Home DNA Damage/DNA Repair DNA/RNA Synthesis 억제제 Floxuridine (FUDR)

연구용

Floxuridine (FUDR) DNA/RNA Synthesis 억제제

제품 번호S1299

Floxuridine (FUDR)은 생체 내에서 5-플루오로우라실로 빠르게 이화되는 전구약물로, 다양한 암, 특히 간으로의 전이를 치료하는 데 사용됩니다. 이는 Poly(ADP-Ribose) polymerase를 억제하고 DNA 손상 및 apoptosis를 유도합니다. 이 화합물은 또한 HSV 및 CMV에 대한 항바이러스 효과가 있습니다.
Floxuridine (FUDR) DNA/RNA Synthesis 억제제 Chemical Structure

화학 구조

분자량: 246.19

바로가기

품질 관리

배치: 순도: 99.99%
99.99

세포 배양, 처리 및 작업 농도

세포주 분석 유형 농도 배양 시간 제형 활성 설명 PMID
CCRF-CEM cell Growth inhibition assay Tested in vitro for the inhibition of cell growth of human T lymphoblastoid CCRF-CEM cell line (ATCC CCL 119), IC50=0.5 μM
CCRF-CEM Growth inhibition assay In vitro concentration required for 50% inhibition of growth of human leukemia cell line CCRF-CEM with hPAP (0.2 unit/mL), GI50=0.0006 μM
LNCaP cells Cytotoxicity assay Cytotoxic concentration in prostate specific antigen (PSA) producing human LNCaP cells, IC50=0.0692 μM
TSU cells Cytotoxicity assay Cytotoxic concentration in non prostate specific antigen (PSA) producing human TSU cells, IC50=0.058 μM
KBALB cell Cytotoxicity assay In vitro cell cytotoxicity against KBALB cell line (transformed fibroblast sarcoma cell line), CC50=6.00E-05 μM
KBALB-STK cell Cytotoxicity assay In vitro cell cytotoxicity against KBALB-STK cell lines expressed in HSV-1 TK, IC50=8.80E-05 μM
L1210 mouse leukemia cells Growth inhibition assay 24 h Growth inhibition in L1210 mouse leukemia cells after 24 h treatment, IC50=0.0041 μM
L1210 mouse leukemia cells Growth inhibition assay 48 h Growth inhibition in L1210 mouse leukemia cells after 48 hr treatment, IC50=0.00064 μM
L5178Y cell Growth inhibition assay Comparative inhibition of L5178Y cell growth in vitro (concentration required for 50% inhibition), IC50=0.00076 μM
L5178Y cells Function assay Inhibitory concentration of compound was calculated on L5178Y cells by [14C]Leu incorporation, IC50=2 μM
L1210 mouse leukemia cells Function assay 2 h Thymidylate synthase inhibition in L1210 mouse leukemia cells after 2 hr treatment, IC50=0.0079 μM
LM cells Function assay 2 h Thymidylate synthase inhibition in thymidine kinase deficient LM cells after 2 hr treatment, IC50=5.4 μM
HT1080 cells Function assay Cytostatic activity against human HT1080 cells by MTT assay, IC50=0.18 μM
L1210 cells Growth inhibition assay 72 h Cytostatic activity against mouse L1210 cells ATCC CCL219 assessed as growth reduction after 72 hrs, IC50=0.012 μM
HL60 cells Growth inhibition assay 72 h Cytostatic activity against human HL60 cells ATCC CCL 240 assessed as growth reduction after 72 hrs, IC50=0.012 μM
CCRF-CEM cells Growth inhibition assay 72 h Cytostatic activity against human CCRF-CEM cells ATCC CCL 119 assessed as growth reduction after 72 hrs, IC50=0.017 μM
L1210 cells Growth inhibition assay 72 h Cytostatic activity in mouse L1210 cells assessed as inhibition of cell growth after 72 hrs, IC50=0.012 μM
HL60 cells Growth inhibition assay 72 h Cytostatic activity in human HL60 cells assessed as inhibition of cell growth after 72 hrs, IC50=0.012 μM
CCRF-CEM cells Growth inhibition assay 72 h Cytostatic activity in human CCRF-CEM cells assessed as inhibition of cell growth after 72 hrs, IC50=0.017 μM
CCRF-CEM cells Function assay 48 h Anticancer activity against human CCRF-CEM cells after 48 hrs by sulforhodamine B assay, GI50=0.00631 μM
K562 cells Function assay 48 h Anticancer activity against human K562 cells after 48 hrs by sulforhodamine B assay, GI50=0.79433 μM
MOLT4 cells Function assay 48 h Anticancer activity against human MOLT4 cells after 48 hrs by sulforhodamine B assay, GI50=0.03981 μM
RPMI8266 cells Function assay 48 h Anticancer activity against human RPMI8266 cells after 48 hrs by sulforhodamine B assay, GI50=0.79433 μM
human SR cells Function assay 48 h Anticancer activity against human SR cells after 48 hrs by sulforhodamine B assay, GI50=0.01259 μM
