PD0166285
Based on 8 publication(s) in Google Scholar
PD0166285, a substrate of P-gp, is a WEE1 inhibitor and a weak Myt1 inhibitor with IC50 values of 24 and 72 nM, respectively. PD0166285 exhibits an IC50 of 3.433 μM for Chk1.
For research use only. We do not sell to patients.
- Purity: 99.46%
- CAS No.: 185039-89-8
- Formula: C26H27Cl2N5O2
- Molecular Weight:512.43
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) PD0166285
More- Acta Pharm Sin B. 2026 Feb.
- Clin Cancer Res. 2020 Jul 1;26(13):3431-3442. [Abstract]
- Cancer Cell Int. 2024 Sep 13;24(1):315. [Abstract]
- FASEB J. 2025 Jul 31;39(14):e70854. [Abstract]
- Reprod Toxicol. 2022 Jun:110:172-179. [Abstract]
- bioRxiv. 2024 Dec 11:2024.12.02.626470. [Abstract]
- Patent. US20240174977A1.
- bioRxiv. 2020 Jun.
Biological Activity
IC50: 24 nM (WEE1), 72 nM (Myt1), 3.433 μM (Chk1)[1].
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| C6 | IC50 |
0.005 μM
Compound: 2a
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Inhibition of PDGF-stimulated Platelet-derived growth factor receptor autophosphorylation in C6 rat glioma cells after 2 hr
Inhibition of PDGF-stimulated Platelet-derived growth factor receptor autophosphorylation in C6 rat glioma cells after 2 hr
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[PMID: 9784112] |
| C6 | IC50 |
0.005 μM
Compound: 63
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Inhibition of PDGF-induced autophosphorylation of PDGF-R in C6 cells
Inhibition of PDGF-induced autophosphorylation of PDGF-R in C6 cells
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[PMID: 9703473] |
| C6 | IC50 |
0.12 μM
Compound: 2a
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C6 glioma 3-day proliferation followed by soft agar growth with continuous treatment
C6 glioma 3-day proliferation followed by soft agar growth with continuous treatment
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[PMID: 9784112] |
| C6 | IC50 |
0.12 μM
Compound: 63
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C6 cell growth in soft agar with continuous treatment
C6 cell growth in soft agar with continuous treatment
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[PMID: 9703473] |
| C6 | IC50 |
0.34 μM
Compound: 2a
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Inhibition of rat C6 glioma cell proliferation in sulforhodamine B assay
Inhibition of rat C6 glioma cell proliferation in sulforhodamine B assay
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[PMID: 9784112] |
| C6 | IC50 |
0.34 μM
Compound: 63
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Inhibition of C6 cell proliferation in sulforhodamine B assay
Inhibition of C6 cell proliferation in sulforhodamine B assay
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[PMID: 9703473] |
| C6 | IC50 |
1.8 μM
Compound: 2a
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C6 glioma 3-day proliferation followed by soft agar growth without treatment
C6 glioma 3-day proliferation followed by soft agar growth without treatment
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[PMID: 9784112] |
| C6 | IC50 |
1.8 μM
Compound: 63
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C6 cell growth in soft agar with discontinued treatment
C6 cell growth in soft agar with discontinued treatment
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[PMID: 9703473] |
| HCT-8 | IC50 |
0.42 μM
Compound: 6q
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Inhibitory activity against HCT-8 human colon adenocarcinoma cells was determined.
Inhibitory activity against HCT-8 human colon adenocarcinoma cells was determined.
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[PMID: 10956222] |
| HEK293 | IC50 |
7.2 nM
Compound: PD0166285
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Binding affinity to human full-length His-tagged Myt1 kinase expressed in HEK293 cells by TR-FRET based binding assay
Binding affinity to human full-length His-tagged Myt1 kinase expressed in HEK293 cells by TR-FRET based binding assay
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[PMID: 22770610] |
| HEK-293T | IC50 |
0.29 μM
Compound: 3; PD-166285
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Antiproliferative activity against HEK293T cells measured after 72 hrs by CellTiter-Blue assay
Antiproliferative activity against HEK293T cells measured after 72 hrs by CellTiter-Blue assay
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[PMID: 28792760] |
| HT-29 | IC50 |
0.28 μM
Compound: 6q
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Inhibitory activity against HT-29 human colon adenocarcinoma cells was determined.
Inhibitory activity against HT-29 human colon adenocarcinoma cells was determined.
