Art. -Nr.: HY-13925

PD0166285

Name: PD0166285
Brand: MedChemExpress
SKU: HY-13925
Price: 165.00 USD
Availability: InStock
Rating: 5 (9 reviews)

9 Cited Publications

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Based on 9 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.

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Reinheit: 99.46%
CAS. Nr.: 185039-89-8
Formel: C₂₆H₂₇Cl₂N₅O₂
Molecular Weight:512.43

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

PD0166285 Chemical Structure

CAS. Nr.: 185039-89-8

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (9)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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^[1].

IC₅₀ & Target

IC50: 24 nM (WEE1), 72 nM (Myt1), 3.433 μM (Chk1)^[1].

Alle Wee1 Isoform-spezifische Produkte anzeigen :

PKMYT1

Cellular Effect

Cell Line	Type	Value	Description	References
C6	IC₅₀	0.005 μM Compound: 2a	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	[PMID: 9784112]
C6	IC₅₀	0.005 μM Compound: 63	Inhibition of PDGF-induced autophosphorylation of PDGF-R in C6 cells Inhibition of PDGF-induced autophosphorylation of PDGF-R in C6 cells	[PMID: 9703473]
C6	IC₅₀	0.12 μM Compound: 2a	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	[PMID: 9784112]
C6	IC₅₀	0.12 μM Compound: 63	C6 cell growth in soft agar with continuous treatment C6 cell growth in soft agar with continuous treatment	[PMID: 9703473]
C6	IC₅₀	0.34 μM Compound: 2a	Inhibition of rat C6 glioma cell proliferation in sulforhodamine B assay Inhibition of rat C6 glioma cell proliferation in sulforhodamine B assay	[PMID: 9784112]
C6	IC₅₀	0.34 μM Compound: 63	Inhibition of C6 cell proliferation in sulforhodamine B assay Inhibition of C6 cell proliferation in sulforhodamine B assay	[PMID: 9703473]
C6	IC₅₀	1.8 μM Compound: 2a	C6 glioma 3-day proliferation followed by soft agar growth without treatment C6 glioma 3-day proliferation followed by soft agar growth without treatment	[PMID: 9784112]
C6	IC₅₀	1.8 μM Compound: 63	C6 cell growth in soft agar with discontinued treatment C6 cell growth in soft agar with discontinued treatment	[PMID: 9703473]
HCT-8	IC₅₀	0.42 μM Compound: 6q	Inhibitory activity against HCT-8 human colon adenocarcinoma cells was determined. Inhibitory activity against HCT-8 human colon adenocarcinoma cells was determined.	[PMID: 10956222]
HEK293	IC₅₀	7.2 nM Compound: PD0166285	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	[PMID: 22770610]
HEK-293T	IC₅₀	0.29 μM Compound: 3; PD-166285	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	[PMID: 28792760]
HT-29	IC₅₀	0.28 μM Compound: 6q	Inhibitory activity against HT-29 human colon adenocarcinoma cells was determined. Inhibitory activity against HT-29 human colon adenocarcinoma cells was determined.	[PMID: 10956222]
MDA-MB-231	IC₅₀	0.16 μM Compound: 3; PD-166285	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	[PMID: 28792760]
MM1.S	IC₅₀	0.52 μM Compound: 3; PD-166285	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	[PMID: 28792760]
NIH3T3	IC₅₀	0.0011 μM Compound: 63	Growth of NIH3T3 cell colonies in soft agar with continuous treatment Growth of NIH3T3 cell colonies in soft agar with continuous treatment	[PMID: 9703473]
NIH3T3	IC₅₀	0.0018 μM Compound: 63	Inhibition of PDGF-induced autophosphorylation of PDGF-R in NIH3T3 cells Inhibition of PDGF-induced autophosphorylation of PDGF-R in NIH3T3 cells	[PMID: 9703473]
NIH3T3	IC₅₀	0.01 μM Compound: 63	Growth of NIH3T3 cell colonies in soft agar with discontinued treatment Growth of NIH3T3 cell colonies in soft agar with discontinued treatment	[PMID: 9703473]
NIH3T3	IC₅₀	0.35 μM Compound: 63	Inhibition of NIH3T3 proliferation by sulforhodamine B assay Inhibition of NIH3T3 proliferation by sulforhodamine B assay	[PMID: 9703473]
SW-620	IC₅₀	0.27 μM Compound: 6q	Inhibitory activity against SW-620 human colon adenocarcinoma cells was determined. Inhibitory activity against SW-620 human colon adenocarcinoma cells was determined.	[PMID: 10956222]

In Vitro

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.

Western Blot Analysis^[1]

Cell Line:

Human and mouse cancer cell lines (HCT116, HT29, DLD-1, HCT8, H460, HeLa, C 26).
Concentration:

0.5 μM.
Incubation Time:

4 h.
Result:

Inhibited Cdc2Y15 and CdcT14 phosphorylation.

In Vivo

Animal Model:

Wild-type, Abcg2^-/-, Abcb1a/b^-/- and Abcb1a/b;Abcg2^-/- FVB mice^[2].
Dosage:

5 mg/kg.
Administration:

IV.
Result:

C_max is about 400 ng/mL.
P-gp, but not BCRP, limited the brain penetration of PD0166285.

Chemical Information

CAS. Nr. 185039-89-8
Appearance Solid
Molecular Weight 512.43
Formel C₂₆H₂₇Cl₂N₅O₂
Color Light yellow to yellow
SMILES

O=C1N(C)C2=NC(NC3=CC=C(OCCN(CC)CC)C=C3)=NC=C2C=C1C4=C(Cl)C=CC=C4Cl
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (9)

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Journal Impact Factor

Acta Pharm Sin B

DeepICER: A deep learning framework for predicting compound-induced gene expression profiles. [Abstract]

2026 May;16(5):2947-2963. PMID: 42180546
Acta Pharm Sin B

2026 Feb.
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

High-dose zearalenone exposure disturbs G2/M transition during mouse oocyte maturation. [Abstract]

2022 Jun:110:172-179. PMID: 35504548
bioRxiv

Origin of Chromosome 12 Trisomy Surge in Human Induced Pluripotent Stem Cells (iPSCs). [Abstract]

2024 Dec 11:2024.12.02.626470. PMID: 39677655
Patent

US20240174977A1.
bioRxiv

2020 Jun.

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9515 mL

9.7574 mL

19.5149 mL

5 mM

0.3903 mL

1.9515 mL

3.9030 mL

10 mM

0.1951 mL

0.9757 mL

1.9515 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: 2.17 mg/mL (4.23 mM); Clear solution; Need warming

This protocol yields a clear solution of 2.17 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
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)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Bioz

Keywords

PD0166285

9 Cited Publications

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PD0166285

Adavosertib

lunresertib

BML-277

Azenosertib

CCT244747

SCH900776

CCT245737

BI 2536

Volasertib

Zedoresertib

(+)-JQ-1

Pomalidomide-C3-adavosertib

Publications Citing Use of MedChemExpress (MCE) PD0166285

Alle Wee1 Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (9)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Bioz

PD0166285

Adavosertib

lunresertib

BML-277

Azenosertib

CCT244747

SCH900776

CCT245737

BI 2536

Volasertib

Zedoresertib

(+)-JQ-1

Pomalidomide-C3-adavosertib

Publications Citing Use of MedChemExpress (MCE) PD0166285

Alle Wee1 Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (9)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PD0166285 Related Classifications

HY-13925 Related Classifications

Bioz