1. Cell Cycle/DNA Damage
    Apoptosis
  2. Wee1
    Apoptosis
  3. PD0166285

PD0166285 

Cat. No.: HY-13925 Purity: 99.46%
Handling Instructions

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

PD0166285 Chemical Structure

CAS No. : 185039-89-8

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 169 In-stock
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5 mg USD 150 In-stock
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10 mg USD 240 In-stock
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25 mg USD 540 In-stock
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50 mg USD 940 In-stock
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100 mg USD 1650 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of PD0166285:

Top Publications Citing Use of Products
  • 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].

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].

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: Cmax 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

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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 65 mg/mL (126.85 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References

Purity: 99.46%

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Keywords:

PD0166285PD 0166285PD-0166285Wee1ApoptosisInhibitorinhibitorinhibit

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PD0166285
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HY-13925
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