Valrubicin

Valrubicin 구조식 이미지
카스 번호:
56124-62-0
상품명:
Valrubicin
동의어(영문):
ad32;CS-703;Valstar;Valtaxin;VALRUBICIN;nsc-246131;Aids004409;Aids-004409;antibioticad32;Valrubicin(R&D)
CBNumber:
CB9425095
분자식:
C34H36F3NO13
포뮬러 무게:
723.64
MOL 파일:
56124-62-0.mol
MSDS 파일:
SDS

Valrubicin 속성

녹는점
116-117 °C
끓는 점
135-136 C
밀도
1.3473 (estimate)
저장 조건
2-8°C
용해도
DMSO(약간 용해됨), 메탄올(약간 용해됨)
물리적 상태
고체
물리적 상태
단단한 모양
산도 계수 (pKa)
7.34±0.60(Predicted)
색상
빨간색
수용성
불용성
InChIKey
ZOCKGBMQLCSHFP-XGMQQLFPNA-N
SMILES
C12=C(O)C3=C(C(=O)C4C=CC=C(OC)C=4C3=O)C(O)=C1C[C@@](O)(C(=O)COC(=O)CCCC)C[C@@H]2O[C@@H]1O[C@H]([C@@H](O)[C@@H](NC(=O)C(F)(F)F)C1)C |&1:21,34,36,38,39,41,r|
안전
  • 위험 및 안전 성명
  • 위험 및 사전주의 사항 (GHS)
위험품 표기 Xi
위험 카페고리 넘버 36/37/38
안전지침서 26-37/39
HS 번호 2941906000
유해 물질 데이터 56124-62-0(Hazardous Substances Data)
독성 dnd-hmn:lym 3 mg/L CJBIAE 58,720,80
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
H312 피부와 접촉하면 유해함 급성 독성 물질 - 경피 구분 4 경고 GHS hazard pictograms P280,P302+P352, P312, P322, P363,P501
H332 흡입하면 유해함 급성 독성 물질 흡입 구분 4 경고 GHS hazard pictograms P261, P271, P304+P340, P312
H340 유전적인 결함을 일으킬 수 있음 (노출되어도 생식세포 유전독성을 일으키지 않는다는 결정적인 증거가 있는 노출경로가 있다면 노출경로 기재) 생식세포 변이원성 물질 구분 1A, 1B 위험 GHS hazard pictograms
H351 암을 일으킬 것으로 의심됨 (노출되어도 암을 일으키지 않는다는 결정적인 증거가 있는 노출경로가 있다면 노출경로 기재) 발암성 물질 구분 2 경고 P201, P202, P281, P308+P313, P405,P501
H360 태아 또는 생식능력에 손상을 일으킬 수 있음 생식독성 물질 구분 1A, 1B 위험 GHS hazard pictograms
예방조치문구:
P201 사용 전 취급 설명서를 확보하시오.
P202 모든 안전 조치 문구를 읽고 이해하기 전에는 취급하지 마시오.
P261 분진·흄·가스·미스트·증기·...·스프레이의 흡입을 피하시오.
P264 취급 후에는 손을 철저히 씻으시오.
P264 취급 후에는 손을 철저히 씻으시오.
P270 이 제품을 사용할 때에는 먹거나, 마시거나 흡연하지 마시오.
P271 옥외 또는 환기가 잘 되는 곳에서만 취급하시오.
P280 보호장갑/보호의/보안경/안면보호구를 착용하시오.
P281 요구되는 개인 보호구를 착용하시오
P301+P310 삼켰다면 즉시 의료기관(의사)의 진찰을 받으시오.
P302+P352 피부에 묻으면 다량의 물로 씻으시오.
P304+P340 흡입하면 신선한 공기가 있는 곳으로 옮기고 호흡하기 쉬운 자세로 안정을 취하시오.
P308+P313 노출 또는 접촉이 우려되면 의학적인 조치· 조언를 구하시오.
P312 불편함을 느끼면 의료기관(의사)의 진찰을 받으시오.
P321 (…) 처치를 하시오.
P322 특정 조치(라벨의 … 참조)
P330 입을 씻어내시오.
P363 다시 사용전 오염된 의류는 세척하시오.
P405 밀봉하여 저장하시오.
P501 ...에 내용물 / 용기를 폐기 하시오.
NFPA 704
0
3 0

