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Chemical Structure| 185039-89-8 Chemical Structure| 185039-89-8

Structure of PD0166285
CAS No.: 185039-89-8

Chemical Structure| 185039-89-8

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PD0166285 inhibits Wee1 and Chk1 at nanomolar concentrations and can hinder G2 checkpoint.

4.5 *For Research Use Only !

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Product Details of PD0166285

CAS No. :185039-89-8
Formula : C26H27Cl2N5O2
M.W : 512.43
SMILES Code : O=C1C(C2=C(Cl)C=CC=C2Cl)=CC3=CN=C(NC4=CC=C(OCCN(CC)CC)C=C4)N=C3N1C
MDL No. :MFCD00950060
InChI Key :IFPPYSWJNWHOLQ-UHFFFAOYSA-N
Pubchem ID :5311382

Safety of PD0166285

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • Wee1

    Wee1, IC50:24 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
MCF10A cells 1 μM PD0166285 shortens G2 phase and overcomes the cycloheximide-induced G2 arrest PMC7802425
Calu1 0 nM, 200 nM, 400 nM, 800 nM 48 hours PD0166285 significantly reduced the number and size of cell colonies and showed anti-tumor effects through CCK8 assay. PMC11396119
NCI-H520 0 nM, 200 nM, 400 nM, 800 nM 48 hours PD0166285 significantly reduced the number and size of cell colonies and showed anti-tumor effects through CCK8 assay. PMC11396119
NCI-H226 0 nM, 200 nM, 400 nM, 800 nM 48 hours PD0166285 significantly reduced the number and size of cell colonies and showed anti-tumor effects through CCK8 assay. PMC11396119
HeLa cells 20 nM BTZ and 0.25 μM 24 h To evaluate the ability of BSA–RuII(CO)2 complex to release CO in HeLa cells, results showed a significant increase in intracellular fluorescence indicating CO release. PMC11239683
SNU449 cells 20 nM BTZ and 0.25 μM 24 h PD0166285 abrogated BTZ-induced G2-phase arrest, promoted mitotic entry, and exacerbated BTZ-induced pyroptosis. PMC11239683
Calu1 0 nM, 200 nM, 400 nM, 800 nM 48 hours PD0166285 significantly reduced the number and size of cell colonies and showed anti-tumor effects through CCK8 assay. PMC11396119
NCI-H520 0 nM, 200 nM, 400 nM, 800 nM 48 hours PD0166285 significantly reduced the number and size of cell colonies and showed anti-tumor effects through CCK8 assay. PMC11396119
NCI-H226 0 nM, 200 nM, 400 nM, 800 nM 48 hours PD0166285 significantly reduced the number and size of cell colonies and showed anti-tumor effects through CCK8 assay. PMC11396119

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice LUSC nude mouse model Intraperitoneal injection 10 mg/kg Tumor size was measured every 2 days for 2 weeks Combination therapy of PD0166285 and cisplatin significantly inhibited tumor growth and increased apoptosis. PMC11396119
C57BL/6J mice Hepa1-6 subcutaneous xenograft model Intraperitoneal injection BTZ (0.65 mg/kg) and PD0166285 (0.26 mg/kg) Every three days for five times BP-Combo significantly suppressed tumor growth and metastasis, prolonged survival of tumor-bearing mice with no obvious toxicity. PMC11239683
Nude mice LUSC xenograft model 10 mg/kg 2 weeks To evaluate the inhibitory effect of PD0166285 combined with cisplatin on LUSC tumor growth, results showed that the combination therapy significantly suppressed tumor growth. PMC11396119
Xenopus laevis embryos Early embryonic cell cycles Pretreated for 2-2.5 hours prior to fertilization and maintained at the same concentration after fertilization and jelly coat removal 50 μM Single treatment, continued until the end of the first cell cycle Investigate the effect of Wee1/Myt1 inhibition on embryonic cell cycle and viability. PD0166285 treatment significantly shortened the first cell cycle duration and dramatically reduced embryo viability. PMC3921120

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.95mL

0.39mL

0.20mL

9.76mL

1.95mL

0.98mL

19.51mL

3.90mL

1.95mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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