클라드리빈

클라드리빈
클라드리빈 구조식 이미지
카스 번호:
4291-63-8
한글명:
클라드리빈
동의어(한글):
클라드리빈
상품명:
Cladribine
동의어(영문):
CDA;Leustat;(2R,3S,5R)-5-(6-aMino-2-chloro-9H-purin-9-yl)-2-(hydroxyMethyl)tetrahydrofuran-3-ol;2CDA;CldAdo;2-Cl-dA;Jk 6251;CS-1392;rwj26251;Leustati
CBNumber:
CB4222723
분자식:
C10H12ClN5O3
포뮬러 무게:
285.69
MOL 파일:
4291-63-8.mol
MSDS 파일:
SDS

클라드리빈 속성

녹는점
181-185 °C(lit.)
알파
D25 -18.8° (c = 1 in DMF)
끓는 점
547.6±60.0 °C(Predicted)
밀도
2.03±0.1 g/cm3(Predicted)
저장 조건
-20°C
용해도
물에 약간 용해되고, 디메틸 설폭사이드에 용해되고, 메탄올에 약간 용해되고, 아세토니트릴에는 거의 용해되지 않습니다. 다형성(5.9)을 보여줍니다.
산도 계수 (pKa)
13.75±0.60(Predicted)
물리적 상태
흰색 고체
색상
흰색에서 연한 노란색
최대 파장(λmax)
265nm(EtOH aq.)(lit.)
Merck
14,2337
안정성
냉동고에 보관
InChIKey
PTOAARAWEBMLNO-HSUXUTPPSA-N
CAS 데이터베이스
4291-63-8(CAS DataBase Reference)
안전
  • 위험 및 안전 성명
  • 위험 및 사전주의 사항 (GHS)
위험품 표기 T
위험 카페고리 넘버 36/37/38-23/24/25
안전지침서 26-37/39-45-36-22
유엔번호(UN No.) UN 2811 6.1 / PGIII
WGK 독일 3
RTECS 번호 AU7357560
HS 번호 29349990
유해 물질 데이터 4291-63-8(Hazardous Substances Data)
독성 LD50 intraperitoneal in mouse: 150mg/kg
그림문자(GHS): GHS hazard pictogramsGHS hazard pictograms
신호 어: Danger
유해·위험 문구:
암호 유해·위험 문구 위험 등급 범주 신호 어 그림 문자 P- 코드
H301 삼키면 유독함 급성 독성 물질 - 경구 구분 3 위험 GHS hazard pictograms P264, P270, P301+P310, P321, P330,P405, P501
H341 유전적인 결함을 일으킬 것으로 의심됨 (노출되어도 생식세포 유전독성을 일으키지 않는다는 결정적인 증거가 있는 노출경로가 있다면 노출경로 기재) 생식세포 변이원성 물질 구분 2 경고 P201,P202, P281, P308+P313, P405,P501
H372 장기간 또는 반복 노출되면 장기(또는, 영향을 받은 알려진 모든 장기를 명시)에 손상을 일으킴 특정 표적장기 독성 - 반복 노출 구분 1 위험 GHS hazard pictograms P260, P264, P270, P314, P501
예방조치문구:
P201 사용 전 취급 설명서를 확보하시오.
P202 모든 안전 조치 문구를 읽고 이해하기 전에는 취급하지 마시오.
P260 분진·흄·가스·미스트·증기·...·스프레이를 흡입하지 마시오.
P264 취급 후에는 손을 철저히 씻으시오.
P264 취급 후에는 손을 철저히 씻으시오.
P270 이 제품을 사용할 때에는 먹거나, 마시거나 흡연하지 마시오.
P301+P310 삼켰다면 즉시 의료기관(의사)의 진찰을 받으시오.
NFPA 704
0
4 0

클라드리빈 MSDS


2-Chloro-2'-deoxyadenosine

클라드리빈 C화학적 특성, 용도, 생산

개요

Cladribine, an adenosine deaminase inhibitor, was introduced in the United States as a single intravenous treatment for hairy cell leukemia. The incorporation of a chlorine atom at the 2-position of deoxyadenosine renders cladribine more resistant to enzymatic attack by adenosine deaminase, resulting in a more prolonged cytotoxic effect. Cladribine efficiently crosses lymphocyte and monocyte cell membranes and is metabolized in cells to the biologically active triphosphate, which inhibits DNA synthesis. While most antineoplastic drugs are active primarily against dividing cells, cladribine destroys both resting and proliferating cells. Its potential uses in the treatment of autoimmune hemolytic anemia, multiple sclerosis, chronic lymphocytic leukemia and various lymphomas have also been evaluated.

화학적 성질

White Crystalline Solid

용도

It is a substituted purine nucleoside with antileukemic activity

Indications

Cladribine (Leustatin) is a synthetic purine nucleoside that is converted to an active cytotoxic metabolite by the enzyme deoxycytidine kinase. Like the other purine antimetabolites, it is relatively selective for both normal and malignant lymphoid cells and kills resting as well as dividing cells by mechanisms that are not completely understood.
The drug is highly active against hairy cell leukemia, producing complete remissions in more than 60% of patients treated with a single 7-day course. Activity has also been noted in other low-grade lymphoid malignancies. The major side effect is myelosuppression.

정의

ChEBI: 2'-Deoxyadenosine in which the hydrogen at position 2 on the purine ring has been substituted by chlorine. It inhibits the synthesis and repair of DNA, particularly in lymphocytes and monocytes, and is used as an antimetabolite antineoplastic drug for the treatment of lymphoid malignancies including hairy-cell leukaemia and chronic lymphocytic leukaemia.

일반 설명

The drug is available in a 10-mg or 10-mL single-use vialfor IV use. Cladribine is used for chronic lymphocyticleukemia, hairy cell leukemia, and non-Hodgkin’s lymphoma.The mechanism of action of this purine deoxyadenosineanalog involves incorporation into DNA resultingin inhibition of DNA chain extension and inhibitionof DNA synthesis and function. This incorporation intoDNA occurs via the triphosphate metabolite active species.The 2-chloro group on the adenine ring produces resistanceto breakdown by adenosine deaminase. Resistance to the anticancereffects can occur because of decreased expressionof the activating enzyme or overexpression of the catabolicenzymes. Oral bioavailability is variable and averages about50%. The drug crosses the blood-brain barrier; however,CSF concentrations reach only 25% of those in plasma. Thedrug is selectively activated inside the cell, and intracellularconcentrations of phosphorylated metabolites exceed thosein plasma. Toxicities include myelosuppression, neutropenia,immunosuppression, fever, nausea, and vomiting.

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