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

PD0166285 dihydrochloride 

Cat. No.: HY-13925A
Handling Instructions

PD0166285 dihydrochloride, a substrate of P-gp, is a WEE1 inhibitor and a weak Myt1 inhibitor with IC50 values of 24 and 72 nM, respectively. PD0166285 dihydrochloride exhibits an IC50 of 3.433 μM for Chk1.

For research use only. We do not sell to patients.

PD0166285 dihydrochloride Chemical Structure

PD0166285 dihydrochloride Chemical Structure

CAS No. : 212391-63-4

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Description

PD0166285 dihydrochloride, a substrate of P-gp, is a WEE1 inhibitor and a weak Myt1 inhibitor with IC50 values of 24 and 72 nM, respectively. PD0166285 dihydrochloride 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

585.35

Formula

C₂₆H₂₉Cl₄N₅O₂

CAS No.

212391-63-4

SMILES

O=C1N(C)C2=NC(NC3=CC=C(OCCN(CC)CC)C=C3)=NC=C2C=C1C4=C(Cl)C=CC=C4Cl.[H]Cl.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

PD0166285PD 0166285PD-0166285Wee1ApoptosisInhibitorinhibitorinhibit

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PD0166285 dihydrochloride
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HY-13925A
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