A549 cells Function assay 48 h Anticancer activity against human A549 cells after 48 hrs by sulforhodamine B assay, GI50=0.01259 μM
EKVX cells Function assay 48 h Anticancer activity against human EKVX cells after 48 hrs by sulforhodamine B assay, GI50=10 μM
HOP62 cells Function assay 48 h Anticancer activity against human HOP62 cells after 48 hrs by sulforhodamine B assay, GI50=0.02512 μM
HOP92 cells Function assay 48 h Anticancer activity against human HOP92 cells after 48 hrs by sulforhodamine B assay, GI50=0.79433 μM
NCI-H226 cells Function assay 48 h Anticancer activity against human NCI-H226 cells after 48 hrs by sulforhodamine B assay
NCI-H23 Function assay 48 h Anticancer activity against human NCI-H23 cells after 48 hrs by sulforhodamine B assay, GI50=10 μM
NCI-H322 Function assay 48 h Anticancer activity against human NCI-H322M cells after 48 hrs by sulforhodamine B assay, GI50=0.50119 μM
NCI-H460 Function assay 48 h Anticancer activity against human NCI-H460 cells after 48 hrs by sulforhodamine B assay, GI50=0.50119 μM
NCI-H522 Function assay 48 h Anticancer activity against human NCI-H522 cells after 48 hrs by sulforhodamine B assay, GI50=0.002 μM
COLO205 cells Function assay 48 h Anticancer activity against human COLO205 cells after 48 hrs by sulforhodamine B assay, GI50=2.51189 μM
HCC2998 cells Function assay 48 h Anticancer activity against human HCC2998 cells after 48 hrs by sulforhodamine B assay, GI50=1.58489 μM
HCT116 cells Function assay 48 h Anticancer activity against human HCT116 cells after 48 hrs by sulforhodamine B assay, GI50=0.001 μM
HCT15 cells Function assay 48 h Anticancer activity against human HCT15 cells after 48 hrs by sulforhodamine B assay, GI50=0.12589 μM
HT-29 cells Function assay 48 h Anticancer activity against human HT-29 cells after 48 hrs by sulforhodamine B assay, GI50=1.99526 μM
KM12 cells Function assay 48 h Anticancer activity against human KM12 cells after 48 hrs by sulforhodamine B assay, GI50=2.51189 μM
SW620 cells Function assay 48 h Anticancer activity against human SW620 cells after 48 hrs by sulforhodamine B assay, GI50=6.30957 μM
SF268 cells Function assay 48 h Anticancer activity against human SF268 cells after 48 hrs by sulforhodamine B assay, GI50=10 μM
SF295 cells Function assay 48 h Anticancer activity against human SF295 cells after 48 hrs by sulforhodamine B assay, GI50=0.01259 μM
SF539 cells Function assay 48 h Anticancer activity against human SF539 cells after 48 hrs by sulforhodamine B assay, GI50=0.03981 μM
SNB19 cells Function assay 48 h Anticancer activity against human SNB19 cells after 48 hrs by sulforhodamine B assay, GI50=1.99526 μM
SNB75 cells Function assay 48 h Anticancer activity against human SNB75 cells after 48 hrs by sulforhodamine B assay, GI50=0.19953 μM
U251 cells Function assay 48 h Anticancer activity against human U251 cells after 48 hrs by sulforhodamine B assay, GI50=0.12589 μM
LOXIMVI cells Function assay 48 h Anticancer activity against human LOXIMVI cells after 48 hrs by sulforhodamine B assay, GI50=0.02512 μM
MALME-3M cells Function assay 48 h Anticancer activity against human MALME-3M cells after 48 hrs by sulforhodamine B assay, GI50=7.94328 μM
M14 cells Function assay 48 h Anticancer activity against human M14 cells after 48 hrs by sulforhodamine B assay, GI50=0.15849 μM
SK-MEL-2 cells Function assay 48 h Anticancer activity against human SK-MEL-2 cells after 48 hrs by sulforhodamine B assay, GI50=10 μM
SK-MEL-28 cells Function assay 48 h Anticancer activity against human SK-MEL-28 cells after 48 hrs by sulforhodamine B assay, GI50=1.99526 μM
SK-MEL-5 cells Function assay 48 h Anticancer activity against human SK-MEL-5 cells after 48 hrs by sulforhodamine B assay, GI50=0.19953 μM
UACC257 cells Function assay 48 h Anticancer activity against human UACC257 cells after 48 hrs by sulforhodamine B assay, GI50=3.16228 μM
