MedChemExpress - Model PD173955 -260415-63-2

PD173955 is an orally active inhibitor of Src (IC50= 22 nM), Yes, Abl, ATP and MAP kinases. PD173955 can effectively prevent the mitotic process and has anticancer activity[1][2][3][4].

PD173955

MCE China：PD173955

Brand：MedChemExpress (MCE)

Cat. No.HY-10395

CAS：260415-63-2

Purity：99.12%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping：Room temperature in continental US; may vary elsewhere.

Description：PD173955 is an orally active inhibitor of Src (IC50= 22 nM), Yes, Abl, ATP and MAP kinases. PD173955 can effectively prevent the mitotic process and has anticancer activity.

In Vitro：PD173955 inhibits cell growth in MDA-MB-468 and MCF-7 breast cancer cells with IC50 values of 500 nM and 1 μM, respectively[1]. PD173955 (100 nM; 10 min) significantly inhibits the activity of src and yes kinases in MDA-MB-468 breast cancer cells[1]. PD173955 (5 μM; 24 h) can block the cells in the G2-M phase and has anti-mitotic activity in MDA-MB-468 breast cancer cells[1]. PD166326 (0.1-1000 nM; 42 h) can inhibit cell proliferation in R10(-) cells with IC50 0.2 nM, and can inhibit stem cell factor (SCF) -dependent proliferation in parental MO7e cells with IC50 12 nM[4].

In Vivo：PD166326 (50 mg/kg; Oral gavage; Twice daily) has anti-leukemia activity in CML mice[4].

IC50 & Target：IC50: 22 nM (Src)[1]. Cellular Effect Cell Line Type Value Description References

References：

[1]. Moasser MM, et al. Inhibition of Src kinases by a selective tyrosine kinase inhibitor causes mitotic arrest. Cancer Res. 1999 Dec 15;59(24):6145-52. PMID: 10626805. [Content Brief]

[2]. Martinelli G, et al. Dual tyrosine kinase inhibitors in chronic myeloid leukemia. Leukemia. 2005 Nov;19(11):1872-9. [Content Brief]

[3]. Netzer WJ, et al. Gleevec shifts APP processing from a β-cleavage to a nonamyloidogenic cleavage. Proc Natl Acad Sci U S A. 2017 Feb 7;114(6):1389-1394. [Content Brief]

[4]. Wolff NC, et al. PD166326, a novel tyrosine kinase inhibitor, has greater antileukemic activity than imatinib mesylate in a murine model of chronic myeloid leukemia. Blood. 2005 May 15;105(10):3995-4003. [Content Brief]

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MedChemExpress - Model PD173955 -260415-63-2

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PD173955