Cyclophosphamide Monohydrate
别名: NSC-26271 Monohydrate 中文名称：环磷酰胺一水物
Cyclophosphamide Monohydrate是一种氮芥类烷化剂，使烷基连接到DNA的鸟嘌呤碱基。与DNA交联，造成DNA链断裂，引起突变。具有细胞毒性作用。
Cyclophosphamide Monohydrate Chemical Structure
CAS: 6055-19-2
客户使用Selleck的Cyclophosphamide Monohydrate发表文献34篇
产品质控
Cyclophosphamide Monohydrate相关产品
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| 相关产品 | Lomeguatrib O6-Benzylguanine Methyl methanesulfonate Lobaplatin (D-19466) | 点击展开 |
| 相关化合物库 | FDA药物库 天然产物库 凋亡分子化合物库 DNA损伤/ DNA修复化合物库 细胞周期化合物库 | 点击展开 |
DNA alkylator抑制剂选择性比较
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| HL60 cells | Cytotoxicity assay | Cytotoxicity against human HL60 cells by MTT assay, IC50=8.79 μM | 20850303 | ||
| K562 | Antiproliferative assay | 48 hr | Antiproliferative activity against Homo sapiens (human) K562 cells after 48 hr by MTT assay, IC50 = 0.153 μM. | ChEMBL | |
| MCF7 | Cytotoxicity assay | 48 hr | Cytotoxicity against Homo sapiens (human) MCF7 cells after 48 hr by SRB assay, IC50 = 10 mM. | 19372630 | |
| HepG2 | Cytotoxicity assay | 48 hr | Cytotoxicity against Homo sapiens (human) HepG2 cells after 48 hr by MTT assay, IC50 = 0.24 μM. | ChEMBL | |
| U2932 | Antitumor assay | 50 mg/kg | 5 consecutive days | Antitumor activity against human U2932 cells xenografted in SCID mouse assessed as reduction in tumor burden at 50 mg/kg, ip administered for 5 consecutive days measured up to day 40 post cell injection | 28605593 |
| MDA-MB-231 | Cytotoxicity assay | 48 hr | Cytotoxicity against Homo sapiens (human) MDA-MB-231 cells after 48 hr by MTT assay, IC50 = 0.09 μM. | ChEMBL | |
| K562 | Cytotoxicity assay | 48 hr | Cytotoxicity against Homo sapiens (human) K562 cells after 48 hr by MTT assay, IC50 = 0.15 μM. | ChEMBL | |
| NCI-H522 | Antitumor assay | 50 mg/kg | 28 days | Antitumor activity against human NCI-H522 cells xenografted in Balb/c nude mouse assessed as tumor growth inhibition at 50 mg/kg, ig administered once daily for 28 days relative to control | 28092860 |
| U87MG | Anticancer assay | 80 mg/kg | 6 days | Anticancer activity against human U87MG cells xenografted in athymic mouse assessed as tumor suppression at 80 mg/kg, iv Q2D for 6 days | 21106377 |
| MX1 | Antitumor assay | 120 mg/kg | up to 3 weeks | Antitumor activity against human MX1 cells xenografted in nude mouse adjuvant model assessed as increase in mouse survival time at 120 mg/kg, po BID measured up to 3 weeks | 20726512 |
| U87 MG | Antitumor assay | 80 mg/kg | Antitumor activity in human U87 MG cells xenografted mouse at 80 mg/kg, iv administered in Q2D x 5 schedule | 18450456 | |
| B-cells | Immunosuppressive assay | 100 mg/kg | 8 days | Immunosuppressive activity against MAV-1 infected BALB/c mouse assessed as B cells suppression at 100 mg/kg, ip treated 8 days before infection for 4 weeks measured 14 days post infection by flow cytometry | 18268085 |
| T-cells | Immunosuppressive assay | 100 mg/kg | 8 days | Immunosuppressive activity against MAV-1 infected BALB/c mouse assessed as T cells suppression at 100 mg/kg, ip treated 8 days before infection for 4 weeks measured 14 days post infection by flow cytometry | 18268085 |