UACC62 cells Function assay 48 h Anticancer activity against human UACC62 cells after 48 hrs by sulforhodamine B assay, GI50=0.03981 μM
IGROV1 cells Function assay 48 h Anticancer activity against human IGROV1 cells after 48 hrs by sulforhodamine B assay, GI50=2.51189 μM
OVCAR-3 cells Function assay 48 h Anticancer activity against human OVCAR-3 cells after 48 hrs by sulforhodamine B assay, GI50=2.51189 μM
OVCAR4 cells Function assay 48 h Anticancer activity against human OVCAR4 cells after 48 hrs by sulforhodamine B assay, GI50=10 μM
OVCAR5 cells Function assay 48 h Anticancer activity against human OVCAR5 cells after 48 hrs by sulforhodamine B assay, GI50=6.30957 Μm
OVCAR8 cells Function assay 48 h Anticancer activity against human OVCAR8 cells after 48 hrs by sulforhodamine B assay, GI50=0.12589 μM
SKOV3 cells Function assay 48 h Anticancer activity against human SKOV3 cells after 48 hrs by sulforhodamine B assay, GI50=1.99526 μM
786-0 cells Function assay 48 h Anticancer activity against human 786-0 cells after 48 hrs by sulforhodamine B assay, GI50=0.1 μM
A498 cells Function assay 48 h Anticancer activity against human A498 cells after 48 hrs by sulforhodamine B assay, GI50=1.25893 μM
ACHN cells Function assay 48 h Anticancer activity against human ACHN cells after 48 hrs by sulforhodamine B assay, GI50=0.03162 μM
Caki1 cells Function assay 48 h Anticancer activity against human Caki1 cells after 48 hrs by sulforhodamine B assay, GI50=0.03162 μM
SN12C cells Function assay 48 h Anticancer activity against human SN12C cells after 48 hrs by sulforhodamine B assay, GI50=0.19953 μM
TK10 cells Function assay 48 h Anticancer activity against human TK10 cells after 48 hrs by sulforhodamine B assay, GI50=5.01187 μM
UO31 cells Function assay 48 h Anticancer activity against human UO31 cells after 48 hrs by sulforhodamine B assay, GI50=0.12589 μM
PC3 cells Function assay 48 h Anticancer activity against human PC3 cells after 48 hrs by sulforhodamine B assay, GI50=0.31623 μM
DU145 cells Function assay 48 h Anticancer activity against human DU145 cells after 48 hrs by sulforhodamine B assay, GI50=0.25119 μM
MCF7 cells Function assay 48 h Anticancer activity against human MCF7 cells after 48 hrs by sulforhodamine B assay, GI50=0.00631 μM
NCI/ADR-RES cells Function assay 48 h Anticancer activity against human NCI/ADR-RES cells after 48 hrs by sulforhodamine B assay, GI50=1.25893 μM
MDA-MB-231 cells Function assay 48 h Anticancer activity against human MDA-MB-231 cells after 48 hrs by sulforhodamine B assay, GI50=3.98107 μM
Hs 578T cells Function assay 48 h Anticancer activity against human Hs 578T cells after 48 hrs by sulforhodamine B assay, GI50=3.98107 μM
MDA-MB-435 cells Function assay 48 h Anticancer activity against human MDA-MB-435 cells after 48 hrs by sulforhodamine B assay, GI50=3.16228 μM
MDA-N cells Function assay 48 h Anticancer activity against human MDA-N cells after 48 hrs by sulforhodamine B assay, GI50=1.25893 μM
BT549 cells Function assay 48 h Anticancer activity against human BT549 cells after 48 hrs by sulforhodamine B assay, GI50=1 μM
T47D cells Function assay 48 h Anticancer activity against human T47D cells after 48 hrs by sulforhodamine B assay, GI50=1.25893 μM
HepG2 cells Cytotoxicity assay 72 h Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay, EC50=18.84 μM
A549 cells Cytotoxicity assay 72 h Cytotoxicity against human A549 cells after 72 hrs by MTT assay, EC50=9.74 μM
LAC cells Cytotoxicity assay 72 h Cytotoxicity against human LAC cells after 72 hrs by MTT assay, EC50=32.09 μM
HeLa cells Cytotoxicity assay 72 h Cytotoxicity against human HeLa cells after 72 hrs by MTT assay, EC50=10.26 μM
MDA-MB-231 cells Cytotoxicity assay Cytotoxicity against human MDA-MB-231 cells overexpressing urokinase plasminogen activator, IC50=0.21 μM
human ACHN cells Function assay Anticancer activity against human ACHN cells by SRB assay, GI50=2.1 μM
