Cyclophosphamide Monohydrate

別名: NSC-26271 Monohydrate 中文名稱：環(huán)磷酰胺一水物

目錄號(hào)：S2057 Purity: 99.20%

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(xì)胞毒性作用。

Cyclophosphamide Monohydrate Chemical Structure

CAS: 6055-19-2

規(guī)格	價(jià)格	庫存
50mg	785.09	現(xiàn)貨
200mg	2375.1	現(xiàn)貨
1g	5487.3	現(xiàn)貨
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產(chǎn)品質(zhì)控

批次：純度： 99.20%

99.20

Cyclophosphamide Monohydrate相關(guān)產(chǎn)品

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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(xì)胞周期化合物庫	點(diǎn)擊展開

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系	實(shí)驗(yàn)類型	給藥濃度	孵育時(shí)間	活性描述	文獻(xiàn)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
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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(xì)胞毒性作用。

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(qiáng)細(xì)胞凋亡，并降低調(diào)控T細(xì)胞的穩(wěn)態(tài)增殖。Cyclophosphamide下調(diào)GITR和FoxP3的表達(dá)，其涉及T(REGs)的抑制活性。^[1] Cyclophosphamide增加原代人肝細(xì)胞培養(yǎng)物中CYP3A4，CYP2C8，和 CYP2C9蛋白水平，從而提高培養(yǎng)的肝細(xì)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(xì)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(shí)，會(huì)產(chǎn)生姐妹染色單體互換。^[3]
實(shí)驗(yàn)圖片	檢測方法	檢測指標(biāo)	實(shí)驗(yàn)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(huì)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(diǎn)試驗(yàn)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(dá)的全細(xì)胞疫苗中，能夠增強(qiáng)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(qiáng)疫苗的功效，而不是通過對癌細(xì)胞的直接細(xì)胞溶解作用發(fā)揮它的作用。^[4]

體內(nèi)研究(In Vivo)

體內(nèi)研究活性

Cyclophosphamide會(huì)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(diǎn)試驗(yàn)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(dá)的全細(xì)胞疫苗中，能夠增強(qiáng)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(qiáng)疫苗的功效，而不是通過對癌細(xì)胞的直接細(xì)胞溶解作用發(fā)揮它的作用。^[4]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試驗(yàn)信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
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

參考文獻(xiàn)
[1] Lutsiak ME, et al. Blood, 2005, 105(7), 2862-2868. [2] Chang TK, et al. Cancer Res, 1997, 57(10), 1946-1954. [3] Anderson D, et al. Mutat Res, 1995, 330(1-2), 115-181. [4] Machiels JP, et al. Cancer Res, 2001, 61(9), 3689-3697. [5] Magni M, et al. Int J Mol Sci. 2022 Mar 30;23(7):3834. [6] Li P, et al. Nat Immunol. 2021 Sep;22(9):1107-1117. [7] Weber GF. Molecular Therapies of Cancer. 2014 Dec 8:9–112. [8] Huyan XH, et al. Int Immunopharmacol. 2011;11(9):1293-1297. + 展開

參考文獻(xiàn)

[1] Lutsiak ME, et al. Blood, 2005, 105(7), 2862-2868.
[2] Chang TK, et al. Cancer Res, 1997, 57(10), 1946-1954.
[3] Anderson D, et al. Mutat Res, 1995, 330(1-2), 115-181.

[4] Machiels JP, et al. Cancer Res, 2001, 61(9), 3689-3697.
[5] Magni M, et al. Int J Mol Sci. 2022 Mar 30;23(7):3834.
[6] Li P, et al. Nat Immunol. 2021 Sep;22(9):1107-1117.
[7] Weber GF. Molecular Therapies of Cancer. 2014 Dec 8:9–112.
[8] Huyan XH, et al. Int Immunopharmacol. 2011;11(9):1293-1297.

+ 展開

化學(xué)信息&溶解度

分子量	279.1	分子式	C₇H₁₅Cl₂N₂O₂P.H₂O
CAS號(hào)	6055-19-2	SDF	Download Cyclophosphamide Monohydrate SDF
Smiles	C1CNP(=O)(OC1)N(CCCl)CCCl.O
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1年-80°C溶于溶劑
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1個(gè)月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 55 mg/mL ( (197.06 mM) ；DMSO吸濕會(huì)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)

DMSO : 56 mg/mL ( (200.64 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請使用新開封DMSO)

Water : 56 mg/mL (200.64 mM)

Ethanol : 56 mg/mL (200.64 mM)

DMSO : 56 mg/mL ( (200.64 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請使用新開封DMSO)

Water : 56 mg/mL (200.64 mM)

Ethanol : 56 mg/mL (200.64 mM)

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

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(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計(jì)算器分子量計(jì)算器

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動(dòng)物的藥量）

給藥劑量 mg/kg 動(dòng)物平均體重 g 每只動(dòng)物給藥體積 μL 動(dòng)物數(shù)量只

第二步：請輸入動(dòng)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(jì)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(jìn)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.

C1=C0/X	C1:	LOG(C1):
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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):

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