PD0166285

Name: PD0166285
Brand: MedChemExpress
SKU: HY-13925
Rating: 5.0 (5 reviews)

Cat. No.: HY-13925 Purity: 99.46%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

PD0166285 Chemical Structure

CAS No. : 185039-89-8

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 186	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 186	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 165	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 264	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 594	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1034	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1815	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of PD0166285:

PD0166285 dihydrochloride Get quote

5 Publications Citing Use of MCE PD0166285

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity
Purity & Documentation
References
Customer Review

Description

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].

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	0.12 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	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]
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]
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	0.35 μM Compound: 63	Inhibition of NIH3T3 proliferation by sulforhodamine B assay Inhibition of NIH3T3 proliferation by sulforhodamine B assay	[PMID: 9703473]

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.

Molecular Weight

512.43

Formula

C₂₆H₂₇Cl₂N₅O₂

CAS No.

185039-89-8

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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

Purity: 99.46%

Select Batch:

Data Sheet (276 KB) SDS (393 KB)

COA (251 KB) HNMR (181 KB) LCMS (356 KB)

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

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

PD0166285 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PD0166285185039-89-8PD 0166285PD-0166285Wee1ApoptosisInhibitorinhibitorinhibit

Your Recently Viewed Products:

Product Name

Salutation

Applicant Name *

Email Address *

Phone Number *

Organization Name *

Department *

Requested quantity *

Country or Region *

Remarks

Product Name

Lot #

Applicant Name *

Email Address *

Phone Number

Department *

Organization Name *

Country or Region *

Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

PD0166285

Customer Review

Other Forms of PD0166285:

PD0166285 Related Antibodies

5 Publications Citing Use of MCE PD0166285

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Purity & Documentation

References

Customer Review

PD0166285 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

PD0166285 Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report