PD-173955

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PD173955 是 src 家族选择性酪氨酸激酶抑制剂，对 Src、Yes 和 Abl 激酶的 IC50 约为 22 nM；对 FGFRα 的作用较弱，对 InsR 和 PKC 没有活性。

PD-173955 is a src tyrosine kinase inhibitor. PD173955 inhibited Bcr-Abl-dependent cell growth. PD173955 showed cell cycle arrest in G(1). PD173955 has an IC(50) of 1-2 nM in kinase inhibition assays of Bcr-Abl, and in cellular growth assays it inhibits Bcr-Abl-dependent substrate tyrosine phosphorylation. PD173955 inhibited kit ligand-dependent c-kit autophosphorylation (IC(50) = approximately 25 nM) and kit ligand-dependent proliferation of M07e cells (IC(50) = 40 nM) but had a lesser effect on interleukin 3-dependent (IC(50) = 250 nM) or granulocyte macrophage colony-stimulating factor (IC(50) = 1 microM)-dependent cell growth.

Cell Cycle Analysis Cell Line:MDA-MB-468 Concentration:5 μM Incubation Time:24 h Result:Blocked 95% of the cells in the G2-M phase.Cell Proliferation Assay Cell Line:MO7e, R10(-)(a cell line derived from P210-MO7e) Concentration:0.1 nM, 1 nM, 10 nM, 100 nM, 1000 nM Incubation Time:48 h Result:Completely blocked the growth of R10 cells at 2.5 nM.Inhibited stem cell factor (SCF) -dependent proliferation at 5-10 nM and completely inhibited SCF-dependent growth at 50 nM.

Animal Model:Balb/c mice model of chronic myeloid leukemia (CML)Dosage:50 mg/kg Administration:Oral gavage (p.o.), Twice daily for 4 days Result:Significantly inhibited constitutive tyrosine phosphorylation of numerous proteins (including Lyn) in primary Bcr/abl expressing leukemia cells.Reduced the number of mice with splenomegaly and inhibited splenomegaly in at least half of the mice compared to the control group.Was effective in reducing the peripheral blood granulocytosis of the murine CML-like disease.

PD173955 | PD 173955

Others

Antioxidant

Bcr-Abl| Src

Cancer

——

260415-63-2

443.35

C21H16Cl2N4OS

>98% (HPLC)

DMSO : ≥ 32 mg/mL; 72.18 mM

CSc1cccc(Nc2ncc3cc(c(=O)n(C)c3n2)c2c(Cl)cccc2Cl)c1

6-(2,6-dichlorophenyl)-8-methyl-2-((3-(methylthio)phenyl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one

(-20℃)

With Ice Pack

≥ 2 years