Vincristine
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Vincristine 속성
- 녹는점
- 211-216 ºC
- 알파
- D25 +17°; D25 +26.2° (ethylene chloride)
- 끓는 점
- 761.92°C (rough estimate)
- 밀도
- 1.1539 (rough estimate)
- 굴절률
- 1.6000 (estimate)
- 저장 조건
- Store at -20°C, protect from light
- 용해도
- Soluble in Chloroform,Dichloromethane,Ethyl Acetate,DMSO,Acetone,etc.
- 물리적 상태
- 가루
- 산도 계수 (pKa)
- 5.4(at 25℃)
- 안정성
- 안정적이지만 열에 민감할 수 있습니다. 강한 산화제와 호환되지 않습니다.
- CAS 데이터베이스
- 57-22-7
안전
유엔번호(UN No.) | 1544 | ||
---|---|---|---|
위험 등급 | 6.1(a) | ||
포장분류 | II | ||
유해 물질 데이터 | 57-22-7(Hazardous Substances Data) | ||
독성 | LD50 i.p. in mice: 5.2 mg/kg (Adamson) |
Vincristine C화학적 특성, 용도, 생산
개요
A complex dimeric alkaloid isolated from Vinca minor, this base has the structure given above based upon chemical and spectroscopic data. It resembles Vinblastine in its pharmacological action. Depending on the dosage, it causes either thrombocytosis with no effect upon the leucocytes, or thrombocytopenia accompanied by peucopenia in rats. Thrombocytosis persists even after prolonged treatment with drugs given in the correct dosage.화학적 성질
solid물리적 성질
Appearance: needlelike crystals were produced when recrystallized by methanol. The other properties of vincristine are similar to vinblastine.역사
Vinblastine and vincristine were extracted from vinca, and researchers found that they are the main ingredient of vinca which have antitumor activity. This is an accidental harvest by hard work and inspiration during scientific research process. It was firstly reported as an important discovery by Annals of the New York Academy of Sciences, and one report was published by Robert Noble and Charles Thomas Beer . They demonstrated that vinblastine can cause severe leukopenia. In 1963, vincristine (trade name, Oncovin) developed by Eli Lilly was approved by the US FDA, it provided a good choice for tumor chemotherapy program and gradually became the essential tumor chemotherapy drugs.At the early stages of the study, vinblastine and vincristine are directly extracted from the vinca, but the cost is high, and the extraction efficiency is low . Especially the specific chiral monomer compounds with biological activity are difficult to obtain. In the following years, the researchers used genetic engineering, biosynthesis, chemical synthesis, and other technical methods to explore and optimize the production process of vinblastine drugs. In particular, the rise of asymmetric synthesis provides a more economical choice for the synthesis of vinblastine compounds and increases productivity to more than 22% . At the same time, the pharmaceutical dosage forms were developed from the beginning as simple sulfate injection to liposomal preparations and nanoparticle preparations, which improve the efficacy, reduce adverse reactions, and play better antitumor effect.
용도
Antineoplastic[Note—Graphic formula same as for Vinblastine Sulfate, except that R is CHO].Indications
It was recorded in the Pharmacopoeia of the People’s Republic of China (2015), the British Pharmacopoeia (2017), the United States Pharmacopeia (40), the Japanese Pharmacopoeia (17th ed.), the European Pharmacopoeia (9th ed.), and The International Pharmacopoeia (5th ed.).Vincristine sulfate injection is used to treat leukemia, lymphadenoma, non-small cell lung cancer, nephroblastoma, and neuroblastoma in clinical practice generally, but the effect of vinblastine is better than vincristine in Hodgkin lymphoma treatment.
일반 설명
A white crystalline solid. Melting point 218°C. Used as an antineoplastic.건강위험
Highly toxic, may be fatal if inhaled, swallowed or absorbed through skin. Avoid any skin contact. Effects of contact or inhalation may be delayed. Fire may produce irritating, corrosive and/or toxic gases. Runoff from fire control or dilution water may be corrosive and/or toxic and cause pollution.화재위험
Flash point data for Vincristine are not available, but Vincristine is probably combustible.Pharmacology
Vinblastine drugs have a strong inhibitory effect on monozygotic leukemia, breast cancer, liver cancer, ovarian cancer, head and neck cancer, testicular cancer, solid sarcoma, and malignant melanin in a variety of spontaneous or transplanted lymphocytic leukemias. Although the structure of vinblastine and vincristine is very similar, there are some differences in pharmacological effects, and there is no crossresistance .The mechanism of vinblastine and vincristine is similar as cell cycle-specific antineoplastic agents. They all inhibit tubulin polymerization, interfere spindle microtubule formation, block the cell cycle in M phase, and then inhibit the proliferation of cancer cells . X-ray diffraction results showed that Vinblastine targets at the hydrophobic structure on tubulin, Vinblastine inserted into the trough as the wedge, blocking the polymerization of tubulin, making a spirochete structure of tubulin itself form, and loss of biological role . However, this antitumor effect can affect other rapid proliferation cells, and then small intestinal epithelial cells and bone marrow cells will be inhibited, which is one of the reasons of gastrointestinal side effects and bone marrow transplantation side effects. The effect of vincristine is better than vinblastine, and the dosage is lower, the probability and intensity of side effects are lower. Recently, it has been found that vinblastine and vincristine can also suppress growth of tumor cell by inhibiting the synthesis of RNA and protein.
