PD0166285 dihydrochloride

Cat. No.: HY-13925A: FAQs
Data Sheet Handling Instructions

Molarity Calculator

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

CAS No. : 212391-63-4

Size		Stock
MOQ		Minimum order quantity
50 mg		Get quote
100 mg		Get quote
250 mg		Get quote
Other size		Get quote

Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

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

Other In-stock Forms of PD0166285 dihydrochloride:

PD0166285

Other Forms of PD0166285 dihydrochloride:

PD0166285 In-stock

5 Publications Citing Use of MCE PD0166285 dihydrochloride

Featured Recommendations

•Related Small Molecules:

•Related Proteins:

Biological Activity
Purity & Documentation
References
Customer Review

Description

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].

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

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.

Purity & Documentation

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]