Vincristine
(Synonyms: 长春新碱,Leurocristine; NSC-67574; 22-Oxovincaleukoblastine) 目录号 : GC38410
An antimitotic inhibitor of tubulin polymerization
Cas No.:57-22-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Vincristine is an antimitotic vinca alkaloid, isolated from the plant V. rosea. It irreversibly blocks mitosis by binding to tubulin (Ki = 85 nM) and inhibiting tubulin polymerization.1,2 Vincristine is exported from cells via the ATP-
1.Jordan, M.A., Himes, R.H., and Wilson, L.Comparison of the effects of vinblastine, vincristine, vindesine, and vinepidine on microtubule dynamics and cell proliferation in vitroCancer Res.45(6)2741-2747(1985) 2.Towle, M.J., Salvato, K.A., Wels, B.F., et al.Eribulin induces irreversible mitotic blockade: Implications of cell-based pharmacodynamics for in vivo efficacy under intermittent dosing conditionsCancer Res.71(2)496-505(2011) 3.van Tellingen, O., Buckle, T., Jonker, J.W., et al.P-glycoprotein and Mrp1 collectively protect the bone marrow from vincristine-induced toxicity in vivoBr. J. Cancer89(9)1776-1782(2003) 4.Chan, H.S.L., Haddad, G., Thorner, P.S., et al.P-glycoprotein expression as a predictor of the outcome of therapy for neuroblastomaNew Engl. J. Med.325(23)1608-1614(1991)
| Cas No. | 57-22-7 | SDF | |
| 别名 | 长春新碱,Leurocristine; NSC-67574; 22-Oxovincaleukoblastine | ||
| Canonical SMILES | CC[C@@]1(C=CCN2CC3)[C@@]2([H])[C@@]3(C4=CC([C@](C5=C6C7=CC=CC=C7N5)(C[C@](C[C@](CC)(O)C8)([H])C[N@@]8CC6)C(OC)=O)=C(OC)C=C4N9C=O)[C@]9([H])[C@](C(OC)=O)(O)[C@@H]1OC(C)=O | ||
| 分子式 | C46H56N4O10 | 分子量 | 824.96 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C, protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.2122 mL | 6.0609 mL | 12.1218 mL |
| 5 mM | 0.2424 mL | 1.2122 mL | 2.4244 mL |
| 10 mM | 0.1212 mL | 0.6061 mL | 1.2122 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Genetic factors influencing the development of vincristine-induced neurotoxicity
Expert Opin Drug Metab Toxicol 2021 Feb;17(2):215-226.PMID:33283553DOI:10.1080/17425255.2021.1855141.
Introduction: One of the most common side effects during Vincristine (VCR) use is the establishment of VCR-induced peripheral neuropathy (VIPN). Among several risk factors that can influence the development of VIPN, such as cumulative dose and patient's age, sex, ethnicity, and genetic variants, this review is focused on the genetic variability. Areas covered: A literature research was performed firstly using the following PubMed search string ((((CIPN OR (Vincristine AND neurotoxicity OR (Vincristine AND neuropathy))) AND (polymorphisms OR (genetic variants OR (genetic factors OR (genetic profile OR (pharmacogenetics OR (genome-wide OR (genetic risk OR (expression genotype))))))))))) but also other relevant papers cited by the selected articles were included. Based on the obtained results, we identified two main categories of genes: genes involved in pharmacokinetics (genes related to metabolism and transport) or pharmacodynamics (genes related to mechanism of action) of VCR. Expert opinion: Despite several clinical retrospective studies investigating the possible correlations between patient genotype and VIPN onset, contrasting and inconsistent results are reported. In conclusion, given the clinical relevance of VIPN, further and more focused research would be fundamental in order to identify genetic variants able to predict its development and to allow a safer management of treated patients.
CD38-Directed Vincristine Nanotherapy for Acute Lymphoblastic Leukemia
Biomacromolecules 2022 Jan 10;23(1):377-387.PMID:34913676DOI:10.1021/acs.biomac.1c01342.
Acute lymphoblastic leukemia (ALL) is the most common malignancy in children. Although intensive chemotherapy greatly improved the survival rate, it is often accompanied by severe and lifelong side effects as a result of weak ALL selectivity. The intensive and poorly selective chemotherapy is also detrimental to patients' immune system. There is an urgent need to develop more selective and less toxic chemotherapy for ALL. Here, we report daratumumab-polymersome-vincristine (DP-VCR) as a CD38-directed nanotherapy for ALL. DP-VCR showed selective uptake in CD38-positive 697 and Nalm-6-Luc ALL cells and potent anti-ALL activity with an IC50 as low as 0.06 nM VCR, which was 13.7-fold more potent than free VCR. In contrast, no toxicity to human peripheral blood mononuclear cells was detected for DP-VCR even at 108.3 nM VCR. The apoptotic assays confirmed a high selectivity of DP-VCR to CD38-positive ALL cells. DP-VCR exhibited superior treatment of both 697 and Nalm-6-Luc orthotopic ALL models to all controls, as revealed by significant survival benefit and marked reduction of leukemia burden in bone marrow, blood, spleen, and liver. Importantly, DP-VCR induced few side effects. DP-VCR emerges as a safe and potent nanotherapy for CD38-positive ALL.