Clinical Use
Vincristine is an important component of the curative combination chemotherapy for acute lymphoblastic leukemia, Hodgkin’s disease (the MOPP regimen), and non-Hodgkin’s lymphomas. It is also used in several regimens for pediatric solid tumors, including Wilms’ tumor, Ewing’s sarcoma, rhabdomyosarcoma, and neuroblastoma; in adult tumors of the breast, lung, and cervix; and in sarcomas. Its relative lack of myelosuppression makes it more attractive than vinblastine for use in combination with myelotoxic drugs.Vinblastine is especially useful in testicular carcinomas and is also active in Hodgkin’s disease, other types of lymphomas, breast cancer, and renal cell carcinoma.부작용
All vinca alkaloids are severe vesicants that can induce necrosis, cellulitis, and/or thrombophlebitis. Proper needle placement before administration should be assured to eliminate the risk of extravasation. Unlike the tissue damage caused by the vesicant action of nitrogen mustards and antibiotic antineoplastics, cold exacerbates tissue destruction. If extravasation occurs, apply heat for 1 hour fours time a day for 3 to 5 days, coupled with local hyaluronidase injections. Vinca alkaloids are all Category D teratogens and are fatal if administered by the intrathecal route.참고 문헌
Mokry et al., Experientia, 18, 564 (1962) Pharmacology: Chandorkar.,lnd. J. Physiol. Pharmacol., 17, 105 (1973)Vincristine 준비 용품 및 원자재
원자재
준비 용품
Vincristine 공급 업체
글로벌( 196)공급 업체
공급자 | 전화 | 이메일 | 국가 | 제품 수 | 이점 |
---|---|---|---|---|---|
Hebei Chuanghai Biotechnology Co,.LTD | +86-13131129325 |
sales1@chuanghaibio.com | China | 5882 | 58 |
Henan Tianfu Chemical Co.,Ltd. | +86-0371-55170693 +86-19937530512 |
info@tianfuchem.com | China | 21667 | 55 |
Nanjing Finetech Chemical Co., Ltd. | 025-85710122 17714198479 |
sales@fine-chemtech.com | CHINA | 885 | 55 |
Shanghai Zheyan Biotech Co., Ltd. | 18017610038 |
zheyansh@163.com | CHINA | 3620 | 58 |
career henan chemical co | +86-0371-86658258 +8613203830695 |
sales@coreychem.com | China | 29888 | 58 |
Chengdu Biopurify Phytochemicals Ltd. | +8618080483897 |
sales@biopurify.com | China | 3772 | 58 |
Nanjing Dolon Biotechnology Co.,Ltd. | 18905173768 |
sales@dolonchem.com | CHINA | 2972 | 58 |
Shaanxi Pioneer Biotech Co., Ltd . | +8613259417953 |
sales@pioneerbiotech.com | China | 3000 | 58 |
Hubei xin bonus chemical co. LTD | 86-13657291602 |
linda@hubeijusheng.com | CHINA | 22968 | 58 |
Chongqing Chemdad Co., Ltd | +86-023-6139-8061 +86-86-13650506873 |
sales@chemdad.com | China | 39916 | 58 |
Vincristine 관련 검색:
시클로스포린 A 에토포시드 멜팔란 빈크리스틴 황산염
VINBLASTINE
Vincamine
Verbena Oil
Vetivert oil
VERBENALIN
Podophyllotoxin
Docetaxel
Vinpocetine
N-Formyl Leurosine (Vincristine Impurity G),Vincristine Impurity G
[G-3H]VINCRISTINE SULFATE,VINCRISTINE SULFATE [3H(G)]
VINCRISTINE SULPHATE - REFERENCE SPECTRUM
4-Desacetyl Vincristine
Vincristine
VINCRISTINE SULFATE, [3H]- 1-10 CI(37-370 GBQ)/MMOL, MORPURE HPLC PURIFIED, DELIVERED >= 97% PURE WITH HPLC RADIOCHROMATOGRAM