탈리도마이드

탈리도마이드
탈리도마이드 구조식 이미지
카스 번호:
50-35-1
한글명:
탈리도마이드
동의어(한글):
탈리도마이드;탈리도마이드및그염류
상품명:
Thalidomide
동의어(영문):
2-(2,6-Dioxopiperidin-3-yl)isoindoline-1,3-dione;Neo;k17;Celgene;Contergan;α-Phthalimidoglutarimide;2-(2,6-dioxopiperidin-3-yl)-1H-isoindole-1,3(2H)-dione;K 17;E-217;Sedin
CBNumber:
CB0311476
분자식:
C13H10N2O4
포뮬러 무게:
258.23
MOL 파일:
50-35-1.mol
MSDS 파일:
SDS

탈리도마이드 속성

녹는점
269-271°C
끓는 점
401.48°C (rough estimate)
밀도
1.2944 (rough estimate)
굴절률
1.5300 (estimate)
저장 조건
Keep in dark place,Sealed in dry,Room Temperature
용해도
45%(w/v) 수성 2-히드록시프로필-β-시클로덱스트린: 0.6mg/mL
물리적 상태
흰색 고체
산도 계수 (pKa)
10.70±0.40(Predicted)
색상
하얀색
수용성
22&C에서 <0.1g/100mL
최대 파장(λmax)
300nm(lit.)
Merck
14,9255
안정성
안정적인. 타기 쉬운. 강한 산화제와 호환되지 않습니다.
InChIKey
UEJJHQNACJXSKW-UHFFFAOYSA-N
CAS 데이터베이스
50-35-1(CAS DataBase Reference)
NIST
Phthalimide, n-(2,6-dioxo-3-piperidyl)-(50-35-1)
EPA
Thalidomide (50-35-1)
안전
  • 위험 및 안전 성명
  • 위험 및 사전주의 사항 (GHS)
위험품 표기 T
위험 카페고리 넘버 46-61-21-25-62-22
안전지침서 53-22-26-36/37/39-45
유엔번호(UN No.) UN 2811 6.1/PG 3
WGK 독일 3
RTECS 번호 TI4375000
위험 등급 6.1(b)
포장분류 III
HS 번호 29337900
유해 물질 데이터 50-35-1(Hazardous Substances Data)
독성 LD50 oral in mouse: 2gm/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
H312 피부와 접촉하면 유해함 급성 독성 물질 - 경피 구분 4 경고 GHS hazard pictograms P280,P302+P352, P312, P322, P363,P501
예방조치문구:
P201 사용 전 취급 설명서를 확보하시오.
P202 모든 안전 조치 문구를 읽고 이해하기 전에는 취급하지 마시오.
P264 취급 후에는 손을 철저히 씻으시오.
P264 취급 후에는 손을 철저히 씻으시오.
P280 보호장갑/보호의/보안경/안면보호구를 착용하시오.
P301+P310 삼켰다면 즉시 의료기관(의사)의 진찰을 받으시오.
NFPA 704
0
2 0

탈리도마이드 MSDS


2-(2,6-Dioxo-3-piperidinyl)-1H-isoindole-1,3(2H)-dione

탈리도마이드 C화학적 특성, 용도, 생산

화학적 성질

White Powder

용도

Inhibits FGF-induced angiogenesis. Inhibits replication of human immunodeficiency virus type 1. Teratogenic sedative. There is now a growing clinical interest in Thalidomide, and it is introduced as an immunomodulatory agent used primarily in combination with dexamethasone to treat multiple myeloma.

Indications

Thalidomide (Thalomid) is a derivative of glutamic acid that is chemically related to glutethimide. It exerts a number of biological effects as an immunosuppressive, antiinflammatory, and antiangiogenic agent, yet its mechanisms of action have not been fully elucidated. Thalidomide potently inhibits production of tumor necrosis factor (TNF) and interleukin (IL) 12, and its effect on these and other cytokines may account for some of its clinical effects.

정의

ChEBI: A dicarboximide that is isoindole-1,3(2H)-dione in which the hydrogen attached to the nitrogen is substituted by a 2,6-dioxopiperidin-3-yl group.

