PD325901
N-{[(2R)-2,3-dihydroxypropyl]oxy}-3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]benzamide
CAS: 391210-10-9;870474-62-7
Molecular Formula: C16H14F3IN2O4
PD325901 - Names and Identifiers
PD325901 - Physico-chemical Properties
| Molecular Formula | C16H14F3IN2O4 |
| Molar Mass | 482.19 |
| Density | 1.817±0.06 g/cm3(Predicted) |
| Melting Point | 112-114°C |
| Solubility | Soluble in DMF (~25 mg/ml), DMSO (96 mg/ml at 25 °C), ethanol (40 mg/ml at 25 °C) |
| Appearance | White to off-white solid |
| Color | white to off-white |
| pKa | 13.45±0.20(Predicted) |
| Storage Condition | 2-8°C |
| 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. |
| Refractive Index | 1.645 |
| Use | An inhibitor of MEK and suppressor of ERK phosphorylation |
| In vitro study | PD0325901 has a higher permeability than another MEK inhibitor CI-1040. Compared with CI-1040, PD 0325901 can reach the deeper layer of the system. PD0325901 is a non-ATP competitive MAPK kinase MEK inhibitor with an IC50 of 0.33nM for inhibition of MEK in murine colon 26 cells. The threonine/tyrosine kinase MEK is a key component of the RAS/RAF/MEK/ERK signaling pathway and is normally activated in human tumor cells. PD0325901 inhibited MEK accurately and effectively, with a K I value of 1nm when acting on MEK1 and mek2. The phosphorylation effect of PD0325901 on ERK1 and ERK2 was about 500 times stronger than that of CI-1040. |
| In vivo study | PD0325901 prevents the growth of melanoma cell lines, so that the cell cycle of the xenograft mouse model stops in the G1 phase, causing apoptosis after oral administration of 25 mg/kg PD032590124 alone, the phosphorylation of ERK was blocked by more than 50%. The anti-cancer activity of PD 0325901 has been used in the study of a wider range of human transplanted tumors, and in the human tumor model studied, 6/7 was significantly inhibited by PD 0325901. PD0325901 inhibits the growth of malignant melanoma cell lines. PD0325901 inhibited the growth of TPC-1 cells and K2 cells with GI50 of 11 and 6.3 nM, respectively. PD0325901 also significantly inhibited the growth of PTC cells carrying BRAF mutations at very low concentrations (10 nM) and only slightly increased the growth of PTC cells carrying RET/PTC1 rearrangements at the same concentrations. PD0325901 acts on a variety of PTC cell lines and effectively inhibits ERK1/2 phosphorylation. |
PD325901 - Risk and Safety
| Risk Codes | R25 - Toxic if swallowed R48 - Danger of serious damage to health by prolonged exposure R50 - Very Toxic to aquatic organisms |
| Safety Description | S22 - Do not breathe dust. S36/37/39 - Wear suitable protective clothing, gloves and eye/face protection. S61 - Avoid release to the environment. Refer to special instructions / safety data sheets. |
| UN IDs | UN 2811 6.1 / PGIII |
| WGK Germany | 3 |
| HS Code | 29242990 |
| Hazard Class | IRRITANT |
PD325901 - Introduction
PD0325901 is a selective, ATP non-competitive MEK inhibitor with IC50 of 0.33 nM, which is about 500 times stronger than CI-1040.
Last Update：2022-10-16 17:25:03
PD325901 - Reference Information
| use | N-[(2R)-2, 3-dihydroxypropoxy]-3, 4-Difluoro-2-[(2-fluoro-4-iodobenzene) amino] benzamide is a mitogenic extracellular kinase 1/2(MEK1 / 2) inhibitor; strong activity. Detection of cancer cell types in vitro. Selective MEK inhibitors. |
| biological activity | Mirdametinib (PD0325901) is a selective, non-ATP competitive MEK inhibitor. IC50 is 0.33 nM in cell-free test, and its inhibitory effect on phosphorylation of ERK1 and ERK2 is about 500 times stronger than that of CI-1040. Phase 2. |
| target | TargetValue MEK (Cell-free say) 0.33 nM |
| Target | Value |
| MEK (Cell-free assay) | 0.33 nM |
| in vitro study | PD0325901 has higher permeability than another MEK inhibitor CI-1040. Compared with CI-1040, PD 0325901 can reach a deeper level of the system. PD0325901 is a non-ATP competitive MAPK kinase MEK inhibitor, and IC50 is 0.33nM when MEK of murine colon 26 cells is inhibited. Threonine/tyrosine kinase MEK is a key component of the RAS/RAF/MEK/ERK signaling pathway and is usually activated in human tumor cells. PD0325901 accurately and effectively inhibit MEK, the value of K I is 1nM when it acts on MEK1 and MEK2. The phosphorylation effect of PD0325901 on cell ERK1 and ERK2 is about 500 times stronger than that of CI-1040. |
| in vivo study | PD0325901 prevent the growth of melanoma cell lines, stop the cell cycle of xenograft mouse model in G1 phase, and cause apoptosis. after oral administration of 25 mg/kg PD032590124 alone, the phosphorylation of ERK was blocked to more than 50%. The anticancer activity of PD 0325901 has been used in the wider study of human transplanted tumors. In the human tumor models studied, 6/7 was significantly inhibited by PD 0325901. PD0325901 inhibits the growth of malignant melanoma cell lines. PD0325901 inhibit the growth of TPC-1 cells and K2 cells, GI50 is 11 and 6.3 nM respectively. Very low PD0325901 concentration (10 nM) also significantly inhibited the growth of PTC cells carrying BRAF mutation, and only slightly increased the growth of PTC cells carrying RET/PTC1 rearrangement at the same concentration. PD0325901 acts on a variety of PTC cell lines and effectively inhibits ERK1/2 phosphorylation. |
Last Update：2024-04-09 20:45:29
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Tel: 609-228-6898
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