CRT0066101 dihydrochloride - CAS:1883545-60-5 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	CRT0066101 dihydrochloride
英文名称:	CRT0066101 dihydrochloride
CAS No:	1883545-60-5	分子式:	C₁₈H₂₄Cl₂N₆O	分子量:	411.33
CAS No:	1883545-60-5
分子式:	C₁₈H₂₄Cl₂N₆O
分子量:	411.33

安全技术说明书(PDF) MSDS(PDF) 点击下载产品说明书(PDF)

C10864 CRT0066101 dihydrochloride ≥98% (psaitong)

相关产品

CRT0066101 dihydrochloride
CAS No：1883545-60-5
CID755673
CAS No：521937-07-5
kb NB 142-70
CAS No：1233533-04-4
CID-2011756
CAS No：638156-11-3

包装规格：

5mg 10mg 25mg 50mg 100mg in glass bottle

溶解性：

溶于DMSO（≥ 25 mg/mL）

产品描述：

基本信息

产品编号：C10864
产品名称：CRT0066101 dihydrochloride
CAS:	1883545-60-5	储存条件	粉末	-20℃	四年

分子式：	C18H24Cl2N6O		溶于液体	-80℃	六个月
分子量	411.33			-20℃	一个月
化学名：
Solubility (25°C)	体外	DMSO	82mg/mL (199.35mM)
		Ethanol	25mg/mL warmed with 50ºC water bath (60.77mM)
		Water	2mg/mL warmed with 50ºC water bath (4.86mM)
	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	2.4311mL	12.1557mL	24.3114mL
5mM	0.4862 mL	2.4311mL	4.8623mL
10mM	0.2431mL	1.2156mL	2.4311mL
50mM	0.0486mL	0.2431mL	0.4862mL

生物活性

产品描述	是有效，选择性的 PKD 抑制剂，对PKD1，2和3的IC50值分别为1，2.5和2nM。
靶点/IC₅₀	PKD1 (Cell-free assay)	PKD3 (Cell-free assay)	PKD2 (Cell-free assay)
	1nM	2nM	2.5nM
体外研究	CRT0066101 specifically blocks PKD1/2 activity and does not suppress PKCα/PKCβ/PKCε activity in multiple cancer cell types including A549 (lung) and MiaPaCa-2 (pancreas). CRT0066101 significantly inhibits Panc-1 cell proliferation with an IC50 value of 1 µM. Treatment with CRT0066101 results in a 6-10 fold induction of apoptosis in Panc-1 cells. CRT0066101 significantly reduces cell proliferation of Colo357,Panc-1,MiaPaCa-2, and AsPC-1 cells but has a modest effect in Capan-2 cells. CRT0066101 (5µM) blocks both the basal and NT-induced pS916-PKD1/2 (activated PKD1/2) in Panc-1 and Panc-28 cells. CRT0066101 reduces PKD-dependent NF-κB activation and NF-κB-dependent gene expressions in Panc-1.Optimal therapeutic concentrations (8 µM) of CRT0066101 are detectable 6 h after oral administration of this drug.CRT0066101 given orally (80mg/kg/day) for 28 days significantly abrogates PaCa growth in Panc-1 subcutaneous xenograft model. Activated PKD1/2 expression in the treated tumor-explants is significantly inhibited with peak tumor concentration (12µM) of CRT0066101 achieved within 2 h after oral administration. Further, CRT0066101 given orally (80mg/kg/day) for 21 days in Panc-1 orthotopic model potently blocks tumor growth in vivo.CRT0066101 significantly reduces Ki-67+proliferation index, increases TUNEL+ apoptotic cells (p<0.05), and abrogates expression of NF-κB-dependent proteins including cyclin D1, survivin,and cIAP-1.
体内研究	Optimal therapeutic concentrations (8µM) of CRT0066101 are detectable 6 h after oral administration of this drug.CRT0066101 given orally (80mg/kg/day) for 28 days significantly abrogates PaCa growth in Panc-1 subcutaneous xenograft model. Activated PKD1/2 expression in the treated tumor-explants is significantly inhibited with peak tumor concentration (12µM) of CRT0066101 achieved within 2h after oral administration. Further, CRT0066101 given orally (80mg/kg/day) for 21 days in Panc-1 orthotopic model potently blocks tumor growth in vivo.CRT0066101 significantly reduces Ki-67+proliferation index, increases TUNEL+ apoptotic cells (p<0.05), and abrogates expression of NF-κB-dependent proteins including cyclin D1, survivin,and cIAP-1.

推荐实验方法(仅供参考)

细胞实验:
细胞系	Panc-1细胞
浓度	5μM
处理时间	1 小时
方法	将control vectors或过表达PKD1的载体转染到Panc-1细胞中，转染23小时后，用DMSO或5μM CRT0066101对细胞进行预处理，处理1小时，然后提取核蛋白，通过EMSA检测NF-κB的激活情况。

动物实验:

Mice: Nineteen days after implantation of Panc-1 cells, tumor areas are, on average 0.3 cm2 and are randomized into the following groups (n=8 mice per group): (a) vehicle (control) 5% dextrose administered by oral gavage once daily and (b) 80mg/kg CRT0066101 dissolved in 5% dextrose administered by oral gavage once daily. Tumors are measured in 2 dimensions every 2 to 3 days by calipers and area is calculated by multiplying length by width. Therapy is given until tumors reached their designated size limits (1.44 cm2) or until day 24 in CRT0066101 treated group. Final tumor areas are compared among groups using a Student's t test and Fisher’s exact test with p<0.05.

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

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

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稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入输出 )

* = *

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初始浓度:
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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