PD 166326 (CAS 185039-91-2) || Cayman Chemical

PD 166326 New

Cayman Chemical Item Number 9000988

(CAS 185039-91-2)

PD 166326 (CAS 185039-91-2)

Description

PD 166326 is a pyridopyrimidine-type inhibitor of receptor tyrosine kinases that inhibits c-abl (IC₅₀ = 8 nM) and Bcr/Abl-dependent cell growth (IC₅₀ = 0.4 nM).^1,2 In addition to targeting a select group of receptor tyrosine kinases, PD 166326 also potently inhibits c-src (IC₅₀ = 6 nM).² Orally administered PD 166326 is well tolerated and effectively blocks Bcr/Abl kinase activity in vivo.³ Moreover, PD 166326 affects a distinct set of kinases from those targeted by imatinib mesylate (STI571) and can reduce the growth of some imatinib-resistant cells both in vitro and in vivo in animal models of chronic myelogenous leukemia.^2,4,3

1 Wisniewski, D., Lambek, C.L., Liu, C., et al. Characterization of potent inhibitors of the Bcr-Abl and the c-kit receptor tyrosine kinases. Cancer Res 62(15) 4244-4255 (2002).

2 Huron, D.R., Gorre, M.E., Kraker, A.J., et al. A novel pyridopyrimidine inhibitor of abl kinase is a picomolar inhibitor of Bcr-abl-driven K562 cells and is effective against STI571-resistant Bcr-abl mutants. Clin Cancer Res 9(4) 1267-1273 (2003).

3 Wolff, N.C., Veach, D.R., Tong, W.P., et al. PD166326, a novel tyrosine kinase inhibitor, has greater antileukemic activity than imatinib mesylate in a murine model of chronic myeloid leukemia. Blood 105(10) 3995-4003 (2005).

4 Azam, M., Nardi, V., Shakespeare, W.C., et al. Activity of dual SRC-ABL inhibitors highlights the role of BCR/ABL kinase dynamics in drug resistance. Proc Natl Acad Sci USA 103(24) 9244-9249 (2006).

Formal Name

6-(2,6-dichlorophenyl)-2-[[3-(hydroxymethyl)phenyl]amino]-8-methyl-pyrido[2,3-d]pyrimidin-7(8H)-one

CAS Number

185039-91-2

Molecular Formula

C₂₁H₁₆Cl₂N₄O₂

Formula Weight

427.3

Formulation

A crystalline solid

Purity

≥98%

λ_max

212, 259, 307, 362 nm

Stability

1 year

Storage

-20°C

Shipping

Room temperature in continental US; may vary elsewhere

SMILES

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OCC1=CC=CC(NC2=NC(N(C)C(C(C3=C(Cl)C=CC=C3Cl)=C4)=O)=C4C=N2)=C1

Size

Global Purchasing

1 mg 
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5 mg 
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10 mg 
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