Polo-like Kinase Inhibitor III
GW843682X
CAS: 660868-91-7
Molecular Formula: C22H18F3N3O4S
Polo-like Kinase Inhibitor III - Names and Identifiers
Polo-like Kinase Inhibitor III - Physico-chemical Properties
| Molecular Formula | C22H18F3N3O4S |
| Molar Mass | 477.46 |
| Density | 1.45±0.1 g/cm3(Predicted) |
| Boling Point | 609.1±65.0 °C(Predicted) |
| Solubility | DMSO: >10mg/mL |
| Appearance | solid |
| Color | off-white |
| pKa | 15.03±0.50(Predicted) |
| Storage Condition | 2-8°C |
| MDL | MFCD09971143 |
| Use | GW843682X |
| In vitro study | GW843682X (compound 1) is effective on inhibition of growth of tumor cells, with IC 50 s of 0.41, 0.57, 0.11, 0.38, and 0.70 μM for A549, BT474, HeLa, H460 and HCT116 cell lines. GW843682X dose-dependently inhibits PLK1 phosphorylation of Ser15-p53, with an IC 50 of 0.14 μM. GW843682X (3 μM) causes a strong G2-M arres in HDF cells and H460 cells after treatment for 24, 48, and 72 h. GW843682X (5 μM) leads to apoptosis in H460 cells instead of HDF cells. GW843682X inhibits proliferation of U937 cells with an EC 50 of 120 nM. GW843682X (500 nM) in combination with 5 µM VP-16 suppresses 50% of entry into mitosis in U937 cells. GW843682X (0.06-1 μM) has inhibitory activities against proliferation of acute leukemia cells, and potentiates the anti-proliferative activity of vincristine. Moreover, GW843682X (0.1-1 μM) induces apoptosis of leukemia cells in a dose- and time-dependent manner. GW843682X (0.5-1 μM) dephosphorylates Bcl-xl in leukemia cells. |
Polo-like Kinase Inhibitor III - Risk and Safety
| Hazard Symbols | Xi - Irritant |
| Risk Codes | 36/37/38 - Irritating to eyes, respiratory system and skin. |
| Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36/37 - Wear suitable protective clothing and gloves. |
| WGK Germany | 3 |
Polo-like Kinase Inhibitor III - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.094 ml | 10.472 ml | 20.944 ml |
| 5 mM | 0.419 ml | 2.094 ml | 4.189 ml |
| 10 mM | 0.209 ml | 1.047 ml | 2.094 ml |
| 5 mM | 0.042 ml | 0.209 ml | 0.419 ml |
Last Update：2024-01-02 23:10:35
Polo-like Kinase Inhibitor III - Reference Information
| biological activity | GW843682X is selective, ATP-competitive PLK1 and PLK3 inhibitors, IC50 values are 2.2 nM and 9.1 nM respectively, and the selectivity is more than 100 times that of other 30 kinases. |
| target | PLK1 2.2 nM (IC 50 ) PLK3 9.1 nM (IC 50 ) PDGFR1β 160 nM (IC 50 ) VEGFR2 360 nM (IC 50 ) Aurora A 4800 nM (IC 50) CDK2/Cyclin A 7600 nM (IC 50 ) |
| in vitro study | GW843682X (compound 1) is effective on inhibition of growth of tumor cells, with IC 50 s of 0.41, 0.57, 0.11, 0.38, and 0.70 μ m for a549, bt474, hela, h460 and hct116 cell lines. GW843682X dose-dependently inhibits PLK1 phosphorylation of Ser15-p53, with an IC 50 of 0.14 μ m. GW843682X (3 μ m) causesa strong G2-M arres in HDF cells and H460 cells after treatment for 24, 48, and 72 h. GW843682X (5 μ m) led to apoptosis in H460 cells instead of HDF cells. GW843682X inhibits proliferation of U937 cells with an EC 50 of 120 nm. GW843682X (500 nm) in combination with 5 m VP-16 suppresses 50% entry into mitosis in U937 cells. GW843682X (0.06-1 μM) has inhibitory activities against proliferation of acute leukemia cells, and potentiates the anti-proliferative activity of vincristine. Moreover, GW843682X (0.1-1 μM) induces apoptosis of leukemia cells in a dose- and time-dependent manner. GW843682X (0.5-1 μM) dephosphorylates Bcl-xl in leukemia cells. |
Last Update：2024-04-09 21:54:55
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CAS: 660868-91-7
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CAS: 660868-91-7
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Product Name: GW843682X Visit Supplier Webpage Request for quotation
CAS: 660868-91-7
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 660868-91-7
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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