Vincristine-induced dysphagia
South Med J 1978 Nov;71(11):1364-5.PMID:715485DOI:10.1097/00007611-197811000-00014.
Dysphagia was observed in two patients receiving combination chemotherapy for metastatic carcinoma of the breast. Results of esophagogram and esophagoscopy were unremarkable. Vincristine, an anticancer drug, was incriminated as the causative agent. Cessation of Vincristine therapy resulted in definite improvement. In one patient, inadvertent administration of Vincristine caused prompt recurrence of dysphagia, which again disappeared upon discontinuation of the drug. The major toxicity of Vincristine is neurologic. The exact mechanism for vincristine-induced dysphagia is unknown, but it does appear to be reversible.
Vincristine sulfate liposome injection: a guide to its use in refractory or relapsed acute lymphoblastic leukemia
BioDrugs 2013 Feb;27(1):69-74.PMID:23329395DOI:10.1007/s40259-012-0002-5.
Adult patients with acute lymphoblastic leukemia frequently relapse or are refractory to conventional treatments. The Vincristine sulfate liposome injection (Marqibo(®)) encapsulates the drug in a liposome composed of sphingomyelin and cholesterol to improve tumor drug exposure. At a dose of 2.25 mg/m(2) once weekly, this formulation was associated with an overall response rate of 35 % in adults with Philadelphia chromosome-negative relapsed or refractory disease. There were no new or unexpected toxicities.
Vincristine liposomal--INEX: lipid-encapsulated Vincristine, onco TCS, transmembrane carrier system--vincristine, vincacine, Vincristine sulfate liposomes for injection, VSLI
Drugs R D 2004;5(2):119-23.PMID:15293876DOI:10.2165/00126839-200405020-00012.
INEX Pharmaceuticals is developing a liposomal formulation of Vincristine [Onco TCS, vincacine, VSLI, Vincristine sulfate liposomes for injection] for the treatment of relapsed aggressive non-Hodgkin's lymphoma (NHL) and other cancers. It is being developed using INEX's proprietary drug-delivery technology platform called the transmembrane carrier systems (TCS), which enables the targeted intracellular delivery of various therapeutic agents. Liposomal Vincristine is expected to have certain advantages over the existing standard preparation of Vincristine because the use of TCS technology enables the Vincristine to circulate in the blood for longer, accumulate in the tumour, and be released over an extended period of time at the tumour site. The application of TCS technology to any agent, including Vincristine, has the potential to increase the efficacy and decrease the side effects of the agent. INEX decided in 1998 to focus on gaining approval for liposomal Vincristine in the treatment of relapsed aggressive NHL because no standard therapy was approved for this indication. In 1999, liposomal Vincristine was granted accelerated development status by the US FDA, which enables the FDA to approve it based on the surrogate endpoint of a single clinical trial. In addition, the FDA granted liposomal Vincristine fast track status in August 2000. In April 2001, INEX and Elan Corporation formed a joint venture for the development and commercialisation of liposomal Vincristine, with both companies contributing assets to the venture including worldwide rights to the product and intellectual property rights. The joint venture was called IE Oncology. However, in June 2002, Elan announced that it was going to focus its business strategy on three specific areas, which would not include cancer therapies. INEX announced it had regained 100% ownership of liposomal Vincristine in April 2003, by reacquiring the 19.9% equity interest held by Elan and in addition retaining a fully paid-up licence to Elan's intellectual property pertaining to liposomal Vincristine. All obligations to Elan under the agreement will be met through three milestone payments totalling $8 million. Some of the milestones may be paid in shares valued at the then current market price. In January 2004, INEX and Enzon Pharmaceuticals formed a strategic partnership to develop and commercialise liposomal Vincristine. Under the terms of the agreement, Enzon receives the exclusive North American commercialisation rights for liposomal Vincristine for all indications. INEX will receive upfront and milestone payments as well as a percentage of commercial sales. Additionally, the formation of this partnership triggered a US$3 million payment from INEX to the former joint venture partner, Elan Corporation. Nine clinical trials of liposomal Vincristine are currently being conducted, including one phase I/II trial and eight phase II trials. A phase II/III trial was completed in December 2002. In September 2003, Inex commenced a 'rolling submission' for liposomal Vincristine by submitting the first of three major sections of the NDA to the FDA. The second major section was submitted to the FDA in December 2003. INEX expects to complete the filing with the submission of the clinical section of the NDA in the first quarter of 2004. Dow Jones Newswires reported on 1 October 2001 that the CEO of INEX expects Onco TCS to achieve sales of between $US100 and $US400 million annually for the company. FDA approval was then predicted for late 2002 or early 2003.