中文名称: | PD180970 | ||||
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英文名称: | PD180970 | ||||
别名: | PD180970 6-(2,6-Dichlorophenyl)-2-[(4-fluoro-3-methylphenyl)amino]-8-methyl-pyrido[2,3-d]pyrimidin-7(8H)-one | ||||
CAS No: | 287204-45-9 | 分子式: | C21H15Cl2FN4O | 分子量: | 429.27 |
CAS No: | 287204-45-9 | ||||
分子式: | C21H15Cl2FN4O | ||||
分子量: | 429.27 |
基本信息
产品编号:P60048 |
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产品名称:PD180970 |
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CAS: |
287204-45-9 |
储存条件 |
粉末 |
-20℃ |
四年 |
分子式: |
溶于液体 |
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分子量 |
429.27 |
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化学名: |
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Solubility (25°C) |
体外 |
DMSO |
92mg/mL (200.04mM) |
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Ethanol |
Insoluble |
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Water |
Insoluble |
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体内(现配现用) |
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<1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 |
生物活性
产品描述 |
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 5nM。PD180970 还抑制 Src 和 KIT 激酶,IC50 分别为 0.8nM 和 50nM。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。 |
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靶点/IC50 |
Bcr-Abl 5nM (IC50, p210Bcr-Abl kinase) |
Src 0.8nM (IC50) |
KIT 50nM (IC50) |
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体外研究 |
PD180970 (0.5μM; 24-96 hours) treatment causes cell death K562 cells. PD180970 (0.5μM; 24-48 hours) treatment induces apoptosis of K562 cells. The result shows increase in annexin V-PI doublepositive cells. PD180970 inhibits tyrosine phosphorylation of p210Bcr-Abl, Gab2, and CrkL in K562 cells with IC50 values of 170nM, 80nM, and 80nM, respectively. In vitro, PD180970 potently inhibits autophosphorylation of p210Bcr-Abl (IC50 of 5nM) and the kinase activity of purified recombinant Abl tyrosine kinase (IC50 of 2.2nM). The blocking Bcr-Abl kinase activity using PD180970 in the human K562 CML cell line resulted in inhibition of Stat5 DNAbinding activity with an IC50 of 5nM. |
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Cell Line: |
K562 cells |
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Concentration: |
0.5μM |
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Incubation Time: |
24 hours, 48 hours, 72 hours, 96 hours |
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Result: |
Resulted in cell death. |
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Apoptosis Analysis |
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Cell Line: |
K562 cells |
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Concentration: |
0.5μM |
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Incubation Time: |
24 hours, 48 hours |
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Result: |
Increased annexin V-positive/PI-negative cells. |
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体内研究 |
PD180970 (5mg/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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Animal Model: |
Male C57BL/6J mice (3-4 months old) injected with MPTP |
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Dosage: |
5mg/kg |
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Administration: |
Intraperitonial injection; daily; for 7 days |
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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. |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )