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Cyclophosphamide Monohydrate
別名: NSC-26271 Monohydrate 中文名稱：環(huán)磷酰胺一水物
Cyclophosphamide Monohydrate是一種氮芥類烷化劑，使烷基連接到DNA的鳥嘌呤堿基。與DNA交聯(lián)，造成DNA鏈斷裂，引起突變。具有細胞毒性作用。Cyclophosphamide?(NSC-26271) Monohydrate 可用于誘導(dǎo)貧血動物模型。
Cyclophosphamide Monohydrate Chemical Structure
CAS: 6055-19-2
產(chǎn)品質(zhì)控
批次：
純度：
99.20%
99.20
Cyclophosphamide Monohydrate相關(guān)產(chǎn)品
| 相關(guān)靶點 | AGT | 點擊展開 |
|---|---|---|
| 相關(guān)產(chǎn)品 | Lomeguatrib Methyl methanesulfonate Lobaplatin (D-19466) | 點擊展開 |
| 相關(guān)化合物庫 | FDA藥物庫 天然產(chǎn)物庫 凋亡分子化合物庫 DNA損傷/ DNA修復(fù)化合物庫 細胞周期化合物庫 | 點擊展開 |
細胞實驗數(shù)據(jù)示例
| 細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
|---|---|---|---|---|---|
| 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 | ||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | Cyclophosphamide Monohydrate是一種氮芥類烷化劑，使烷基連接到DNA的鳥嘌呤堿基。與DNA交聯(lián)，造成DNA鏈斷裂，引起突變。具有細胞毒性作用。Cyclophosphamide?(NSC-26271) Monohydrate 可用于誘導(dǎo)貧血動物模型。 |
|---|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | Cyclophosphamide (CY)是一種化學(xué)治療劑，對免疫系統(tǒng)具有劑量依賴性雙重作用。Cyclophosphamide治療增強細胞凋亡，并降低調(diào)控T細胞的穩(wěn)態(tài)增殖。Cyclophosphamide下調(diào)GITR和FoxP3的表達，其涉及T(REGs)的抑制活性。[1] Cyclophosphamide增加原代人肝細胞培養(yǎng)物中CYP3A4，CYP2C8，和 CYP2C9蛋白水平，從而提高培養(yǎng)的肝細胞中它們自身的4-羥基化比率。[2] 代謝活化存在下，Cyclophosphamide使Salmonella tryphimurium的堿基對取代菌株產(chǎn)生突變，但是在 E. coli顯色測試中顯示為陰性。代謝活化存在下，Cyclophosphamide能夠使各種人工培養(yǎng)的細胞中產(chǎn)生基因突變，染色體畸變，微核和姐妹染色單體互換，并且代謝活化不存在時，會產(chǎn)生姐妹染色單體互換。[3] |
|||
|---|---|---|---|---|
| 實驗圖片 | 檢測方法 | 檢測指標 | 實驗圖片 | 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 |
|
31654636 | |
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | Cyclophosphamide會使大鼠，小鼠和中國倉鼠體內(nèi)產(chǎn)生染色體損傷和微核，并且在小鼠斑點試驗和Muta小鼠轉(zhuǎn)基因lacZ構(gòu)建體中產(chǎn)生基因突變。[3] Cyclophosphamide，以確定的順序加入到GM-CSF-分泌的，neu-表達的全細胞疫苗中，能夠增強疫苗的潛在作用以延緩neu轉(zhuǎn)基因小鼠體內(nèi)的腫瘤生長。Cyclophosphamide通過增強疫苗的功效，而不是通過對癌細胞的直接細胞溶解作用發(fā)揮它的作用。[4] |
|
|---|---|---|
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT06186700 | Active not recruiting | Breast Cancer Female |
Mansoura University |
December 25 2023 | Phase 2 |
| NCT06085742 | Recruiting | Breast Cancer |
University of Illinois at Chicago |
November 22 2023 | Phase 2 |
| NCT05800041 | Not yet recruiting | Gout Tophus |
RenJi Hospital|Westlake Therapeutics |
April 10 2023 | Early Phase 1 |
化學(xué)信息&溶解度
| 分子量 | 279.1 | 分子式 | C7H15Cl2N2O2P.H2O |
| CAS號 | 6055-19-2 | SDF | Download Cyclophosphamide Monohydrate SDF |
| Smiles | C1CNP(=O)(OC1)N(CCCl)CCCl.O | ||
| 儲存條件(自收到貨起) | |||
|
體外溶解度 |
DMSO : 55 mg/mL ( (197.06 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Water : 55 mg/mL (197.06 mM) Ethanol : 55 mg/mL (197.06 mM) |
摩爾濃度計算器 |
|
體內(nèi)溶解度 現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動物體內(nèi)配方計算器 | ||||
實驗計算
動物體內(nèi)配方計算器（澄清溶液）
第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）
mg/kg
g
μL
只
第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結(jié)果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；
體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
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常見問題及建議解決方法
問題 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.
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