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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;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;PD 0325901
N-[(2R)-2,3-Dihydroxypropoxy]-3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]benzamide | | CAS: | 391210-10-9 | | MF: | C16H14F3IN2O4 | | MW: | 482.19 | | EINECS: | 687-152-7 | | Product Categories: | MAPK;Inhibitor;Inhibitors;Aromatics;Chiral Reagents;Intermediates & Fine Chemicals;Pharmaceuticals;API | | Mol File: | 391210-10-9.mol |  |
| | 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 |
| 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) 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 0325901 Preparation Products And Raw materials |
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