Oxaliplatin
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Oxaliplatin 속성
- 알파
- +74.5-78.0 (D/20)(c=0.5,H2O)
- 저장 조건
- 2-8°C
- 용해도
- 물에 약간 용해되고, 메탄올에 매우 약간 용해되며, 무수 에탄올에는 거의 용해되지 않습니다.
- 물리적 상태
- 고체
- 물리적 상태
- 단단한 모양
- 색상
- 흰색에서 거의 흰색
- 수용성
- 가열 및/또는 초음파 처리를 통해 물에 용해됨
- Merck
- 14,6912
- 안정성
- 안정적인. 시원하게 보관하세요. 산화제와 호환되지 않습니다.
- InChI
- InChI=1/C6H12N2.C2H2O4.Pt/c7-5-3-1-2-4-6(5)8;3-1(4)2(5)6;/h5-8H,1-4H2;(H,3,4)(H,5,6);/q-2;;+4/p-2/t5-,6-;;/s3
- InChIKey
- ZROHGHOFXNOHSO-BNTLRKBRSA-L
- SMILES
- O=C1C([O-][Pt+2]2(N[C@]3([H])CCCC[C@@]3([H])N2)[O-]1)=O |&1:6,12,r|
- CAS 데이터베이스
- 61825-94-3
안전
- 위험 및 안전 성명
- 위험 및 사전주의 사항 (GHS)
위험품 표기 | Xn,Xi | ||
---|---|---|---|
위험 카페고리 넘버 | 36/37/38-40-42/43 | ||
안전지침서 | 26-36 | ||
유엔번호(UN No.) | 2811 | ||
WGK 독일 | 3 | ||
RTECS 번호 | TP2275850 | ||
위험 등급 | 6.1(a) | ||
포장분류 | II | ||
HS 번호 | 28439000 | ||
독성 | LD50 intraperitoneal in mouse: 19800ug/kg |
Oxaliplatin C화학적 특성, 용도, 생산
개요
Oxaliplatin is a second generation platinum drug prepared in three steps from either k2tCl4 or K2Ptl4. It has an antitumor spectrum similar to cisplatin, however, it is more effective against L1210 leukemia and cisplatin resistant L1210. It is also effective against B16 melanoma but has a dose limiting toxicity of peripheral sensory neuropathy that is reversible upon cessation of the drug. The (R,R)- enantiomer has greater activity than the (S,S)-isomer but this is tumor line dependent, e.g., there was no difference found for P-388 or Sarcoma 180. Clinical drug administration based on circadium timing showed it was better tolerated when given 16 h after the onset of light. Oxaliplatin binds to guanineN7 and can lead to bidentate chelation that results in the bending of DNA. This feature is recognized by high mobility group proteins (HMG) which impedes repair reactions and stops replication and transcription.화학적 성질
White Crystalline Solid용도
Oxaliplatin is a platinum-based antineoplastic agent that functions by forming DNA adducts specifically in cancer cells, preventing DNA replication and transcription which leads to cell death. Oxaliplatin has cytotoxic effects in a broad range of cell lines, including colon, ovarian, and lung cancer, with IC50 values ranging from 0.5-240, 0.12-19.8, and 2.6-6.1 μM, respectively. Through its general cytotoxic effects, oxaliplatin has anti-tumor activity against advanced colorectal cancer and is typically administered with fluorouracil and leucovorin in a combination known as FOLFOX.일반 설명
Oxaliplatin is available in 50- and 100-mg vials for IV administrationin the treatment of ovarian cancer, metastaticcolorectal cancer, and early stage colon cancer in combinationwith 5-fluorouracil/leucovorin. The activation of theagent occurs in low-chloride environments to give theaquated species, which subsequently reacts with DNA in amanner similar to cisplatin. The mechanisms of resistance aresimilar for the two agents; however, oxaliplatin is not recognizedby MMR enzymes and does not show cross-resistancewith cisplatin. The agent is widely distributed, highly proteinbound (85%–88%), and irreversibly binds to erythrocytes.Numerous metabolites have been identified many of whichare produced as a result of nonenzymatic processes and includechloro-, dichloro-, monoaquo-, and diaquo-species.The parent and metabolites are eliminated primarily in theurine with a long terminal elimination half-life of 240 hours.Neurotoxicity is dose limiting and normally presents as peripheralneuropathy, which may be exacerbated by exposureto low temperatures. The neurotoxicity is normally reversiblein contrast to that seen with cisplatin, which may be irreversible.Other adverse effects include nausea, vomiting, diarrhea,myelosuppression, and hypersensitivity reactions.Ototoxicity and renal toxicity occur only rarely in contrast tocisplatin.생물학적 활성
Oxaliplatin is a platinum-containing DNA-crosslinking agent. It induces the formation of DNA inter- and intrastrand crosslinks and DNA-protein crosslinks, inhibits DNA and RNA synthesis, and induces apoptosis in cancer cells. Oxaliplatin is cytotoxic to cisplatin-sensitive A2780(1A9) and KB-3-1 cells and cisplatin-resistant A2780-E(80) and KB-CP20 cells (IC50s = 0.12, 0.39, 4.7, and 2.7 μM, respectively). It reduces tumor growth in an HCCLM3 mouse xenograft model when administered at doses of 5 or 10 mg/kg once per week. Formulations containing oxaliplatin have been used in the treatment of advanced colorectal cancer and as an adjuvant in stage III colon cancer.부작용
Hematopoietec system: Oxaliplatin has a certain blood toxicity. When used alone, it can cause the following adverse effects: anemia, leukopenia, neutropenia, thrombocytopenia, sometimes reaching grade 3 or 4. Increases hematologic toxicities such as neutropenia and thrombocytopenia when combined with 5-fluorouracil.Digestive system: can cause nausea, vomiting, and diarrhea when used alone. These symptoms can sometimes be very serious. These side effects are significantly exacerbated when used in combination with 5-fluorouacil. Use of prophylactic and/or therapeutic antiemetic drugs is recommended.
