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PD0166285 is identified to inhibit Wee1 activity at nanomolar concentrations. The inhibitor abrogates G2/M checkpoint inducing early cell division. This G2 checkpoint abrogation by PD0166285 was demonstrated to kill cancer cells, there at a toxic highest dose of 0.5 muM in some cell lines for exposure periods of no longer than 6 hours. PD0166285 does not inhibit Cdc2/cyclin B but inhibits Chk1 kinase at a much higher concentration (3433 nM).
In vivo, PD0166285 at 0.5 μM concentration can inhibit Cdc2Y15/T14 phosphorylation in all cell lines tested, regardless of their p53 status and pharmacological targeting of WEE1 by PD0166285 sensitizes U251-FM GBM tumors to IR in vivo.
| Cell Experiment | |
|---|---|
| Cell lines | B16 mouse melanoma cells |
| Preparation method | B16 cells (1 × 105 cells in 100 mm-dishes) are maintained in medium overnight. In addition, the cells are treated with (0, 0.5, 1.0, or 2.0 μM) PD0166285 (including DMSO vehicle) for indicated times. The cells are washed twice with phosphate-buffered saline (PBS). Next, the cells are trypsinized, so the cell numbers in each dish are determined by using a computed cell-counter (Sysmex CDA-500) according to manufacturer's recommendation. |
| Concentrations | 0.5, 1, 2 μM |
| Incubation time | 4 h, 24 h |
| Animal Experiment | |
|---|---|
| Animal models | Nude mice with implanted GBM cells |
| Formulation | DMSO |
| Dosages | 0, 20, 100, 200, or 400 µM in 100 µl |
| Administration | s.c. |
| Molecular Weight | 512.43 |
| Formula | C26H27Cl2N5O2 |
| CAS Number | 185039-89-8 |
| Solubility (25°C) | DMSO: ≥ 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Checkpoint Products |
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AZD7762 is a potent ATP-competitive checkpoint kinase inhibitor with an IC50 of 5 and <10 nM for CHK1 and CHK2 respectively. |
| BIBR1532
BIBR1532 is a potent and selective telomerase inhibitor with IC50 of 100 nM. BIBR 1532 inhibits the proliferation of JVM13 leukemia cells with an IC50 of 52 μM, and similar effect also occurs in other leukemia cell lines such as Nalm-1, HL-60, and Jurkat. BIBR1532 is also an inhibitor of TERT, the rate-limiting enzyme in the regulation of telomerase activity. |
| PF-477736
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| SCH 900776
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| Rabusertib (LY2603618)
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