中文名称: | D-I03 一键复制产品信息 | ||||
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英文名称: | D-I03 | ||||
别名: | N-[2-(diethylamino)ethyl]-N'-[2-(4-ethylpiperazin-1-yl)-4-methylquinolin-6-yl]thiourea;1-(2-(Diethylamino)ethyl)-3-(2-(4-ethylpiperazin-1-yl)-4-methylquinolin-6-yl)thiourea;MLS001197673;HMS2850O18;SMR000559928;VU0483593-1 | ||||
CAS No: | 688342-78-1 | 分子式: | C13H20N2O2 | 分子量: | 428.64 |
CAS No: | 688342-78-1 | ||||
分子式: | C13H20N2O2 | ||||
分子量: | 428.64 |
基本信息
产品编号:D10803 |
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产品名称:D-I03 |
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CAS: |
688342-78-1 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式: |
溶于液体 |
-80℃ |
两年 |
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分子量 |
428.64 |
-20℃ |
一个月 |
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化学名: |
N-[2-(diethylamino)ethyl]-N'-[2-(4-ethylpiperazin-1-yl)-4-methylquinolin-6-yl]thiourea |
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Solubility (25°C) |
体外 |
DMSO |
86mg/mL (200.63mM) |
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Ethanol |
10mg/mL (23.32mM) |
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Water |
Insoluble |
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体内 |
现配现用 |
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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 |
2.3330mL |
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。 |
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靶点/IC50 |
RAD52 25.8μM(Ki) |
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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 |
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Cell Line: |
Capan-1 (BRCA2− ) and UWB1.289 (BRCA1+ ) cells |
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Concentration: |
0μM, 2.5μM, 5μM, or 10μM |
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Incubation Time: |
On days 1 and 3 |
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Result: |
Preferentially suppressed the growth of Capan-1 and UWB1.289 cells. |
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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. |
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Animal Model: |
Nu/nu mice injected with BRCA1-deficient MDA-MB-436 cells |
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Dosage: |
50mg/kg/day |
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Administration: |
Intraperitoneal injection; daily; for 7 days |
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Result: |
Reduced BRCA1-deficient MDA-MB-436 tumor growth. |
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 )