PC3 cells Function assay Anticancer activity against human PC3 cells by SRB assay, GI50=4.97 μM
MDA-MB-231 cells Function assay Anticancer activity against human MDA-MB-231 cells by SRB assay, GI50=0.16 μM
FM3A cells Function assay 2 days Cytostatic activity against mouse FM3A cells after 2 days by coulter counting analysis, IC50=0.0094 μM
HeLa cells Function assay Cytostatic activity against human HeLa cells in presence of 20 uM thymidine, IC50=8.5 μM
LLC cells Cytotoxicity assay 24 h Cytotoxicity against mouse LLC cells after 24 hrs by resazurin assay, IC50=14.2 μM
LLC cells Cytotoxicity assay 72 h Cytotoxicity against mouse LLC cells after 72 hrs by resazurin assay, IC50=2 μM
RAW264.7 cells Cytotoxicity assay 72 h Cytotoxicity against mouse RAW264.7 cells after 72 hrs by resazurin assay, IC50=30 μM
A549 cells Cytotoxicity assay 72 h Cytotoxicity against human A549 cells assessed as cell viability after 72 hrs by WST-8 assay, IC50=0.047 μM
A2780 cells Cytotoxicity assay 5 days Cytotoxicity against human A2780 cells after 5 days by MTT assay, IC50=0.026 μM
LMTK cells Cytotoxicity assay 5 days Cytotoxicity against thymidine kinase-deficient mouse LMTK cells after 5 days by MTT assay, IC50=4.5 μM
A549 cells Cytotoxicity assay 72 h Cytotoxicity against human A549 cells after 72 hrs by microplate reader method, IC50=0.0124 μM
CEM cells Function assay 72 h Cytostatic activity against human CEM cells expressing human ENT1 transporter after 72 hrs by cell counting in presence of NBMPR, IC50=0.8 μM
Hela cells Function assay 72 h Cytostatic activity against human HeLa cells after 72 hrs by cell counting, IC50=0.05 μM
CEM/0 cells Function assay 72 h Cytostatic activity against human CEM/0 cells after 72 hrs by cell counting, IC50=0.022 μM
L1210/0 cells Function assay 48 h Cytostatic activity against mouse L1210/0 cells after 48 hrs by cell counting, IC50=0.0009 μM
MCF7 cells Cytotoxicity assay 72 h Cytotoxicity against human MCF7 cells after 72 hrs by SRB assay, IC50=12.19 μM
HeLa cells Cytotoxicity assay 72 h Cytotoxicity against human HeLa cells after 72 hrs by SRB assay, IC50=6.5 μM
HL60 cells Proliferation assay 72 h Antiproliferative activity against human HL60 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=0.24 μM
SW707 cells Proliferation assay 72 h Antiproliferative activity against human SW707 cells assessed as growth inhibition after 72 hrs by SRB method, IC50=23.86 μM
LoVo cells Proliferation assay 72 h Antiproliferative activity against human LoVo cells assessed as growth inhibition after 72 hrs by SRB method, IC50=19.07 μM
BALB/3T3 cell Proliferation assay 72 h Antiproliferative activity against mouse BALB/3T3 cells assessed as growth inhibition after 72 hrs by SRB method, IC50=23.9 μM
HFF cells Function assay 72 h Antiparasitic activity against Toxoplasma gondii ATCC 50839 infected in HFF cells after 72 hrs by beta-galactosidase reporter gene assay, EC50=0.91 μM
CCRFCEM cells Function assay Cytostatic activity against human CCRFCEM cells by MTT assay, IC50=0.29 μM
RXF393 cells Function assay 48 h Anticancer activity against human RXF393 cells after 48 hrs by sulforhodamine B assay, GI50=3.98107 μM
HL-60(TB) cells Function assay 48 h Anticancer activity against human HL-60(TB) cells after 48 hrs by sulforhodamine B assay, GI50=0.19953 μM
L1210 cells Function assay 15 mins Inhibition of thymidylate synthase in mouse L1210 cells assessed as inhibition of tritium release from [5-3H]deoxyuridine after preincubation for 15 mins by liquid scintillation counting, IC50=0.0006 μM
Colo-357 cells Function assay 100 μM 15 mins Activity at MRP5 in human Colo-357 cells assessed as 5-FdUMP accumulation at 100 uM after 15 mins
KB cells Cytotoxicity assay 72 h Cytotoxicity against human KB cells after 72 hrs by SRB assay, IC50=8.69 μM
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성

