Vinorelbine ditartrate(Synonyms: 酒石酸长春瑞滨; KW-2307; Nor-5′-anhydrovinblastine ditartrate)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Vinorelbine ditartrate (Synonyms: 酒石酸长春瑞滨; KW-2307; Nor-5′-anhydrovinblastine ditartrate) 纯度: 98.08%

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(Synonyms: 酒石酸长春瑞滨; KW-2307;  Nor-5

Vinorelbine ditartrate Chemical Structure

CAS No. : 125317-39-7

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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:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: Saline

    Solubility: 20 mg/mL (18.53 mM); Clear solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.08 mg/mL (1.93 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (1.93 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 3.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.08 mg/mL (1.93 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (1.93 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 4.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (1.93 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (1.93 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
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.

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.

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Vinflunine ditartrate(Synonyms: 酒石酸长春氟宁)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Vinflunine ditartrate (Synonyms: 酒石酸长春氟宁)

Vinflunine ditartrate 是一种长春花生物碱家族的氟化微管抑制剂。Vinflunine ditartrate 具有抗血管生成,破坏血管和抗转移的活性。Vinflunine ditartrate 可用于尿路上皮移行细胞癌,非小细胞肺癌和乳腺癌的研究。

Vinflunine ditartrate(Synonyms: 酒石酸长春氟宁)

Vinflunine ditartrate Chemical Structure

CAS No. : 194468-36-5

规格 价格 是否有货
5 mg ¥8500 询问价格 & 货期
10 mg ¥13600 询问价格 & 货期

* Please select Quantity before adding items.

生物活性

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.

储存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

参考文献
  • [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.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Vinorelbine-d3 ditartrate(Synonyms: KW-2307-d3 ditartrate; Nor-5′-anhydrovinblastine-d3 ditartrate)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Vinorelbine-d3 ditartrate (Synonyms: KW-2307-d3 ditartrate; Nor-5′-anhydrovinblastine-d3 ditartrate)

Vinorelbine-d3 (KW-2307-d3) ditartrate 是 Vinorelbine ditartrate 的氘代物。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-d3 ditartrate(Synonyms: KW-2307-d3 ditartrate; Nor-5

Vinorelbine-d3 ditartrate Chemical Structure

CAS No. : 35674-14-7

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

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.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Vinorelbine-d3 ditartrate(Synonyms: KW-2307-d3 ditartrate; Nor-5′-anhydrovinblastine-d3 ditartrate)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Vinorelbine-d3 ditartrate (Synonyms: KW-2307-d3 ditartrate; Nor-5′-anhydrovinblastine-d3 ditartrate)

Vinorelbine-d3 (KW-2307-d3) ditartrate 是 Vinorelbine ditartrate 的氘代物。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-d3 ditartrate(Synonyms: KW-2307-d3 ditartrate; Nor-5

Vinorelbine-d3 ditartrate Chemical Structure

CAS No. : 35674-14-7

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

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.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Vinorelbine-d3 ditartrate(Synonyms: KW-2307-d3 ditartrate; Nor-5′-anhydrovinblastine-d3 ditartrate)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Vinorelbine-d3 ditartrate (Synonyms: KW-2307-d3 ditartrate; Nor-5′-anhydrovinblastine-d3 ditartrate)

Vinorelbine-d3 (KW-2307-d3) ditartrate 是 Vinorelbine ditartrate 的氘代物。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-d3 ditartrate(Synonyms: KW-2307-d3 ditartrate; Nor-5

Vinorelbine-d3 ditartrate Chemical Structure

CAS No. : 35674-14-7

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

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.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务