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PD0166285

Cat. No. M9208
PD0166285 Structure
Synonym:

PD166285

Size Price Availability Quantity
10mM*1mL USD 167  USD167 In stock
5mg USD 147  USD147 In stock
10mg USD 237  USD237 In stock
25mg USD 535  USD535 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

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.

Protocol
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.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 512.43
Formula C26H27Cl2N5O2
CAS Number 185039-89-8
Purity >98%
Solubility DMSO: ≥ 60 mg/mL
Storage at -20°C
References

[1] Mir SE, et al. Cancer Cell. In silico analysis of kinase expression identifies WEE1 as a gatekeeper against mitotic catastrophe in glioblastoma.

[2] Hashimoto O, et al. BMC Cancer. Cell cycle regulation by the Wee1 inhibitor PD0166285, pyrido [2,3-d] pyimidine, in the B16 mouse melanoma cell line.

[3] Wang Y, et al. Cancer Res. Radiosensitization of p53 mutant cells by PD0166285, a novel G(2) checkpoint abrogator.

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  Catalog
Abmole Inhibitor Catalog




Keywords: PD0166285, PD166285 supplier, Checkpoint, inhibitors

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