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PD173955

Catalog No. T3063   CAS 260415-63-2
Synonyms: PD173955, inhibit, Src, Inhibitor, PD 173955, PD-173955, Bcr-Abl, Apoptosis

PD173955 is src family-selective tyrosine kinase inhibitor with IC50 of ~22 nM for Src, Yes and Abl kinase; less potent for FGFRα and no activity on InsR and PKC.

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PD173955, CAS 260415-63-2
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Purity: 98%
Biological Description
Chemical Properties
Storage & Solubility Information
Description PD173955 is src family-selective tyrosine kinase inhibitor with IC50 of ~22 nM for Src, Yes and Abl kinase; less potent for FGFRα and no activity on InsR and PKC.
Targets&IC50 Src:22 nM
Kinase Assay In Vitro Bcr-Abl Kinase Assays: Bcr-Abl complexed to SHIP2 is immunoprecipitated from cell lysates of K562 cells maintained in log-phase culture conditions. Complexes are collected on protein A-Sepharose, and complexes are washed three times in lysis buffer and then washed twice in abl kinase buffer [50 mM Tris (pH 8.0), 10 mM MgCl2, 1 mM DTT, 2 mM p-nitrophenylphosphate, and 2 μM ATP; New England Biolabs Buffer and protocol]. Kinase assays are performed with 10 μM [γ-32P]ATP/sample for 15–60 min at 30°C in the presence or absence of the indicated concentrations of drug. The reaction is stopped by the addition of SDS-PAGE sample buffer and heated at 100°C for 10 min. Proteins are separated on 7.5% SDS-polyacrylamide gels, gels are dried under vacuum, and phosphorylation is visualized by autoradiography on X-ray film.
Cell Research Cell growth is determined by two methods. For the [3H]thymidine assay, cells (104 cells/well) are cultured in 96-well, round-bottomed plates with diluted DMSO (control) or with varying concentrations of a specific compound that is resuspended in DMSO for 48 h at 37°C. [3H]Thymidine is added at a concentration of 1 μCi/well, and cells are incubated for an additional 18 h. Cells were harvested with the Unifilter system, scintillation fluid (25 μl/well) is added to each well, and [3H]thymidine incorporation is determined on a Packard Scintillation Counter. Data points for all assays are obtained in triplicate, and background incorporation from cell-free wells is determined and subtracted from all data points. For cell viability, control and drug-treated harvested cells are counted on a hemocytometer using the trypan blue dye exclusion method.(Only for Reference)
Synonyms PD173955, inhibit, Src, Inhibitor, PD 173955, PD-173955, Bcr-Abl, Apoptosis
Molecular Weight 443.35
Formula C21H16Cl2N4OS
CAS No. 260415-63-2

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

Ethanol: <1 mg/mL

DMSO: 12 mg/mL (27.1 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
1. Wisniewski D, et al. Cancer Res. 2002, 62(15), 4244-4255. 2. Moasser MM, et al. Cancer Res. 1999, 59(24), 6145-6152.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Compound Library Preclinical Compound Library HIF-1 Signaling Pathway Compound Library TGF-beta/Smad Compound Library Inhibitor Library Anti-Cancer Active Compound Library Anti-Breast Cancer Compound Library Kinase Inhibitor Library Cytoskeletal Signaling Pathway Compound Library Apoptosis Compound Library

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