타미바로텐
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타미바로텐 속성
- 녹는점
- 231-232°C
- 끓는 점
- 449.6±45.0 °C(Predicted)
- 밀도
- 1.154±0.06 g/cm3(Predicted)
- RTECS 번호
- DH6940000
- 저장 조건
- room temp
- 용해도
- DMSO에서 50mM까지 용해됨
- 물리적 상태
- 가루
- 산도 계수 (pKa)
- 3.83±0.10(Predicted)
- 색상
- 흰색에서 황백색까지
안전
WGK 독일 | 3 |
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타미바로텐 C화학적 특성, 용도, 생산
개요
Tamibarotene, a selective agonist of the retinoic acid receptor, was launched in Japan as an oral treatment for relapsed or refractory acute promyelocytic leukemia (APL). APL is a form of acute myeloid leukemia (AML) characterized by a deficiency in mature blood cells and an excess of immature cells called promyelocytes in the bone marrow and peripheral blood. The current standard of care for APL includes treatment with all-trans-retinoic acid (ATRA), either alone or in combination with chemotherapy. ATRA is a high affinity ligand for two types of nuclear receptors, retinoic acid receptor (RAR) and retinoid X receptor (RXR), each of which has three subtypes (-α, -β, and -γ). Activation of RARα by ATRA causes promyelocytes to differentiate and mature, thereby inhibiting their proliferation and inducing disease remission. Although ATRA is one of the most clinically successful retinoids, its usage is hampered by the high rate of adverse effects, instability, and the appearance of ATRA-resistant leukemia cells.Adverse events included retinoic acid syndrome, hyperleukocytosis, xerosis, cheilitis, hypertriglyceridemia, and hypercholesterolemia; however, these side effects were generally milder than with ATRA, which all patients had received previously. Examination of human samples taken from Phase II and III clinical trials revealed that fecal excretion was the major elimination route, and the metabolism of tamibarotene occurred primarily through hydroxylation and taurine conjugation. In vitro, the plasma protein binding of tamibarotene is shown to be >98% in rats, dogs, and humans. Tamibarotene is synthesized from 5,5,8,8-tetramethyl-5,6,7, 8-tetrahydronaphthalene in a four-step sequence consisting of regioselective nitration in the 2-position, reduction of the nitro group by hydrogenation to produce the corresponding aniline derivative, acylation of the aniline intermediate with 4-(carbomethoxy)benzoyl chloride, and hydrolysis of the methyl ester.화학적 성질
Crystalline Solid용도
Tamibarotene, a retinoic acid receptor-α(RARα) agonist, was approved for the treatment of relapsed or refractory acute promyelocytic leukemia (APL) in Japan on June, 2005 and is currently marketed by Nippon Shinyaku Co. This novel drug has shown high remission rate among patients who have recurrent disease after all trans retinoic acid therapy.정의
ChEBI: A dicarboxylic acid monoamide resulting from the condensation of one of the carboxy groups of terephthalic acid with the amino group of 5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-amine.생물학적 활성
Retinoic acid receptor α (RAR α ) agonist that induces differentiation (ED 50 = 0.79 nM) and apoptosis of HL-60 cells in vitro . Exhibits antiproliferative effects against a variety of human tumor cells lines (mean values of 35, 40 and 60% growth inhibition at 0.1, 1 and 10 μ M respectively) and displays anticancer activity against acute promyelocytic leukemia in vivo .타미바로텐 준비 용품 및 원자재
원자재
준비 용품
타미바로텐 공급 업체
글로벌( 202)공급 업체
공급자 | 전화 | 이메일 | 국가 | 제품 수 | 이점 |
---|---|---|---|---|---|
Henan Tianfu Chemical Co.,Ltd. | +86-0371-55170693 +86-19937530512 |
info@tianfuchem.com | China | 21667 | 55 |
ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 |
ivan@atkchemical.com | China | 32836 | 60 |
career henan chemical co | +86-0371-86658258 +8613203830695 |
sales@coreychem.com | China | 29888 | 58 |
BOC Sciences | +1-631-485-4226 |
inquiry@bocsci.com | United States | 19553 | 58 |
Chongqing Chemdad Co., Ltd | +86-023-6139-8061 +86-86-13650506873 |
sales@chemdad.com | China | 39916 | 58 |
Shanghai Standard Technology Co., Ltd. | 18502101150 |
ft-sales@nature-standard.com | CHINA | 1923 | 58 |
Alchem Pharmtech,Inc. | 8485655694 |
sales@alchempharmtech.com | United States | 63711 | 58 |
TopScience Biochemical | 00852-68527855 |
info@itopbiochem.com | China Hong Kong | 902 | 58 |
career henan chemical co | +86-0371-86658258 +8613203830695 |
factory@coreychem.com | China | 29823 | 58 |
Shaanxi Dideu Medichem Co. Ltd | +86-29-87569265 +86-15319487004 |
1015@dideu.com | China | 2132 | 58 |
타미바로텐 관련 검색:
엽산 4-아미노벤조산 글리신 아세트산 안트라닐산
Lenalidomide
Temozolomide
Pyrantel pamoate
Homoharringtonine
Vorinostat
4-Chlorocarbonylbenzoic acid,methyl ester (Tamibarotene)
2-NAPHTHALENAMINE, 5,6,7,8-TETRAHYDRO-
N-(5,5,8,8-Tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)acetamide (Tamibarotene)
4-Ethyl-3-(1-methylethyl)benzenamine
Tamibarotene
5,6,7,8-TETRAHYDRONAPHTHALENE-2-YL-ACETAMIDE
CHEMBRDG-BB 4022344
phosphoric acid