| BALB/c 3T3 | Cytotoxicity assay | In vitro cytotoxicity against BALB/c 3T3 cells, IC50 = 37.6 μM. | 7877150 | ||
| BALB/c 3T3 cells | Cytotoxicity assay | In vitro cytotoxicity was evaluated in mouse embryo BALB/c 3T3 cells, IC50=37.6 μM | 9873412 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Cyclophosphamide Monohydrate是一种氮芥类烷化剂，使烷基连接到DNA的鸟嘌呤碱基。与DNA交联，造成DNA链断裂，引起突变。具有细胞毒性作用。 |
|---|
| 体外研究(In Vitro) | ||||
| 体外研究活性 | Cyclophosphamide (CY)是一种化学治疗剂，对免疫系统具有剂量依赖性双重作用。Cyclophosphamide治疗增强细胞凋亡，并降低调控T细胞的稳态增殖。Cyclophosphamide下调GITR和FoxP3的表达，其涉及T(REGs)的抑制活性。[1] Cyclophosphamide增加原代人肝细胞培养物中CYP3A4，CYP2C8，和 CYP2C9蛋白水平，从而提高培养的肝细胞中它们自身的4-羟基化比率。[2] 代谢活化存在下，Cyclophosphamide使Salmonella tryphimurium的碱基对取代菌株产生突变，但是在 E. coli显色测试中显示为阴性。代谢活化存在下，Cyclophosphamide能够使各种人工培养的细胞中产生基因突变，染色体畸变，微核和姐妹染色单体互换，并且代谢活化不存在时，会产生姐妹染色单体互换。[3] |
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|---|---|---|---|---|
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | PTEN / pAkt / Caspase 3 / GAPDH Caspase 3 / Cleaved-Caspase 3 / Cleaved-PARP / Tubulin Nuclear AIF / Cytosolic AIF / TBP / GAPDH LC3B I / LC3B II / GAPDH |
|
23874108 | |
| Growth inhibition assay | Cell Viability Tumor Volume Tumor Volume |
|
31429028 | |
| IHC | tumor cell invasion TUNEL / Caspase 3 PTEN / pAkt / PCNA ovary of mice Caspase-3 |
|
23874108 | |
| Immunofluorescence | pAKT / pERK Ki-67 / UPK3 / KRT5 / pERK Ki-67 / KRT14 / KRT5 autophagy levels |
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31654636 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 |
Cyclophosphamide会使大鼠，小鼠和中国仓鼠体内产生染色体损伤和微核，并且在小鼠斑点试验和Muta小鼠转基因lacZ构建体中产生基因突变。[3] Cyclophosphamide，以确定的顺序加入到GM-CSF-分泌的，neu-表达的全细胞疫苗中，能够增强疫苗的潜在作用以延缓neu转基因小鼠体内的肿瘤生长。Cyclophosphamide通过增强疫苗的功效，而不是通过对癌细胞的直接细胞溶解作用发挥它的作用。[4] |
|
|---|---|---|
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT06186700 | Not yet recruiting | Breast Cancer Female |
Mansoura University |
December 25 2023 | Phase 2 |
| NCT06085742 | Recruiting | Breast Cancer |
University of Illinois at Chicago |
October 2023 | Phase 2 |
| NCT05800041 | Not yet recruiting | Gout Tophus |
RenJi Hospital|Westlake Therapeutics |
April 10 2023 | Early Phase 1 |
化学信息&溶解度
| 分子量 | 279.1 | 分子式 | C7H15Cl2N2O2P.H2O |
| CAS号 | 6055-19-2 | SDF | Download Cyclophosphamide Monohydrate SDF |
| Smiles | C1CNP(=O)(OC1)N(CCCl)CCCl.O | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 55 mg/mL ( (197.06 mM)； DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : 55 mg/mL Ethanol : 55 mg/mL |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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常见问题及建议解决方法
问题 1:
Why S2057 Cyclophosphamide Monohydrate shows no activity in vitro assays?
回答：
The activity of this product in vitro is controversial and has not been fully determined. Cyclophosphamide is a prodrug and may need Cytochrome P450 to convert it to the active form: 4-hydroxy cyclophosphamide. It is widely used in vivo, if you are going to use it in vitro, you may need to supplement Cytochrome P450 exogenously.
