Vinflunine ditartrate is the first fluorinated microtubule inhibitor belonging to the Vinca alkaloids family. Vinflunine ditartrate has anti-angiogenic, vascular-disrupting and anti-metastatic activities. Vinflunine ditartrate can be used for the research of transitional cell carcinoma of the urothelial tract, non-small cell lung cancer, and carcinoma of the breast[1][2].
IC50 & Target
microtubule[1]
体外研究 (In Vitro)
Vinflunine (0.01-10 μM; 45 min) induces a rapid change in endothelial cell shape: cells retracted and assumed a rounded morphology[2]. Vinflunine (0.01-10 μM; 1 h) disrupts newly formed capillary-like structures[2]. Vinflunine (0.01-10 μM; 1 h) inhibits endothelial cell motility, with an IC50 of 0.71 μM[2]. Vinflunine (0.001-10 μM; 1-72 h) inhibits endothelial cell proliferation in vitro[2].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
Vinflunine (0.08-20 mg/kg; i.v.) reduces the number of experimental liver metastases by human LS174T colon cancer cells[2]. Vinflunine (0.63-5 mg/kg; i.v. before and 2 d after Matrigel implantation) inhibits the bFGF-induced angiogenic response in mice in a dose-dependent manner[2].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Female athymic nude mice (BALB/c/Ola/Hsd-nu) were implanted LS174T cells[2]
Dosage:
0.08, 0.16, 1.25, 5, 10, 20 mg/kg
Administration:
I.v. on days 4, 7, 11, 14, 18 and 21 after tumour cell implantation
Result:
Induced a dose-dependent reduction in the number of metastatic foci at the surface of the liver and was well tolerated.
Clinical Trial
分子量
1117.10
Formula
C53H66F2N4O20
CAS 号
194468-36-5
中文名称
酒石酸长春氟宁
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Bennouna J, et, al. Vinflunine: a new microtubule inhibitor agent. Clin Cancer Res. 2008 Mar 15;14(6):1625-32.
[2]. Kruczynski A, et, al. Anti-angiogenic, vascular-disrupting and anti-metastatic activities of vinflunine, the latest vinca alkaloid in clinical development. Eur J Cancer. 2006 Nov;42(16):2821-32.
Vinorelbine-d3 (KW-2307-d3) ditartrate is the deuterium labeled Vinorelbine ditartrate. Vinorelbine (ditartrate) is an anti-mitotic agent which inhibits the proliferation of Hela cells with IC50 of 1.25 nM.
体外研究 (In Vitro)
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
1082.12
Formula
C53H63D3N4O20
CAS 号
35674-14-7
中文名称
酒石酸长春瑞滨 d3 (双酒石酸盐)
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.
[2]. Ngan VK, et al. Mechanism of mitotic block and inhibition of cell proliferation by the semisynthetic Vinca alkaloids vinorelbine and its newer derivative vinflunine. Mol Pharmacol. 2001 Jul;60(1):225-32.
[3]. Liu XM, et al. Unique induction of p21(WAF1/CIP1)expression by vinorelbine in androgen-independent prostate cancer cells. Br J Cancer. 2003 Oct 20;89(8):1566-73.
[4]. Poirier VJ, et al. Toxicity, dosage, and efficacy of vinorelbine (Navelbine) in dogs with spontaneous neoplasia. J Vet Intern Med. 2004 Jul-Aug;18(4):536-9.
[5]. Pierro JA, et al. Phase I clinical trial of vinorelbine in tumor-bearing cats. J Vet Intern Med. 2013 Jul-Aug;27(4):943-8.
Vinorelbine-d3 (KW-2307-d3) ditartrate is the deuterium labeled Vinorelbine ditartrate. Vinorelbine (ditartrate) is an anti-mitotic agent which inhibits the proliferation of Hela cells with IC50 of 1.25 nM.
体外研究 (In Vitro)
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
1082.12
Formula
C53H63D3N4O20
CAS 号
35674-14-7
中文名称
酒石酸长春瑞滨 d3 (双酒石酸盐)
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.
[2]. Ngan VK, et al. Mechanism of mitotic block and inhibition of cell proliferation by the semisynthetic Vinca alkaloids vinorelbine and its newer derivative vinflunine. Mol Pharmacol. 2001 Jul;60(1):225-32.
[3]. Liu XM, et al. Unique induction of p21(WAF1/CIP1)expression by vinorelbine in androgen-independent prostate cancer cells. Br J Cancer. 2003 Oct 20;89(8):1566-73.
[4]. Poirier VJ, et al. Toxicity, dosage, and efficacy of vinorelbine (Navelbine) in dogs with spontaneous neoplasia. J Vet Intern Med. 2004 Jul-Aug;18(4):536-9.
[5]. Pierro JA, et al. Phase I clinical trial of vinorelbine in tumor-bearing cats. J Vet Intern Med. 2013 Jul-Aug;27(4):943-8.
Vinorelbine-d3 (KW-2307-d3) ditartrate is the deuterium labeled Vinorelbine ditartrate. Vinorelbine (ditartrate) is an anti-mitotic agent which inhibits the proliferation of Hela cells with IC50 of 1.25 nM.