Nervous system: Peripheral sensory neuropathy characterized by peripheral neuritis. Sometimes associated with convulsions and sensory disturbances in the mouth, upper respiratory tract, and upper GI tract.
Safety Profile
A poison by intraperitoneal route. When heated to decomposition it emits toxic vapors of NOx and Pt.Synthesis
An aqueous solution of 5 g of (1R,2R)-(-)-1,2-DiaMinocyclohexane and 18 g of K2(PtCl4) was reacted for 12 h at room temperature to give 12 g of compound (I). 6: 8 g of silver nitrate was added to an aqueous solution of 3 g of compound (I) and stirred for 2-3 h away from light, then 4.8 g of dipotassium oxalate was added and the reaction was carried out for 8 h at room temperature to give oxaliplatin.Mode of action
Oxaliplatin, a platinum derivative, is an alkylating agent. Acts on DNA through production of alkylating conjugates, inhibiting its synthesis and reproduction by forming interchain and intrachain cross-links. Following intracellular hydrolysis, the platinum compound binds to DNA forming cross-links which inhibit DNA replication and transcription, resulting in cell death.Oxaliplatin 준비 용품 및 원자재
원자재
질산 은
Dipotassium rabdosiin Rabdosiin
1,2-사이클로헥산디아민
1-Butanaminium, N,N,N-tributyl-, ethanedioate (2:1)
백금,디클로로(1,2-시클로헥산디아민-N,N')-,[sp-4-2-(1R-trans)]-
(1R,2R)-(-)-1,2-Diaminocyclohexane
칼륨 옥살산염 모노수화물
옥살산 디암모늄
플라티오누스 칼륨 염화물
준비 용품
Oxaliplatin 공급 업체
글로벌( 564)공급 업체
공급자 | 전화 | 이메일 | 국가 | 제품 수 | 이점 |
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SHANDONG BOYUAN PHARMACEUTICAL CO., LTD. | +86-0531-69954981 +8615666777973 |
dwyane.wang@boyuanpharm.com | China | 211 | 58 |
Hebei Yanxi Chemical Co., Ltd. | +86-17531190177; +8617531190177 |
peter@yan-xi.com | China | 5873 | 58 |
Sinoway Industrial co., ltd. | 0592-5800732; +8613806035118 |
xie@china-sinoway.com | China | 990 | 58 |
Hebei Zhuanglai Chemical Trading Co.,Ltd | +8613343047651 |
admin@zlchemi.com | China | 3002 | 58 |
Hebei Shengyang Water Conservancy Engineering Co., Ltd. | +8615373025980 |
clara@hbshengyang.com | China | 873 | 58 |
Henan Tianfu Chemical Co.,Ltd. | +86-0371-55170693 +86-19937530512 |
info@tianfuchem.com | China | 21668 | 55 |
Hangzhou FandaChem Co.,Ltd. | 008657128800458; +8615858145714 |
fandachem@gmail.com | China | 9332 | 55 |
Nanjing Finetech Chemical Co., Ltd. | 025-85710122 17714198479 |
sales@fine-chemtech.com | CHINA | 885 | 55 |
ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 |
ivan@atkchemical.com | China | 32760 | 60 |
Jiangsu Yew Pharmaceutical Co., Ltd. | +86-510-66865338 +86-189-2133-5032 @ |
junwenjiang@live.cn | CHINA | 30 | 60 |