Home DNA Damage/DNA Repair Alkylating Agent 억제제 Cyclophosphamide Monohydrate

연구용

Cyclophosphamide Monohydrate Alkylating Agent

제품 번호: S2057

Cyclophosphamide Monohydrate는 질소 머스타드 Alkylating Agent의 일종으로, DNA의 구아닌 염기에 알킬기를 결합하여 DNA를 가교 결합시키고, 이로 인해 가닥 절단 및 돌연변이를 유발하는 것으로 밝혀졌습니다.Cyclophosphamide (NSC-26271) Monohydrate는 빈혈 동물 모델을 유도하는 데 사용될 수 있습니다.
Cyclophosphamide Monohydrate Alkylating Agent 억제제 Chemical Structure

화학 구조

분자량: 279.1

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품질 관리 (Quality Control)

배치: 순도: 99.20%
99.20

세포 배양, 처리 및 작업 농도
(Cell Culture, Treatment & Working Concentration)

세포주 분석 유형 농도 배양 시간 제형 활성 설명 PMID
HL60 cells Cytotoxicity assay Cytotoxicity against human HL60 cells by MTT assay, IC50=8.79 μM 20850303
BALB/c 3T3 cells Cytotoxicity assay In vitro cytotoxicity was evaluated in mouse embryo BALB/c 3T3 cells, IC50=37.6 μM 9873412
BALB/c 3T3 Cytotoxicity assay In vitro cytotoxicity against BALB/c 3T3 cells, IC50 = 37.6 μM. 7877150
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
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
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
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
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
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
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
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
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

분자량 279.1 화학식

C7H15Cl2N2O2P.H2O

 보관 (수령일로부터)
CAS 번호 6055-19-2 SDF 다운로드 원액 보관

동의어 NSC-26271 Monohydrate Smiles C1CNP(=O)(OC1)N(CCCl)CCCl.O

용해도 (Solubility)

In vitro
배치:

DMSO : 55 mg/mL (197.06 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : 55 mg/mL

Ethanol : 55 mg/mL

몰농도 계산기

질량 농도 부피 분자량
희석 계산기 분자량 계산기

In vivo
배치:

생체 내 제형 계산기 (투명한 용액)

1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)

mg/kg g μL

2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

계산 결과:

작업 농도: mg/ml;

DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH2O, 혼합하고 투명하게 합니다.

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.

참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.

작용 메커니즘 (Mechanism of Action)

시험관 내(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).

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.

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.

생체 내(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.

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.

참조
  • [4] https://pubmed.ncbi.nlm.nih.gov/11325840/
  • [5] https://pubmed.ncbi.nlm.nih.gov/35409194/
  • [6] https://pubmed.ncbi.nlm.nih.gov/34385713/
  • [7] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7123643/
  • [8] https://pubmed.ncbi.nlm.nih.gov/21530682/

적용 분야 (Applications)

방법 바이오마커 이미지 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
S2057-WB-1
23874108
Growth inhibition assay Cell Viability Tumor Volume Tumor Volume
S2057-Growth-inhibition-assay-1
31429028
IHC tumor cell invasion TUNEL / Caspase 3 PTEN / pAkt / PCNA ovary of mice Caspase-3
S2057-IHC-1
23874108
Immunofluorescence pAKT / pERK Ki-67 / UPK3 / KRT5 / pERK Ki-67 / KRT14 / KRT5 autophagy levels
S2057-IF-1
31654636

임상시험 정보 (Clinical Trial Information)

(데이터 출처 https://clinicaltrials.gov, 업데이트 날짜 2026-07-22)

NCT 번호 모집 조건 스폰서/협력자 시작일 단계
NCT04877613 ACTIVE_NOT_RECRUITING
Metastatic Medullary Thyroid Cancer; Recurrent Thyroid Gland Medullary Carcinoma
University of Pennsylvania
 2021-08-19 PHASE1
NCT03935893 ACTIVE_NOT_RECRUITING
Gastric Cancer; Colorectal Cancer; Pancreatic Cancer; Sarcoma; Mesothelioma; Neuroendocrine Tumors; Squamous Cell Cancer; Merkel Cell Carcinoma; Mismatch Repair Deficiency; Microsatellite Instability
Udai Kammula
 2019-12-03 PHASE2
NCT07220187 NOT_YET_RECRUITING
Richter Syndrome; Transformed Chronic Lymphocytic Leukemia to Diffuse Large B-Cell Lymphoma; Transformed Small Lymphocytic Lymphoma to Diffuse Large B-Cell Lymphoma
SWOG Cancer Research Network
 2026-08-31 PHASE3
NCT05463133 RECRUITING
Chronic Granulomatous Disease
National Institute of Allergy and Infectious Diseases (NIAID)
 2022-07-08 PHASE1; PHASE2
NCT05508009 RECRUITING
SIOD; Cystinosis; FSGS; SLE Nephritis; CKD Stage 4
Alice Bertaina
 2023-01-10 PHASE1; PHASE2
NCT06205290 WITHDRAWN
Leukemia, Lymphocytic, Chronic, B-Cell
Juno Therapeutics, Inc., a Bristol-Myers Squibb Company
 2024-01-16 PHASE3

자주 묻는 질문 (Frequently Asked Questions)

질문 1:
Why does it show no activity in vitro assays?

답변:
The activity of this compound in vitro is controversial and has not been fully determined. It 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.