CAS NO: | 260415-63-2 |
规格: | ≥98% |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
250mg | 电议 |
500mg | 电议 |
Molecular Weight (MW) | 443.35 |
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Formula | C21H16Cl2N4OS |
CAS No. | 260415-63-2 |
Storage | -20℃ for 3 years in powder form |
-80℃ for 2 years in solvent | |
Solubility (In vitro) | DMSO: 15 mg/mL (33.8 mM) |
Water:<1 mg/mL | |
Ethanol:<1 mg/mL | |
Other info | Chemical Name: 6-(2,6-dichlorophenyl)-8-methyl-2-((3-(methylthio)phenyl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one InChi Key: VAARYSWULJUGST-UHFFFAOYSA-N InChi Code: InChI=1S/C21H16Cl2N4OS/c1-27-19-12(9-15(20(27)28)18-16(22)7-4-8-17(18)23)11-24-21(26-19)25-13-5-3-6-14(10-13)29-2/h3-11H,1-2H3,(H,24,25,26) SMILES Code: O=C1C(C2=C(Cl)C=CC=C2Cl)=CC3=CN=C(NC4=CC=CC(SC)=C4)N=C3N1C |
Synonyms | PD 173955; PD173955; PD-173955 |
In Vitro | In vitro activity: 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. 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. Kinase Assay: 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 Assay: Cell growth is determined by two methods. For the [3H]thymidine assay, cells (104 cells/well, 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)) 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. |
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In Vivo | |
Animal model | |
Formulation & Dosage | |
References | Cancer Res. 2002 Aug 1;62(15):4244-55; Cancer Res. 1999 Dec 15;59(24):6145-52. |
PD173955 inhibits Bcr-Abl-dependent substrate tyrosine phosphorylation in vivo. Cancer Res. 2002 Aug 1;62(15):4244-55. | PD173955 induces strong accumulation in G1 phase of the cell cycle. Cancer Res. 2002 Aug 1;62(15):4244-55. | PD173955 and PD166326 selectively inhibit the growth of primary CD34+ CML primitive progenitor cells from a patient with chronic phase CML. Cancer Res. 2002 Aug 1;62(15):4244-55. |