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PD180970

CAS No. : 287204-45-9

MCE 国际站：PD180970

产品活性：PD180970 是一种高效且具有 ATP 竞争性的 p210^Bcr-Abl 激酶抑制剂，可抑制 p210^Bcr-Abl 的自磷酸化，IC₅₀ 为 5 nM。PD180970 还抑制 Src 和 KIT 激酶，IC₅₀ 分别为 0.8 nM 和 50 nM。PD180970 可诱导 K562 白血病细胞凋亡 (apoptosis)，可用于慢性粒细胞白血病的研究。

研究领域：Protein Tyrosine Kinase/RTK  |  Apoptosis

作用靶点：Bcr-Abl  |  Src  |  c-Kit  |  Apoptosis

In Vitro: PD180970 (0.5 μM; 24-96 hours) treatment causes cell death K562 cells.
PD180970 (0.5 μM; 24-48 hours) treatment induces apoptosis of K562 cells. The result shows increase in annexin V-PI double-positive cells.
PD180970 inhibits tyrosine phosphorylation of p210Bcr-Abl, Gab2, and CrkL in K562 cells with IC50 values of 170 nM, 80 nM, and 80 nM, respectively. In vitro, PD180970 potently inhibits autophosphorylation of p210^Bcr-Abl (IC₅₀ of 5 nM) and the kinase activity of purified recombinant Abl tyrosine kinase (IC₅₀ of 2.2 nM).
The blocking Bcr-Abl kinase activity using PD180970 in the human K562 CML cell line resulted in inhibition of Stat5 DNA-binding activity with an IC₅₀ of 5 nM.

In Vivo: PD180970 (5 mg/kg; intraperitonial injection; daily; for 7 days) mitigates MPTP-induced neuronal loss in mice. PD180970 has the neuroprotective ability in a preclinical mouse model of Parkinson's disease (PD).

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