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: 2026-07-16 07:06:08
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. |
Computed Descriptors for PD 0325901
| InChIKey | SUDAHWBOROXANE-SECBINFHSA-N |
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