-fluoro-4-iodophenyl)amino)-benzamide, PD325901;PD325901, PD0325901, N-((2R)-2,3-Dihyroxypropoxy)-3,4-difluoro-2-((2-fluoro-4-iodophenyl)amino)-benzamide, PD 0325901, MEK Inhibitor III

CAS NO.：391210-10-9
Empirical Formula: C16H14F3IN2O4
Molecular Weight: 482.19
MDL number: MFCD08435926
EINECS: 687-152-7
SAFETY DATA SHEET (SDS)
Update Date: 2023-06-30 15:45:59

What is PD 0325901?

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

The Uses of PD 0325901

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).

The Uses of PD 0325901

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

Properties of PD 0325901

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.

Safety information for PD 0325901

Signal word	Danger
Pictogram(s)	Skull and Crossbones Acute Toxicity GHS06 Health Hazard GHS08
GHS Hazard Statements	H301:Acute toxicity,oral H373:Specific target organ toxicity, repeated exposure H413:Hazardous to the aquatic environment, long-term hazard
Precautionary Statement Codes	P260:Do not breathe dust/fume/gas/mist/vapours/spray. P264:Wash hands thoroughly after handling. P264:Wash skin thouroughly after handling. P270:Do not eat, drink or smoke when using this product. P273:Avoid release to the environment. P314:Get medical advice/attention if you feel unwell. P301+P310:IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.