Vincristine通过与微管蛋白结合而抑制微管聚合,IC50为32 μM。
Vincristine is a naturally occurring alkaloid that potently inhibits the tubulin addition with the inhibition constant Ki value of 0.085 μM and exhibits an anti-proliferative activity against B16 melanoma cells with the half maximal inhibition concentration IC50 value of 0.45 M.
Saline
10 nM
3 mg/kg 腹腔注射
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 | |
例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。
[1] Jordan MA, et al. Cancer Res, 1985, 45(6), 2741-2747.
[2] Li, Y., et al. 1992. Biochem. Biophys. Res. Commun. 187: 722-729.
[3] Zhang, J., et al. 1996. Proc. Natl. Acad. Sci. U.S.A. 93: 5325-5328.
分子式 C46H58N4O14S |
分子量 923.04 |
CAS号 2068-78-2 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 90 mg/mL |
Water 40 mg/mL |
Ethanol <1 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT00038207 | Soft Tissue Sarcoma|Lymphoma|Leukemia|Wilms' Tumor|Osteosarcoma | Drug: Liposomal Vincristine | M.D. Anderson Cancer Center|Inex Pharmaceuticals | Phase 2 | 2000-06-01 | 2012-07-27 |
NCT00555464 | Hemangioma | Drug: Vincristine|Drug: Prednisone | Medical College of Wisconsin|FDA Office of Orphan Products Development | Phase 2 | 2007-11-01 | 2013-06-04 |
NCT01222780 | Sarcoma|Neuroblastoma|Wilms Tumor|Leukemia|Lymphoma|Brain Tumors | Drug: Marqibo | Spectrum Pharmaceuticals, Inc|National Cancer Institute (NCI) | Phase 1|Phase 2 | 2010-09-01 | 2015-05-26 |
NCT02337478 | Recurrent Adult Acute Myeloid Leukemia | Drug: Vincristine Sulfate Liposome|Other: Laboratory Biomarker Analysis | Wake Forest University Health Sciences|National Cancer Institute (NCI)|Spectrum Pharmaceuticals, Inc | Phase 2 | 2015-05-01 | 2017-01-17 |
NCT01397825 | Diffuse Large B-Cell Lymphoma|Transformed Follicular Lymphoma|Mantle Cell Lymphoma|Burkitt's Lymphoma | Drug: Alisertib (MLN8237) + Rituximab + Vincristine | Millennium Pharmaceuticals, Inc.|Takeda | Phase 1|Phase 2 | 2011-08-01 | 2016-11-17 |
NCT00022555 | AIDS-related Diffuse Large Cell Lymphoma|AIDS-related Diffuse Mixed Cell Lymphoma|AIDS-related Peripheral/Systemic Lymphoma|AIDS-related Small Noncleaved Cell Lymphoma | Drug: bryostatin 1|Drug: vincristine sulfate | National Cancer Institute (NCI) | Phase 1 | 2001-11-01 | 2013-01-24 |
NCT00145041 | Malignant Melanoma | Drug: Vincristine Sulfate Liposomes Injection | Spectrum Pharmaceuticals, Inc | Phase 1 | 2005-02-01 | 2014-03-27 |
NCT02923388 | Vincristine Induced Peripheral Neuropathy (VIPN) | Drug: Injection Mecobalamin,|Drug: Tablet Pyridoxine hydrochloride|Drug: Intravenous normal saline 1 ml|Drug: Placebo pill | Bangabandhu Sheikh Mujib Medical University, Dhaka, Bangladesh | Phase 2 | 2016-10-01 | 2016-10-14 |
NCT00058305 | Extranodal Marginal Zone B-cell Lymphoma of Mucosa-associated Lymphoid Tissue|Nodal Marginal Zone B-cell Lymphoma|Recurrent Adult Diffuse Large Cell Lymphoma|Recurrent Adult Diffuse Mixed Cell Lymphoma|Recurrent Adult Diffuse Small Cleaved Cell Lymphoma|Recurrent Grade 1 Follicular Lymphoma|Recurrent Grade 2 Follicular Lymphoma|Recurrent Grade 3 Follicular Lymphoma|Recurrent Mantle Cell Lymphoma|Recurrent Marginal Zone Lymphoma|Recurrent Small Lymphocytic Lymphoma|Splenic Marginal Zone Lymphoma | Drug: bryostatin 1|Drug: vincristine sulfate|Other: laboratory biomarker analysis | National Cancer Institute (NCI) | Phase 2 | 2003-03-01 | 2013-01-09 |
NCT02861040 | Recurrent Adult Acute Lymphoblastic Leukemia|Refractory Adult Acute Lymphoblastic Leukemia | Other: Laboratory Biomarker Analysis|Other: Pharmacological Study|Drug: Vincristine Sulfate Liposome|Drug: Volasertib | Northwestern University|National Comprehensive Cancer Network|National Cancer Institute (NCI) | Phase 1 | 2016-08-01 | 2016-12-13 |
NCT00003166 | Recurrent Adult Burkitt Lymphoma|Recurrent Adult Diffuse Large Cell Lymphoma|Recurrent Adult Diffuse Mixed Cell Lymphoma|Recurrent Adult Immunoblastic Large Cell Lymphoma|Recurrent Adult Lymphoblastic Lymphoma|Recurrent Grade 3 Follicular Lymphoma|Recurrent Mantle Cell Lymphoma|Refractory Chronic Lymphocytic Leukemia|Refractory Multiple Myeloma|Stage III Multiple Myeloma | Drug: bryostatin 1|Drug: vincristine sulfate|Other: laboratory biomarker analysis | National Cancer Institute (NCI) | Phase 1 | 1998-05-01 | 2013-01-10 |
NCT00901069 | Lymphoma|Hodgkin Disease|Lymphoma, Non-Hodgkin | Drug: Azacitidine with rituximab, vincristine, and cyclophosphamide | Shams Shakil|Celgene|University of Kentucky | Phase 1 | 2009-05-01 | 2016-10-13 |
NCT00144963 | Acute Lymphoblastic Leukemia | Drug: Vincristine Sulfate Liposomes Injection|Drug: Dexamethasone | Spectrum Pharmaceuticals, Inc | Phase 1|Phase 2 | 2002-07-01 | 2014-03-27 |
NCT02360930 | Leukemia, Acute Lymphoblastic|Leukemia | Children's Hospital Los Angeles | 2014-09-01 | 2015-06-18 | ||
NCT01439347 | Acute Lymphoblastic Leukemia (ALL) | Drug: Vincristine Sulfate Liposomes Injection (VSLI)|Drug: Vincristine Sulfate Injection (VSI) | Spectrum Pharmaceuticals, Inc | Phase 3 | 2012-03-01 | 2016-07-20 |
NCT02879643 | ALL, Childhood|Lymphoblastic Leukemia, Acute, Childhood|Lymphoblastic Leukemia, Acute | Drug: Marqibo in combination with UK ALL R3 | Therapeutic Advances in Childhood Leukemia Consortium|Spectrum Pharmaceuticals, Inc | Phase 1 | 2016-07-01 | 2017-01-25 |
注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。
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