PD166326
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MedKoo CAT#: 406173

CAS#: 185039-91-2

Description: PD166326 is one of the most potent members of the pyridopyrimidine class of protein tyrosine kinase inhibitors. In mice with the CML-like disease, PD166326 rapidly inhibited Bcr/Abl kinase activity after a single oral dose and demonstrated marked antileukemic activity in vivo. In vivo, PD166326 was also superior to imatinib mesylate in inhibiting the constitutive tyrosine phosphorylation of numerous leukemia-cell proteins, including the src family member Lyn. PD166326 also prolonged the survival of mice with imatinib mesylate-resistant CML induced by the Bcr/Abl mutants P210/H396P and P210/M351T.


Chemical Structure

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PD166326
CAS# 185039-91-2

Theoretical Analysis

MedKoo Cat#: 406173
Name: PD166326
CAS#: 185039-91-2
Chemical Formula: C21H16Cl2N4O2
Exact Mass: 426.06503
Molecular Weight: 427.28334
Elemental Analysis: C, 59.03; H, 3.77; Cl, 16.59; N, 13.11; O, 7.49

Price and Availability

Size Price Availability Quantity
5.0mg USD 230.0 2 Weeks
25.0mg USD 570.0 2 Weeks
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Synonym: PD166326; PD166326; PD 166326.

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

InChi Key: ZIQFYVPVJZEOFS-UHFFFAOYSA-N

InChi Code: InChI=1S/C21H16Cl2N4O2/c1-27-19-13(9-15(20(27)29)18-16(22)6-3-7-17(18)23)10-24-21(26-19)25-14-5-2-4-12(8-14)11-28/h2-10,28H,11H2,1H3,(H,24,25,26)

SMILES Code: O=C1C(C2=C(Cl)C=CC=C2Cl)=CC3=CN=C(NC4=CC=CC(CO)=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

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 427.28334 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: Grosso S, Puissant A, Dufies M, Colosetti P, Jacquel A, Lebrigand K, Barbry P, Deckert M, Cassuto JP, Mari B, Auberger P. Gene expression profiling of imatinib and PD166326-resistant CML cell lines identifies Fyn as a gene associated with resistance to BCR-ABL inhibitors. Mol Cancer Ther. 2009 Jul;8(7):1924-33. doi: 10.1158/1535-7163.MCT-09-0168. Epub 2009 Jun 30. PubMed PMID: 19567819.

2: Wolff NC, Veach DR, Tong WP, Bornmann WG, Clarkson B, Ilaria RL Jr. PD166326, a novel tyrosine kinase inhibitor, has greater antileukemic activity than imatinib mesylate in a murine model of chronic myeloid leukemia. Blood. 2005 May 15;105(10):3995-4003. Epub 2005 Jan 18. PubMed PMID: 15657179; PubMed Central PMCID: PMC1895078.

3: von Bubnoff N, Veach DR, van der Kuip H, Aulitzky WE, Sänger J, Seipel P, Bornmann WG, Peschel C, Clarkson B, Duyster J. A cell-based screen for resistance of Bcr-Abl-positive leukemia identifies the mutation pattern for PD166326, an alternative Abl kinase inhibitor. Blood. 2005 Feb 15;105(4):1652-9. Epub 2004 Sep 30. PubMed PMID: 15459011.



Additional Information