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PD173955

Catalog No. T3063 CAS 260415-63-2

Synonyms: PD-173955, PD 173955

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

Pack Size	Availability	Price/USD
1 mg	In stock	$ 62.00
2 mg	In stock	$ 88.00
5 mg	In stock	$ 155.00
10 mg	In stock	$ 277.00
25 mg	In stock	$ 469.00
50 mg	In stock	$ 675.00
100 mg	In stock	$ 942.00
1 mL * 10 mM (in DMSO)	In stock	$ 166.00

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Purity: 99.28%

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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
In vivo	PD173955 serves as a Src inhibitor, effectively inhibiting mitotic progression during the early stages of mitosis across various cell types while inducing apoptosis to varying degrees. It efficiently suppresses Bcr-Abl-dependent cellular growth, displaying an IC50 value of 2-35 nM in Bcr-Abl-positive cell lines, which is approximately 100 to 200 times more sensitive than in Bcr-Abl-negative cell lines. Additionally, PD173955 inhibits the stem cell factor-dependent proliferation of M07e cells by blocking the ligand-dependent autophosphorylation of c-kit, with an IC50 of 40 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	PD-173955, PD 173955
Molecular Weight	443.35
Formula	C21H16Cl2N4OS
CAS No.	260415-63-2

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 12 mg/mL (27.1 mM)

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 Active Compound Library Kinase Inhibitor Library Anti-Neurodegenerative Disease Compound Library Tyrosine Kinase Inhibitor Library Inhibitor Library HIF-1 Signaling Pathway Compound Library Anti-Parkinson's Disease Compound Library Reprogramming Compound Library Angiogenesis related Compound Library Bioactive Compound Library

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Keywords

PD173955 260415-63-2 Angiogenesis Apoptosis Cytoskeletal Signaling Tyrosine Kinase/Adaptors Src Bcr-Abl inhibit Inhibitor PD-173955 PD 173955 inhibitor

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