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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 212391-63-4
- Formel: C26H29Cl4N5O2
- Molecular Weight:585.35
-
Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biologische Aktivität
-
Chemical Information
- Reinheit & Dokumentation
- Verweise
-
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.
Biologische Aktivität
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.
-
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.
-
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.
Chemical Information
-
CAS. Nr. 212391-63-4
-
Molecular Weight 585.35
-
Formel C26H29Cl4N5O2
-
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
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (9)
-
Journal Impact Factor
-
Most Recent
-
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 -
-
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 -
-
Reinheit & Dokumentation
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]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
PD0166285 dihydrochloride Related Classifications
HY-13925A Related Classifications
Powered by Bioz