中文名称: D-I03  一键复制产品信息
英文名称: D-I03
CAS No: 688342-78-1
分子式: C13H20N2O2
分子量: 428.64
D10803 D-I03 ≥98% (普西唐-psaitong)
包装规格:
1mg 5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性:
溶于DMSO(≥ 100 mg/mL)
产品描述:

基本信息

产品编号:D10803

产品名称:D-I03

CAS:

688342-78-1

 

储存条件

粉末

-20℃

四年

 

 

分子式:

C13H20N2O2

溶于液体

-80℃

两年

分子量

428.64

-20℃

一个月

化学名: 

N-[2-(diethylamino)ethyl]-N'-[2-(4-ethylpiperazin-1-yl)-4-methylquinolin-6-yl]thiourea

 

Solubility (25°C)

 

体外

DMSO

86mg/mL (200.63mM)

Ethanol

10mg/mL (23.32mM)

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

2.3330mL

11.6648mL

23.3296mL

5mM

0.4666mL

2.3330mL

4.6659mL

10mM

0.2333mL

1.1665mL

2.3330mL

50mM

0.0467mL

0.2333mL

0.4666mL

 

 

生物活性

产品描述

一种选择性 RAD52 抑制剂,Kd 为 25.8μM。D-I03 抑制 RAD52 依赖性单链退火 (SSA) 和 D 环形成,IC50 分别为 5μM 和 8μM。

靶点/IC50

RAD52 
(Cell-free assay)

25.8μM(Ki)

 

体外研究

D-I03 (0-10μM; on days 1 and 3; Capan-1 and UWB1.289 cells) treatment preferentially suppressed the growth of Capan-1 and UWB1.289 cells in a concentration-dependent manner.

D-I03 inhibits RAD52 foci formation induced by cisplatin in BCR-ABL1-positive BRCA1-deficient 32Dcl3murine hematopoietic cell line that expresses GFP-RAD52. In the presence of D-I03 (2.5μM), the fraction of cells with RAD52 foci is decreased, from 38.7% to 171%; at the same time, the fraction of Cisplatin-treated cells without foci is increased from 48.4% to 71.9%. D-I03 does not effect on RAD51 foci induced by Cisplatin. Also, D-I03 alone induce neither RAD51 foci nor RAD52 foci (in BRCA1- deficient cells) indicating low genotoxicity of D-I03.

Cell Proliferation Assay

Cell Line:

Capan-1 (BRCA2− ) and UWB1.289 (BRCA1+ ) cells

Concentration:

0μM, 2.5μM, 5μM, or 10μM

Incubation Time:

On days 1 and 3

Result:

Preferentially suppressed the growth of Capan-1 and UWB1.289 cells.

 

体内研究

D-I03 (50 mg/kg/day; intraperitoneal injection; daily; for 7 days; nu/nu mice) treatment reduces BRCA1-deficient MDA-MB436 tumor growth. Talazoparib puls D-I03 does not affect the growth of BRCA1-proficient tumors and does not exert any significant toxicity against normal tissues and organs. Pharmacokinetic and toxicity studies indicates that maximal tolerated dose of D-I03 is ≥50mg/kg, and t1/2 is 23.4 hours, resulting in >1μM maximal concentration in peripheral blood.

Animal Model:

Nu/nu mice injected with BRCA1-deficient MDA-MB-436 cells

Dosage:

50mg/kg/day

Administration:

Intraperitoneal injection; daily; for 7 days

Result:

Reduced BRCA1-deficient MDA-MB-436 tumor growth.

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
安全说明:
搜索质检报告(COA)

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):