中文名称: | TAE226 | ||||
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英文名称: | TAE226 | ||||
别名: | TAE226 NVP-TAE226;TAE 226;NVPTAE226;2-((5-chloro-2-((2-methoxy-4-morpholinophenyl)amino)pyrimidin-4-yl)amino)-N-methylbenzamide | ||||
CAS No: | 761437-28-9 | 分子式: | C23H25ClN6O3 | 分子量: | 468.94 |
CAS No: | 761437-28-9 | ||||
分子式: | C23H25ClN6O3 | ||||
分子量: | 468.94 |
基本信息
产品编号:T10304 |
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产品名称:TAE226 |
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CAS: |
761437-28-9 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式: |
溶于液体 |
-80℃ |
六个月 |
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分子量 |
468.94 |
-20℃ |
一个月 |
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化学名: |
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Solubility (25°C) |
体外 |
DMSO |
94mg/mL (200.45mM) |
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Ethanol |
Insoluble |
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Water |
Insoluble |
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体内(现配现用) |
0.5% methylcellulose |
30mg/mL |
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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。 |
制备储备液
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
1mM |
2.1325mL |
10.6623mL |
21.3247mL |
5mM |
0.4265mL |
2.1325mL |
4.2649mL |
10mM |
0.2132mL |
1.0662mL |
2.1325mL |
50mM |
0.0426mL |
0.2132mL |
0.4265mL |
生物活性
产品描述 |
一种有效的具有ATP竞争性的FAK和IGF-1R双重抑制剂,IC50分别为5.5nM、140nM。 |
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靶点/IC50 |
PYK2 |
FAK |
Insulin Receptor |
IGF-1R |
c-Met |
3.5nM |
5.5nM |
43.5nM |
140nM |
160nM |
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体外研究 |
NVP-TAE 226 (TAE226), a potent ATP-competitive inhibitor of several tyrosine protein kinases, in particular FAK and IGF-IR kinases. In a cell-based kinase assays, FAK, IGF-IR kinase, and IR kinase are inhibited with an IC50 range of 100 to 300nM compared with the other kinases tested, which are >10-fold less sensitive. In culture, NVP-TAE 226 inhibits extracellular matrix-induced autophosphorylation of FAK (Tyr395). NVP-TAE 226 also inhibits IGF-I-induced phosphorylation of IGF-IR and activity of its downstream target genes such as MAPK and Akt. NVP-TAE 226 retards tumor cell growth as assessed by a cell viability assay and attenuates G2-M cell cycle progression associated with a decrease in cyclin B1 and phosphorylated cdc2 (Tyr15) protein expression. NVP TAE 226 treatment inhibits tumor cell invasion by at least 50% compared with the control in an in vitro Matrigel invasion assay. Interestingly, TAE226 treatment of tumor cells containing wild-type p53 mainly exhibits G2-M arrest, whereas tumor cells bearing mutant p53 underwent apoptosis. |
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体内研究 |
Treatment with NVP-TAE 226 (TAE226) at 50 or 75mg/kg extends the median survival of U87 xenograft animals by 6 and 7 days, respectively (P=0.084 and P=0.042,respectively, compared with vehicle-treated animals). However, NVP-TAE 226 treatment of LN229-engrafted animals significantly prolongs their median survival by 19 days (P<0.004 for both dosages,compared with vehicle-treated animals). |
推荐实验方法(仅供参考)
细胞实验: |
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Glioma cell cultures are harvested with 0.05% trypsin and seeded in triplicate at 2×104 in 24-well culture plates for 24h before drug treatment. Culture medium is used for mock treatment. Cells are harvested at the indicated day after treatment, and viable cells are counted using the Vi-cell viability analyzer. The antiproliferative activity of NVP-TAE 226 (ranging from 0.25 to 1μM) on cells growing in culture is determined using a tetrazolium-based colorimetric MTT assay. |
动物实验: |
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Mice Male nude mice used for this study are 6 to 8 weeks old. In DMEM/F12 serum-free media (5μL), 5×105 of U87 cells and 1×106 of LN229 cells per mouse are implanted intracranially through a guide-screw system. Four days after injection of the tumor cells, mice are randomized into three groups for each cell line (n=6). Mice in group 1 are treated with 50mg/kg NVP-TAE 226 in 200μL of 0.5% methylcellulose, via an oral gavage. The mice in group 2 receive 75mg/kg NVP-TAE 226 in 200μL of 0.5% methylcellulose. The mice in group 3 the same vehicle used for administration of NVP-TAE 226 (control). Treatment frequency is once a day for 5 days and off for 2 days, for a duration of 4 weeks. Mice are monitored daily. Mice are euthanized when they are moribund, and the whole brain is extracted for rapid freezing in liquid nitrogen and storage at -70℃. |
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 )