Cyclophosphamide Monohydrate

別名：NSC-26271 Monohydrate

製品コード：S2057 純度：99.20%

Cyclophosphamide Monohydrate is a nitrogen mustard alkylating agent, it attaches the alkyl group to the guanine base of DNA, shown to crosslink DNA, causing strand breakage and inducing mutations.

CAS No. 6055-19-2

サイズ	価格(税別)	在庫状況
50mg	JPY 22000	国内在庫あり
200mg	JPY 43500	国内在庫あり
1g	JPY 100500	国内在庫あり

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（35）

製品安全説明書

現在のバッチを見る：純度： 99.20%

99.20

Cyclophosphamide Monohydrate関連製品

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DNA alkylator阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
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
他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

生物活性

製品説明	Cyclophosphamide Monohydrate is a nitrogen mustard alkylating agent, it attaches the alkyl group to the guanine base of DNA, shown to crosslink DNA, causing strand breakage and inducing mutations.

In Vitro
In vitro	Cyclophosphamide (CY) is a chemotherapeutic agent with a dose-dependent, bimodal effect on the immune system. Cyclophosphamide treatment enhances apoptosis and decreases homeostatic proliferation of regulatory T cells. Cyclophosphamide downregulates the expression of GITR and FoxP3, which are involved in the suppressive activity of T(REGs).^[1] Cyclophosphamide increases CYP3A4, CYP2C8, and CYP2C9 protein levels in primary human hepatocyte cultures, which thereby enhances their own rates of 4-hydroxylation in the cultured hepatocytes. ^[2] Cyclophosphamide has produced mutations in base-pair substituting strains of Salmonella tryphimurium in the presence of metabolic activation, but it has been shown to be negative in the E. coli chromotest. Cyclophosphamide has been shown to produce gene mutations, chromosome aberrations, micronuclei and sister chromatid exchanges in a variety of cultured cells in the presence of metabolic activation as well as sister chromatid exchanges without metabolic activation. ^[3]
細胞実験	細胞株	SUP-T1 cells
	濃度	5.84 pM
	反応時間	3 h
	実験の流れ	Cells were treated with indicated concentrations of drug.
実験結果図	Methods	Biomarkers	結果図	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

In Vivo
In Vivo	Cyclophosphamide has also produced chromosome damage and micronuclei in rats, mice and Chinese hamsters, and gene mutations in the mouse spot test and in the transgenic lacZ construct of Muta Mouse. ^[3] Cyclophosphamide, when given in a defined sequence with a GM-CSF-secreting, neu-expressing whole-cell vaccine, enhances the vaccine's potential to delay tumor growth in neu transgenic mice. Cyclophosphamide mediates its effects by enhancing the efficacy of the vaccine rather than via a direct cytolytic effect on cancer cells. ^[4]
動物実験	動物モデル	Female MRL/lpr mice
	投与量	10 mg/kg
	投与経路	i.p.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (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

参考
[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

参考

+ 展開

化学情報

分子量	279.1	化学式	C₇H₁₅Cl₂N₂O₂P.H₂O
CAS No.	6055-19-2	SDF	Download Cyclophosphamide Monohydrate SDFをダウンロードする
Smiles	C1CNP(=O)(OC1)N(CCCl)CCCl.O
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	１ケ月-20°Cin solvent

In vitro
Batch:

DMSO : 55 mg/mL ( (197.06 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : 55 mg/mL

Ethanol : 55 mg/mL

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

技術サポート

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よくある質問（FAQ）

質問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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C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):