中文名称: TAE226
英文名称: TAE226
CAS No: 761437-28-9
分子式: C23H25ClN6O3
分子量: 468.94
T10304 TAE226 ≥98%(HPLC) (psaitong)
包装规格:
5mg 25mg 100mg in glass bottle
溶解性:
溶于DMSO(50mg/mL 超声)
产品描述:

基本信息

产品编号:T10304

产品名称:TAE226

CAS:

761437-28-9

 

储存条件

粉末

-20℃

四年

 

 

分子式:

C23H25ClN6O3

溶于液体

-80℃

六个月

分子量

468.94

-20℃

一个月

化学名: 

 

 

Solubility (25°C)

 

体外

DMSO

94mg/mL (200.45mM)

Ethanol

Insoluble

Water

Insoluble

体内(现配现用)

0.5% methylcellulose

30mg/mL

1mg/ml表示微溶或不溶。

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。

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。

靶点/IC50

PYK2
(cell-free assay)

FAK
(cell-free assay)

Insulin Receptor
(cell-free assay)

IGF-1R
(cell-free assay)

c-Met
(cell-free assay)

3.5nM

5.5nM

43.5nM

140nM

160nM

 

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.

 

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:

 

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:

 

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℃.

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
安全说明:
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参考文献 & 客户发表文献

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

  • =
    *
    *
    *选择对应的单位 *空出希望得到的变量,填写另外两个变量

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 )

  • * = *

连续稀释计算器方程

  • 连续稀释

  • 初始浓度:
  • 稀释倍数:
  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):