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[PMID: 10956222] |
| MDA-MB-231 | IC50 |
0.16 μM
Compound: 3; PD-166285
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Antiproliferative activity against human MDA-MB-231 cells measured after 72 hrs by CellTiter-Blue assay
Antiproliferative activity against human MDA-MB-231 cells measured after 72 hrs by CellTiter-Blue assay
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[PMID: 28792760] |
| MM1.S | IC50 |
0.52 μM
Compound: 3; PD-166285
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Antiproliferative activity against human MM1S cells measured after 72 hrs by CellTiter-Blue assay
Antiproliferative activity against human MM1S cells measured after 72 hrs by CellTiter-Blue assay
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[PMID: 28792760] |
| NIH3T3 | IC50 |
0.0011 μM
Compound: 63
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Growth of NIH3T3 cell colonies in soft agar with continuous treatment
Growth of NIH3T3 cell colonies in soft agar with continuous treatment
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[PMID: 9703473] |
| NIH3T3 | IC50 |
0.0018 μM
Compound: 63
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Inhibition of PDGF-induced autophosphorylation of PDGF-R in NIH3T3 cells
Inhibition of PDGF-induced autophosphorylation of PDGF-R in NIH3T3 cells
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[PMID: 9703473] |
| NIH3T3 | IC50 |
0.01 μM
Compound: 63
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Growth of NIH3T3 cell colonies in soft agar with discontinued treatment
Growth of NIH3T3 cell colonies in soft agar with discontinued treatment
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[PMID: 9703473] |
| NIH3T3 | IC50 |
0.35 μM
Compound: 63
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Inhibition of NIH3T3 proliferation by sulforhodamine B assay
Inhibition of NIH3T3 proliferation by sulforhodamine B assay
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[PMID: 9703473] |
| SW-620 | IC50 |
0.27 μM
Compound: 6q
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Inhibitory activity against SW-620 human colon adenocarcinoma cells was determined.
Inhibitory activity against SW-620 human colon adenocarcinoma cells was determined.
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[PMID: 10956222] |
PD0166285 (0.5 μM) dramatically inhibits irradiation-induced Cdc2 phosphorylation at the Tyr-15 and Thr-14 in seven of seven cancer cell lines[1].
PD0166285 sensitizes radiation-induced cell killing in p53 mutant HT29 cells and in the E6-transfected, p53-null ovarian cancer cell line PA-1 but to a lesser extent in p53 wild-type PA-1 cells. PD0166285 abrogates irradiation-induced G2 arrest and significantly increases mitotic cell populations[1].
PD0166285 acts as a radiosensitizer to sensitize cells to radiation-induced cell death with a sensitivity enhancement ratio of 1.23[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human and mouse cancer cell lines (HCT116, HT29, DLD-1, HCT8, H460, HeLa, C 26).
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Concentration:0.5 μM.
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Incubation Time:4 h.
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Result:Inhibited Cdc2Y15 and CdcT14 phosphorylation.
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Animal Model:Wild-type, Abcg2-/-, Abcb1a/b-/- and Abcb1a/b;Abcg2-/- FVB mice[2].
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Dosage:5 mg/kg.
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Administration:IV.
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Result:Cmax is about 400 ng/mL.
P-gp, but not BCRP, limited the brain penetration of PD0166285.
Chemical Information
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CAS No. 185039-89-8
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Appearance Solid
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Molecular Weight 512.43
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Formula C26H27Cl2N5O2
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Color Light yellow to yellow
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SMILES
O=C1N(C)C2=NC(NC3=CC=C(OCCN(CC)CC)C=C3)=NC=C2C=C1C4=C(Cl)C=CC=C4Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (8)
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Journal Impact Factor
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Most Recent
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Clin Cancer Res
Generation of Genetically Engineered Mouse Lung Organoid Models for Squamous Cell Lung Cancers Allows for the Study of Combinatorial Immunotherapy. [Abstract]2020 Jul 1;26(13):3431-3442. PMID: 32209571 -
Cancer Cell Int
Wee1 inhibitor PD0166285 sensitized TP53 mutant lung squamous cell carcinoma to cisplatin via STAT1. [Abstract]2024 Sep 13;24(1):315. PMID: 39272147 -
FASEB J
Kinesin KIF16B Participates in G2/M Transition and Microtubule Dynamics via Aurora A-PLK1 in Oocyte Meiosis. [Abstract]2025 Jul 31;39(14):e70854. PMID: 40704502 -
Reprod Toxicol
2022 Jun:110:172-179. PMID: 35504548 -
bioRxiv
2024 Dec 11:2024.12.02.626470. PMID: 39677655 -
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Solvent & Solubility
DMSO : 50 mg/mL (97.57 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.88 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Wang Y, et al. Radiosensitization of p53 mutant cells by PD0166285, a novel G(2) checkpoint abrogator. Cancer Res. 2001 Nov 15;61(22):8211-7. [Content Brief]
[2]. Mark C de Gooijer, et al. ATP-binding cassette transporters limit the brain penetration of Wee1 inhibitors. Invest New Drugs. 2018 Jun;36(3):380-387. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9515 mL | 9.7574 mL | 19.5149 mL | 48.7872 mL |
| 5 mM | 0.3903 mL | 1.9515 mL | 3.9030 mL | 9.7574 mL | |
| 10 mM | 0.1951 mL | 0.9757 mL | 1.9515 mL | 4.8787 mL | |
| 15 mM | 0.1301 mL | 0.6505 mL | 1.3010 mL | 3.2525 mL | |
| 20 mM | 0.0976 mL | 0.4879 mL | 0.9757 mL | 2.4394 mL | |
| 25 mM | 0.0781 mL | 0.3903 mL | 0.7806 mL | 1.9515 mL | |
| 30 mM | 0.0650 mL | 0.3252 mL | 0.6505 mL | 1.6262 mL | |
| 40 mM | 0.0488 mL | 0.2439 mL | 0.4879 mL | 1.2197 mL | |
| 50 mM | 0.0390 mL | 0.1951 mL | 0.3903 mL | 0.9757 mL | |
| 60 mM | 0.0325 mL | 0.1626 mL | 0.3252 mL | 0.8131 mL | |
| 80 mM | 0.0244 mL | 0.1220 mL | 0.2439 mL | 0.6098 mL |
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