Valrubicin C화학적 특성, 용도, 생산

개요

Valrubicin was launched as a new 'chemotherapeutic agent for the treatment of bladder cancer, particularly in patients with BCG-refractory carcinoma in situ (CIS) of the bladder for whom immediate cystectomy is unacceptable. It belongs to the class of anthracyclines, the widest used in human cancers, and is a N-trifluoroacetyl 14-valerate derivative of doxorubicin.Valrubicin can be obtained in 3 steps from daunomycin by N-trifluoroacetylation of the sugar moiety then iodination of the 2-acetyl group and introduction of a valerate residue. A proposed mechanism involved in the cytotoxicity of Valrubicin coud be the blockade of SV40 large T antigen helicase; this cellular enzyme is involved in the formation of a ternary complex with DNA to maintain the topographic structure of DNA during transcription. In patients with CIS of bladder refractory to front line and second line therapies, intravesical instillation of Valrubicin resulted in a complete response with a significant rate and allowed a delay in cystectomy. Systemic absorption was minimal and accordingly produced a lower incidence of cardiotoxicity compared with doxorubicin.

화학적 성질

Red Solid

용도

Chemotherapy drug used to treat cancer of the bladder.

일반 설명

Valrubicin is available in 200-mg vials for intravesicular administrationin the treatment of bladder cancer (orphan drugstatus). The increased lipophilicity associated with the valericacid ester and trifluoro acetate functionalities increasestissue penetration and remains intact because, in large measure,of the lack of exposure to hydrolyzing enzymes causedby direct delivery into the bladder followed by voiding ofthe instilled solution. This local action also minimizes cardiotoxicityand other adverse effects seen with other anthracyclines.The major adverse effects that are seen are bladderirritation and reddening of the urine.

Mechanism of action

Valrubicin is an anthracycline that affects a variety of interrelated biological functions, most of which involve nucleic acid metabolism. In cells, it inhibits the incorporation of nucleosides into nucleic acids, causes chromosomal damage, and arrests the cell cycle in G2. Although valrubicin does not bind strongly to DNA, valrubicin metabolites interfere with the normal DNA breaking-resealing action of DNA topoisomerase II.

Clinical Use

Valrubicin currently has orphan drug status in the treatment of bacille Calmette-Guérin (BCG)–refractory bladder cancer (the total patient population is ~1,000 individuals) and is used with patients for whom surgical intervention would result in high morbidity or death.

부작용

The most commonly reported adverse reactions are abdominal pain, urinary tract infection, hematuria, and dysuria. Systemic exposure to the drug and its metabolites would, of course, be greater in patients whose bladder wall integrity has been compromised by disease, and these patients should not receive valrubicin.

Safety Profile

Poison by intraperitoneal route.Human mutation data reported. When heated todecomposition it emits toxic fumes of Fí and NOx.

신진 대사

It is administered directly into the bladder through a catheter (intravesically). The lipophilic drug is water insoluble, but it dissolves in an aqueous vehicle that includes polyoxyethylene glycol and ethanol. The patient retains the drug in the bladder for 2 hours, then voids the solution in the normal fashion. Valrubicin is active as administered, and despite the fact that hydrolysis of the ester and trifluoroacetamide can be envisioned, it is excreted essentially unchanged. Less than 1% of an administered dose is absorbed systemically, so there is essentially no exposure to metabolizing enzymes. The reduced C13-alcoholic metabolite does not form to any appreciable extent during the 2-hour treatment period. Therapy is considered to be almost exclusively local, and there is little risk for cardiac toxicity, bone marrow suppression, drug–drug interactions, or other side effects.

Valrubicin 준비 용품 및 원자재

원자재

준비 용품


Valrubicin 공급 업체

글로벌( 187)공급 업체
공급자 전화 이메일 국가 제품 수 이점
R&D Scientific Inc.
+12266000236
sales@rdscientific.com Canada 1012 58
career henan chemical co
+86-0371-86658258
sales@coreychem.com China 29919 58
Hubei Jusheng Technology Co.,Ltd.
18871490254
linda@hubeijusheng.com CHINA 28180 58
Xiamen AmoyChem Co., Ltd
+86-592-6051114 +8618959220845
sales@amoychem.com China 6387 58
HubeiwidelychemicaltechnologyCo.,Ltd
18627774460
faith@widelychemical.com CHINA 742 58
Hubei xin bonus chemical co. LTD
86-13657291602
linda@hubeijusheng.com CHINA 22968 58
BOC Sciences
+1-631-485-4226
inquiry@bocsci.com United States 19553 58
Beijing Yibai Biotechnology Co., Ltd
0086-182-6772-3597
sales04@yibaibiotech.com CHINA 419 58
Chongqing Chemdad Co., Ltd
+86-023-61398051 +8613650506873
sales@chemdad.com China 39916 58
CONIER CHEM AND PHARMA LIMITED
+8618523575427
sales@conier.com China 47464 58

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