분자량 246.19 화학식

C9H11FN2O5

 보관 (수령일로부터)
CAS 번호 50-91-9 SDF 다운로드 원액 보관

동의어 NSC 27640, Deoxyfluorouridine Smiles C1C(C(OC1N2C=C(C(=O)NC2=O)F)CO)O

용해도

In vitro
배치:

DMSO : 49 mg/mL (199.03 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : 49 mg/mL

Ethanol : 10 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

시험관 내(In vitro)
Floxuridine (FUDR)은 해당 5'-O-모노 아미노산 에스테르 전구약물보다 PEPT1에 대한 더 높은 친화성을 보입니다. 류코보린과 병용 시, 인간 T-림프모세포 백혈병 세포 성장에 대한 시너지 억제 효과를 나타냅니다. 이 화합물은 [(3)H]-이노신과 [(3)H]-아데노신 모두의 흡수를 유의하게 억제하는 반면(대조군의 60-70%), Val, Phe, Pro, Asp, Lys 에스테르를 포함한 아미노산 에스테르 전구약물은 현저히 감소된 억제 효능을 보입니다(대조군의 10-30%). 36일째에 미처리 대조군 세포에 비해 50% 이상 세포 증식을 억제하며, 세포 수는 초기 세포 밀도에 비해 여전히 4배 증가합니다. 또한 인간 테논낭 섬유아세포의 생체 외 증식에 대한 지속적인 효과를 나타냅니다. 짧은 반감기, 가파른 용량 반응 곡선, 높은 전신 청소율 및 높은 간 추출률로 인해 간동맥 주입(HAI)에 이상적인 약물입니다.
참조
  • [4] https://pubmed.ncbi.nlm.nih.gov/1386726/
  • [5] https://pubmed.ncbi.nlm.nih.gov/19383854/

임상시험 정보

(데이터 출처 https://clinicaltrials.gov, 업데이트 날짜 2024-05-22)

NCT 번호 모집 조건 스폰서/협력자 시작일 단계
NCT01042691 Completed
Unresectable Colorectal Liver Metastases
David Bartlett|The Pittsburgh Foundation|Sanofi|University of Pittsburgh
 May 2003 Phase 1
NCT00695201 Completed
Colon Cancer|Rectal Cancer
Memorial Sloan Kettering Cancer Center|University of Medicine and Dentistry of New Jersey|Rutgers The State University of New Jersey|Sanofi
 August 2000 Phase 1

기술 지원

취급 설명서

Tel: +1-832-582-8158 Ext:3

다른 문의사항이 있으시면 메시지를 남겨주세요.

이름을 입력해주세요.
이메일을 입력해주세요. 유효한 이메일 주소를 입력해주세요.
저희에게 무엇이든 작성해주세요.