World Health Organization (WHO)

Notwithstanding the highly potent teratogenic action of thalidomide, this drug retains a place in the treatment of reactional lepromatous leprosy and several serious dermatological conditions refractory to other treatment. In many countries, the competent authorities have granted exemption from licensing requirements to enable doctors to obtain limited supplies of thalidomide under strictly controlled circumstances for use in named patients. Arrangements have also been made by some national drug regulatory authorities for thalidomide to be used in institutions concerned with the treatment of leprosy.

일반 설명

Needles or white powder.

공기와 물의 반응

Insoluble in water.

반응 프로필

Organic amides/imides, such as Thalidomide, react with azo and diazo compounds to generate toxic gases. Flammable gases are formed by the reaction of organic amides/imides with strong reducing agents. Amides are very weak bases (weaker than water). Imides are less basic yet and in fact react with strong bases to form salts. That is, they can react as acids. Mixing amides with dehydrating agents such as P2O5 or SOCl2 generates the corresponding nitrile. The combustion of these compounds generates mixed oxides of nitrogen (NOx).

건강위험

Thalidomide is a strong teratogen. Exposureto this compound during the first trimesterof pregnancy resulted in deformities inbabies. Infants born suffered from ameliaor phocomelia, the absence or severe shortening of limbs. Administration of thalidomide in experimental animals caused fetaldeaths, postimplantation mortality, and specific developmental abnormalities in theeyes, ear, central nervous system, musculoskeletal system, and cardiovascular system. Several thousand children were affected.The drug has been withdrawn from themarket.
Thalidomide is usually administeredorally. Its toxicity is dose dependent. Someother effects are drowsiness, constipation andrash and nerve damage in the arms and legs.
Interest in thalidomide resurged in recentyears because of its antitumor activity in thetreatment of multiple myeloma (Oxberry andJohnson 2006). The compound is an inhibitorof angiogenesis, that is, it prevents formationof new blood vessels in tumors. Also, it hasbeen found to be effective in treating AIDS-related Kaposis sarcoma.

화재위험

Flash point data for Thalidomide are not available; however, Thalidomide is probably combustible.

생물학적 활성

Teratogen, sedative-hypnotic with inherent anti-inflammatory properties. A selective inhibitor of tumor necrosis factor α (TNF- α ) synthesis.

Mechanism of action

Its absorption from the gastrointestinal tract is slow, with peak plasma levels being reached after 3 to 6 hours. It appears to undergo nonenzymatic hydrolysis in the plasma to a large number of metabolites.The elimination half-life is approximately 9 hours.

Clinical Use

Thalidomide is approved for use in the United States for the treatment of cutaneous manifestations of erythema nodosum leprosum, a potentially lifethreatening systemic vasculitis that occurs in some patients with leprosy.Although not approved for other indications, thalidomide has also been shown to be very effective in the management of Beh?et’s disease, HIVrelated mucosal ulceration (aphthosis), and select cases of lupus erythematosus.

부작용

Thalidomide is a highly teratogenic drug, characteristically causing phocomelia (aplasia of the midportions of the limbs). Even a single dose may cause fetal malformation. Thalidomide should be prescribed to women of childbearing potential only when no acceptable alternative exists. Because it is not known whether thalidomide is present in the ejaculate of males receiving the drug, male patients must use a latex condom when engaging in sexual activity with women of childbearing potential.
Other side effects of thalidomide may include sedation (in fact, thalidomide was originally marketed in Europe as a sleeping aid), constipation, and peripheral neuropathy, which may be permanent.

Safety Profile

Poison by ingestion. Moderately toxic by skin contact and intraperitoneal routes. Human teratogenic effects by ingestion: developmental abnormalities of the musculoskeletal and cardiovascular systems. Experimental reproductive effects. Questionable carcinogen with experimental tumorigenic and teratogenic data. Human mutation data reported. It was commonly used as a prescription drug in Europe in the late 1950s and early 1960s. Its use was dscontinued because it was lscovered to cause serious congenital abnormalities in the fetus, notably amelia and phocomelia (absence or deformity of the limbs, including hands and feet) when taken by a woman during early pregnancy. When heated to decomposition it emits toxic fumes of NOx. Used as a sedative and hypnotic.

탈리도마이드 준비 용품 및 원자재

원자재

준비 용품


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