PD180970

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

PD180970 是一种高效且具有 ATP 竞争性的 p210Bcr-Abl 激酶抑制剂，可抑制 p210Bcr-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。

PD180970 is a highly potent and ATP-competitive p210Bcr-Abl kinase inhibitor, with an IC50 of 5 nM for inhibiting the autophosphorylation of p210Bcr-Abl. PD180970 also inhibits Src and KIT kinase with IC50s of 0.8 nM and 50 nM, respectively. PD180970 indcues apoptosis of K562 leukemic cells, and can be used for chronic myelogenous leukemia research.

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 p210Bcr-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.Cell Viability Assay Cell Line:K562 cells Concentration:0.5 μM Incubation Time:24 hours, 48 hours, 72 hours, 96 hours Result:Resulted in cell death.Apoptosis Analysis Cell Line:K562 cells Concentration:0.5 μM Incubation Time:24 hours, 48 hours Result:Increased annexin V-positive/PI-negative cells.

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).Animal Model:Male C57BL/6J mice (3-4 months old) injected with MPTP Dosage:5?mg/kg Administration:Intraperitonial injection; daily; for 7 days Result:Decreased number of activated microglia on activation by MPTP in mice brains. And showed significant reduction in intensity of Iba1 expression in activated microglia.

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Angiogenesis

Bcr-Abl

Bcr-Abl | Src | c-Kit

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287204-45-9

429.27

C21H15Cl2FN4O

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (232.95 mM; 超声助溶 )

Cc1cc(Nc2ncc3cc(-c4c(Cl)cccc4Cl)c(=O)n(C)c3n2)ccc1F

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(-20℃)

With Ice Pack

≥ 2 years