Canertinib dihydrochloride - CAS:289499-45-2 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	Canertinib dihydrochloride
英文名称:	Canertinib dihydrochloride
别名:	卡纽替尼二盐酸盐 CI-1033 dihydrochloride; PD-183805 dihydrochloride
CAS No:	289499-45-2	分子式:	C₂₄H₂₅ClFN₅O₃^.₂HCl	分子量:	558.86
CAS No:	289499-45-2
分子式:	C₂₄H₂₅ClFN₅O₃^.₂HCl
分子量:	558.86

安全技术说明书(PDF) MSDS(PDF) 点击下载产品说明书(PDF)

C11473 Canertinib dihydrochloride ≥98% (psaitong)

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包装规格：

100mg in glass bottle

溶解性：

溶于DMSO（≥50mg/ml）

产品描述：

基本信息

产品编号：C11473

产品名称：Canertinib dihydrochloride

CAS:

289499-45-2

储存条件

粉末

-20℃

四年

分子式：

C24H25ClFN5O3.2HCl

溶于液体

-80℃

两年

分子量

558.86

化学名：

Solubility (25°C)

体外

DMSO

100mg/mL (178.93mM)

Ethanol

20mg/mL (35.78mM)

Water

Insoluble

体内（现配现用）

＜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	1.7894mL	8.9468mL	17.8936mL
5mM	0.3579mL	1.7894mL	3.5787mL
10mM	0.1789mL	0.8947mL	1.7894mL
50mM	0.0358mL	0.1789mL	0.3579mL

生物活性

产品描述	一种有效的，不可逆的EGFR抑制剂；抑制细胞EGFR和ErbB2自身磷酸化的IC50值分别为7.4和9nM。
靶点/IC₅₀	EGFR 7.4nM (IC50)	ErbB2 9nM (IC50)
体外研究	Canertinib dihydrochloride (CI-1033 dihydrochloride) significantly inhibits growth of cultured melanoma cells, RaH3 and RaH5, in a dose-dependent manner. IC50 is approximately 0.8μM and by 5μM both cell lines are completely growth-arrested within 72h of treatment. Incubation of exponentially growing RaH3 and RaH5 with 1μM canertinib accumulated the cells in the G1-phase of the cell cycle within 24h of treatment without induction of apoptosis. 1μM canertinib inhibits ErbB1-3 receptor phosphorylation with a concomitant decrease of Akt-, Erk1/2- and Stat3 activity in both cell lines[2] . Canertinib dihydrochloride also is a potent activator of exosome secretion.
体内研究	Canertinib dihydrochloride (CI-1033 dihydrochloride) shows superior in vivo antitumor activity, giving growth delays in A431 xenografts exceeding 50 days following oral administration. The growth of human malignant melanoma xenografts, RaH3 and RaH5, in nude mice is significantly inhibited by i.p. injections of 40mg/kg/day canertinib (Fig. 4). The anti-proliferative effect on melanoma xenografts is visible already within 4 days of treatment and further increased throughout the treatment period as observed through the differences in tumor volumes, reaching statistical significance within 18 days of treatment.

推荐实验方法(仅供参考)

激酶实验：

Enzyme assays for IC50 determinations are performed in 96-well filter plates. The total volume is 0.1mL containing 20mM Hepes, pH 7.4, 50mM sodium vanadate, 40mM magnesium chloride, 10µM adenosine triphosphate (ATP) containing 0.5mCi of [32P]ATP, 20mg of polyglutamic acid/tyrosine, 10ng of EGFR tyrosine kinase, and appropriate dilutions of inhibitor (Canertinib). All components except the ATP are added to the well and the plate is incubated with shaking for 10min at 25°C. The reaction is started by adding [32P]ATP, and the plate is incubated at 25°C for 10min. The reaction is terminated by addition of 0.1mL of 20% trichloroacetic acid (TCA). The plate is kept at 4°C for at least 15 min to allow the substrate to precipitate. The wells is then washed five times with 0.2mL of 10% TCA and 32P incorporation determined with a plate counter.

细胞实验:
RaH3 and RaH5 cells are treated with increasing concentrations (0-10μM) of Canertinib for 72h. The cells are suspended in buffer and counted.

动物实验:

Mice: Canertinib treatment starts when the tumors show reliable growth. The mice are randomized into control and treatment groups. In the canertinib treated RaH3 group (n=4) and RaH5 group (n=7) each mouse receives i.p. injections of 1.2mg canertinib (40mg/kg/day) in 0.1ml 0.15M NaCl 5 days a week. The control RaH3 (n=3) and RaH5 (n=7) mice receive i.p. injections of vehicle only according to the same regimen. At the end of the treatment period, the mice are sacrificed by cervical dislocation where after the tumors are removed and weighed.

保存条件：

-20℃

UN码：

HazardClass：

危害声明：

安全说明：

搜索质检报告(COA)

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

质量 =

浓度 *

体积 *

分子量

*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):

摩尔浓度计算公式

稀释公式

连续稀释计算器方程

连续稀释

计算结果