Antibodies
PD173955
- 貨號 Cat. No.
- S7269
- 規格 Size
- 5~200mg
- 品牌 Brand
- Selleckchem
Description
PD173955
Catalog No.S7269
PD173955 is a potent Bcr-Abl inhibitor with IC50 of 1-2 nM, also inhibiting Src activity with IC50 of 22 nM.
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Biological Activity
| Description | PD173955 is a potent Bcr-Abl inhibitor with IC50 of 1-2 nM, also inhibiting Src activity with IC50 of 22 nM. | |||||
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| Targets | Bcr-Abl | Src | ||||
| IC50 | 1-2 nM [1] | 22 nM [2] | ||||
| In vitro | PD173955 potently inhibits Bcr-Abl-dependent cell growth with IC50 of 2-35 nM in Bcr-Abl-positive cell lines, about 100- to 200-fold more sensitive than in Bcr-Abl-negative cell lines. PD173955 also inhibits kit ligand-dependent proliferation of M07e cells with IC50 of 40 nM, by inhibition of kit ligand-dependent c-kit autophosphorylation. [1] In addition, PD173955, as a Src inhibitor, potently inhibits mitotic progression during early mitosis in cells of all types and induces varying degrees of apoptotic cell death. [2] | |||||
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| Features | ||||||
Protocol(Only for Reference)
Kinase Assay: [1]
| 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. |
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Cell Assay: [1]
| Cell lines | Bcr-Abl-positive cell lines (R10(+), R10(−), K562, and RWLeu4); Bcr-Abl-negative cell lines (HL-60, SK-N-ER, SK-N-MC, U138MG, and HS-16) |
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| Concentrations | 10 μM |
| Incubation Time | 48 hours |
| Method | 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. |
References
Chemical Information
| Molecular Weight (MW) | 443.35 |
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| Formula | C21H16Cl2N4OS |
| CAS No. | 260415-63-2 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | mg/mL (<1 mM) |
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| Water | mg/mL (<1 mM) | ||
| Ethanol | mg/mL (<1 mM) | ||
| * <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. | |||
| Chemical Name | 6-(2,6-dichlorophenyl)-8-methyl-2-((3-(methylthio)phenyl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one |
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