PD173955是Src激酶家族选择性抑制剂,对Src、Yes和Abl激酶IC50值约为22nM,对FGFR_alpha_抑制性弱,对InsR和PKC无活性。 Information PD173955 PD173955 is a potent Bcr-Abl inhibitor with IC50 of 1-2 nM, also inhibiting Src activity with IC50 of 22 nM. Targets Bcr-Abl ; Src 1 nM-2 nM; 22 nM 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. 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. Cell Research(from reference) 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) Concentrations:10 μM Incubation Time:48 hours
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PD173955
CAS number:260415-63-2 molecular formula:C21H16Cl2N4OS
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| Chinese alias | - | ||
| English alias | PD173955 | PD-173955 | AS-17015 | PD-17395 | A19407 | BCP9001059 | 6-(2,6-DICHLORO-PHENYL)-8-METHYL-2-(3-METHYLSULFANYL-PHENYLAMINO)-8H-PYRIDO[2,3-D]PYRIMIDIN-7-ONE | 6-(2,6-Dichlorophenyl)-8-methyl-2-[[3-(methylthio)phenyl]amino]pyrido[2,3-d]pyrimidin-7( | ||
| CAS number | 260415-63-2 | molecular formula | C21H16Cl2N4OS |
| molecular weight | 443.35 g/mol | Exact mass | - |
| PSA | 83.400 Ų | logp | 5.400 |
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