体外研究 (In Vitro)
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
1082.12
Formula
C53H63D3N4O20
CAS 号
35674-14-7
中文名称
酒石酸长春瑞滨 d3 (双酒石酸盐)
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.
[2]. Ngan VK, et al. Mechanism of mitotic block and inhibition of cell proliferation by the semisynthetic Vinca alkaloids vinorelbine and its newer derivative vinflunine. Mol Pharmacol. 2001 Jul;60(1):225-32.
[3]. Liu XM, et al. Unique induction of p21(WAF1/CIP1)expression by vinorelbine in androgen-independent prostate cancer cells. Br J Cancer. 2003 Oct 20;89(8):1566-73.
[4]. Poirier VJ, et al. Toxicity, dosage, and efficacy of vinorelbine (Navelbine) in dogs with spontaneous neoplasia. J Vet Intern Med. 2004 Jul-Aug;18(4):536-9.
[5]. Pierro JA, et al. Phase I clinical trial of vinorelbine in tumor-bearing cats. J Vet Intern Med. 2013 Jul-Aug;27(4):943-8.
Vinorelbine ditartrate 是一种抗有丝分裂剂，能够抑制 Hela 细胞的增殖，IC50值为 1.25 nM。
Vinorelbine ditartrate Chemical Structure
CAS No. : 125317-39-7
规格
价格
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数量
Free Sample (0.1-0.5 mg)
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10 mM * 1 mL in DMSO
￥773
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10 mg
￥651
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￥2046
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询价
200 mg
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生物活性
Vinorelbine (ditartrate) is an anti-mitotic agent which inhibits the proliferation of Hela cells with IC50 of 1.25 nM.
体外研究 (In Vitro)
Vinorelbine (0.5-5 nM) inhibits cell proliferation by 50% (IC50) at concentrations of 1.25 nM. At concentration of 8 nM vinorelbine, no cells are in anaphase[1]. Vinorelbine time-dependently induces the p53 and p21WAFI/CIP1 expression in androgen-dependent (AD) and- independent (AI) prostate cancer cell lines. Vinorelbine stimulates reporter genes in a concentration-dependent manner[2].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
After vinorelbine treatment, the first neutropenicepisode occurred after the first (4 dogs), second (1), or sixth(1) vinorelbine treatment in the dogs[3]. Vinorelbine is tolerated at a weekly interval in tumor-bearing cats, with an MTD of 11.5 mg/m2[4].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量
1079.11
Formula
C53H66N4O20
CAS 号
125317-39-7
中文名称
酒石酸长春瑞滨；长春瑞宾双酒石酸盐；重酒石酸长春瑞宾
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moisture and light
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
溶解性数据
In Vitro:
DMSO : ≥ 100 mg/mL (92.67 mM)
H2O : ≥ 100 mg/mL (92.67 mM)
*“≥” means soluble, but saturation unknown.
配制储备液
浓度溶剂体积质量
1 mg
5 mg
10 mg
1 mM
0.9267 mL
4.6334 mL
9.2669 mL
5 mM
0.1853 mL
0.9267 mL
1.8534 mL
10 mM
0.0927 mL
0.4633 mL
0.9267 mL
*
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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-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。
In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
[1]. Ngan VK, et al. Mechanism of mitotic block and inhibition of cell proliferation by the semisynthetic Vinca alkaloids vinorelbine and its newer derivative vinflunine. Mol Pharmacol. 2001 Jul;60(1):225-32.
[2]. Liu XM, et al. Unique induction of p21(WAF1/CIP1)expression by vinorelbine in androgen-independent prostate cancer cells. Br J Cancer. 2003 Oct 20;89(8):1566-73.
[3]. Poirier VJ, et al. Toxicity, dosage, and efficacy of vinorelbine (Navelbine) in dogs with spontaneous neoplasia. J Vet Intern Med. 2004 Jul-Aug;18(4):536-9.
[4]. Pierro JA, et al. Phase I clinical trial of vinorelbine in tumor-bearing cats. J Vet Intern Med. 2013 Jul-Aug;27(4):943-8.
Animal Administration [4]
As defined by the study, VRL1 is diluted in 0.9% NaCl to a concentration of 1.5 mg/mL, and given IV over 5 minutes. The intended treatment interval is 7 days for up to 4 treatments. After receiving 4 weekly doses, cats are eligible to continue VRL treatment every 2 weeks.
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献
[1]. Ngan VK, et al. Mechanism of mitotic block and inhibition of cell proliferation by the semisynthetic Vinca alkaloids vinorelbine and its newer derivative vinflunine. Mol Pharmacol. 2001 Jul;60(1):225-32.
[2]. Liu XM, et al. Unique induction of p21(WAF1/CIP1)expression by vinorelbine in androgen-independent prostate cancer cells. Br J Cancer. 2003 Oct 20;89(8):1566-73.
[3]. Poirier VJ, et al. Toxicity, dosage, and efficacy of vinorelbine (Navelbine) in dogs with spontaneous neoplasia. J Vet Intern Med. 2004 Jul-Aug;18(4):536-9.
[4]. Pierro JA, et al. Phase I clinical trial of vinorelbine in tumor-bearing cats. J Vet Intern Med. 2013 Jul-Aug;27(4):943-8.
