PD0166285
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MedKoo CAT#: 406345

CAS#: 185039-89-8

Description: PD0166285 is a potent Wee1 inhibitor and Chk1 inhibitor with activity at nanomolar concentrations. This G2 checkpoint abrogation by PD0166285 was demonstrated to kill cancer cells, there at a toxic highest dose of 0.5 muM in some cell lines for exposure periods of no longer than 6 hours. The deregulated cell cycle progression may have ultimately damaged the cancer cells. We herein report one of the mechanism by which PD0166285 leads to cell death in the B16 mouse melanoma cell line.


Chemical Structure

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PD0166285
CAS# 185039-89-8

Theoretical Analysis

MedKoo Cat#: 406345
Name: PD0166285
CAS#: 185039-89-8
Chemical Formula: C26H27Cl2N5O2
Exact Mass: 511.15418
Molecular Weight: 512.43
Elemental Analysis: C, 60.94; H, 5.31; Cl, 13.84; N, 13.67; O, 6.24

Price and Availability

Size Price Availability Quantity
5.0mg USD 110.0 Same day
10.0mg USD 190.0 Same day
25.0mg USD 350.0 Same day
50.0mg USD 550.0 Same day
100.0mg USD 850.0 Same day
200.0mg USD 1450.0 Same day
500.0mg USD 2250.0 Same day
1.0g USD 3250.0 Same day
2.0g USD 5950.0 2 Weeks
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Synonym: PD0166285; PD 0166285; PD0166285; PD166285; PD 166285; PD166285.

IUPAC/Chemical Name: 6-(2,6-dichlorophenyl)-2-((4-(2-(diethylamino)ethoxy)phenyl)amino)-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one

InChi Key: IFPPYSWJNWHOLQ-UHFFFAOYSA-N

InChi Code: InChI=1S/C26H27Cl2N5O2/c1-4-33(5-2)13-14-35-19-11-9-18(10-12-19)30-26-29-16-17-15-20(25(34)32(3)24(17)31-26)23-21(27)7-6-8-22(23)28/h6-12,15-16H,4-5,13-14H2,1-3H3,(H,29,30,31)

SMILES Code: O=C1C(C2=C(Cl)C=CC=C2Cl)=CC3=CN=C(NC4=CC=C(OCCN(CC)CC)C=C4)N=C3N1C

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 512.43 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Chang JB, Ferrell JE Jr. Mitotic trigger waves and the spatial coordination of the Xenopus cell cycle. Nature. 2013 Aug 29;500(7464):603-7. doi: 10.1038/nature12321. Epub 2013 Jul 17. PubMed PMID: 23863935; PubMed Central PMCID: PMC3758429.

2: PosthumaDeBoer J, Würdinger T, Graat HC, van Beusechem VW, Helder MN, van Royen BJ, Kaspers GJ. WEE1 inhibition sensitizes osteosarcoma to radiotherapy. BMC Cancer. 2011 Apr 29;11:156. doi: 10.1186/1471-2407-11-156. PubMed PMID: 21529352; PubMed Central PMCID: PMC3103478.

3: Mir SE, De Witt Hamer PC, Krawczyk PM, Balaj L, Claes A, Niers JM, Van Tilborg AA, Zwinderman AH, Geerts D, Kaspers GJ, Peter Vandertop W, Cloos J, Tannous BA, Wesseling P, Aten JA, Noske DP, Van Noorden CJ, Würdinger T. In silico analysis of kinase expression identifies WEE1 as a gatekeeper against mitotic catastrophe in glioblastoma. Cancer Cell. 2010 Sep 14;18(3):244-57. doi: 10.1016/j.ccr.2010.08.011. PubMed PMID: 20832752; PubMed Central PMCID: PMC3115571.

4: Hashimoto O, Shinkawa M, Torimura T, Nakamura T, Selvendiran K, Sakamoto M, Koga H, Ueno T, Sata M. Cell cycle regulation by the Wee1 inhibitor PD0166285, pyrido [2,3-d] pyimidine, in the B16 mouse melanoma cell line. BMC Cancer. 2006 Dec 19;6:292. PubMed PMID: 17177986; PubMed Central PMCID: PMC1770931.

5: Kawabe T. G2 checkpoint abrogators as anticancer drugs. Mol Cancer Ther. 2004 Apr;3(4):513-9. Review. PubMed PMID: 15078995.

6: Hashimoto O, Ueno T, Kimura R, Ohtsubo M, Nakamura T, Koga H, Torimura T, Uchida S, Yamashita K, Sata M. Inhibition of proteasome-dependent degradation of Wee1 in G2-arrested Hep3B cells by TGF beta 1. Mol Carcinog. 2003 Apr;36(4):171-82. PubMed PMID: 12669309.

7: Li J, Wang Y, Sun Y, Lawrence TS. Wild-type TP53 inhibits G(2)-phase checkpoint abrogation and radiosensitization induced by PD0166285, a WEE1 kinase inhibitor. Radiat Res. 2002 Mar;157(3):322-30. PubMed PMID: 11839095.

8: Wang Y, Li J, Booher RN, Kraker A, Lawrence T, Leopold WR, Sun Y. Radiosensitization of p53 mutant cells by PD0166285, a novel G(2) checkpoint abrogator. Cancer Res. 2001 Nov 15;61(22):8211-7. PubMed PMID: 11719452.



Additional Information