PD0166285 dihydrochloride
Based on 9 publication(s) in Google Scholar
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.
- CAS No.: 212391-63-4
- Formula: C26H29Cl4N5O2
- Molecular Weight:585.35
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) PD0166285 dihydrochloride
More- Acta Pharm Sin B. 2026 May;16(5):2947-2963. [Abstract]
- 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].
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. 212391-63-4
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Molecular Weight 585.35
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Formula C26H29Cl4N5O2
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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.[H]Cl.[H]Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (9)
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Journal Impact Factor
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Most Recent
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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 -
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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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Purity & Documentation
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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PD0166285 dihydrochloride Related Classifications
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