2'-디옥시-5-플루오로시티딘

한글명:2'-디옥시-5-플루오로시티딘

카스 번호10356-76-0

상품명:2'-DEOXY-5-FLUOROCYTIDINE

CBNumberCB1122369

분자식C9H12FN3O4

포뮬러 무게245.21

MOL 파일10356-76-0.mol

동의어(한글)

2'-디옥시-5-플루오로시티딘

화학적 성질

녹는점	196 °C
끓는 점	465℃
밀도	1.82
굴절률	70 ° (C=1, H2O)
인화점	235℃
저장 조건	Keep in dark place,Inert atmosphere,2-8°C
용해도	DMSO: >20mg/mL
물리적 상태	가루
산도 계수 (pKa)	14.03±0.60(Predicted)
색상	흰색에서 황백색까지
안정성	제공된 대로 구매일로부터 2년 동안 안정적입니다. DMSO의 솔루션은 최대 1개월 동안 -20°에서 보관할 수 있습니다.
CAS 데이터베이스	10356-76-0(CAS DataBase Reference)
EPA	5-Fluoro-2'-deoxycytidine (10356-76-0)

위험 및 안전 성명

위험품 표기

위험 카페고리 넘버

WGK 독일

RTECS 번호

HA3850000

HS 번호

2940.00.6000

NFPA 704:

	0
2		0

그림문자(GHS)

2'-디옥시-5-플루오로시티딘 화학적 특성, 용도, 생산

개요
5-Fluoro-2-Deoxycytidine is an antimetabolite consisting of a fluorinated pyrimidine analog with potential antineoplastic activity. As a prodrug, 5-fluoro-2-deoxycytidine is converted by intracellular deaminases to the cytotoxic agent 5-Fluorouracil (5-FU). 5-FU is subsequently metabolized to active metabolites including 5-fluoro-2-deoxyuridine monophosphate (FdUMP) and 5-fluorouridine triphosphate (FUTP). FdUMP binds to and inhibits thymidylate synthase, thereby reducing the production of thymidine monophosphate, which leads to depletion of thymidine triphosphate. This inhibits DNA synthesis and cell division. FUTP competes with uridine triphosphate for incorporation into the RNA strand thus leading to an inhibition of RNA and protein synthesis. Other fluorouracil metabolites also get incorporated into both DNA and RNA, thereby further hampering cellular growth.
용도
5-fluoro-2'-deoxycytidine has been used in trials studying the treatment of Neoplasms, Lung Neoplasms, Breast Neoplasms, Head and Neck Neoplasms, and Urinary Bladder Neoplasms, among others.
일반 설명
Fine white powder.
공기와 물의 반응
2'-DEOXY-5-FLUOROCYTIDINE is probably light and air sensitive.
건강위험
ACUTE/CHRONIC HAZARDS: When heated to decomposition 2'-DEOXY-5-FLUOROCYTIDINE emits toxic fumes of fluoride ion and NOx.
화재위험
Flash point data for 2'-DEOXY-5-FLUOROCYTIDINE are not available. 2'-DEOXY-5-FLUOROCYTIDINE is probably combustible.
Pharmacology
5-Fluoro-2'-deoxycytidine (FdCyd), a fluoropyrimidine nucleoside analog, has a short (10-minute) half-life and is rapidly degraded in vivo by cytidine deaminase. However, coadministration with tetrahydrouridine (THU), an inhibitor of cytidine/deoxycytidine deaminase, has been shown to increase the AUC of the parent compound more than 4-fold. Increased FdCyd exposure allows it to be taken up intracellularly and converted to its triphosphate, which is incorporated into DNA and inhibits the action of the enzyme DNA methyltransferase (DNMT). Inhibition of DNMT, and in turn DNA methylation, can result in the re-expression of tumor suppressor genes.
Primary objective:
-Determine progression-free survival (PFS) and/or the response rate (CR + PR) of FdCyd administered 5 days per week for 2 weeks, in 28-day cycles, by intravenous infusion over 3 hours along with THU in patients with breast cancer, head and neck cancer, non-small cell lung cancer, and urothelial transitional cell carcinoma.
Exploratory objectives:
Evaluate whether treatment with FdCyd and THU alters DNA methylation patterns in tumor biopsy samples before and during treatment by LINE-1 analysis.
Evaluate the safety and tolerability of FdCyd (100 mg/m(2)) + THU (350 mg/m(2)) administered 5 days per week for 2 weeks, in 28-day cycles, by intravenous infusion over 3 hours.
Measure changes in the number of CTCs following treatment with FdCyd plus THU.
Clinical Use
A DNA methyltransferase inhibitor currently in clinical trials for breast cancer and other solid tumors. Like 5’-Azacytidine and decitabine, 2’-Deoxy-5-fluorocytidine is a pyrimidine analog that integrates into chromatin to inhibit DNA methylation. It blocks proliferation in colon cancer-derived HCT116 cells by activating DNA response pathways. It inhibits various strains of pathogenic avian influenza viruses in vitro and in vivo.

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