Vinorelbine (Synonyms: 长春瑞滨; KW-2307 base)

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Vinorelbine(KW-2307 base)是抗有丝分裂剂，能抑制Hela细胞增殖，IC50为1.25 nM。

该游离形式化合物不稳定，推荐具有相同生物学活性的稳定盐形式 Vinorelbine ditartrate。

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Vinorelbine Chemical Structure

CAS No. : 71486-22-1

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Vinorelbine 的其他形式现货产品:

Vinorelbine ditartrate

Other Forms of Vinorelbine:

Vinorelbine ditartrate In-stock

MCE 顾客使用本产品发表的 14 篇科研文献

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生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Vinorelbine is an anti-mitotic agent which inhibits the proliferation of Hela cells with IC₅₀ of 1.25 nM.

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A-431	IC₅₀	60 nM Compound: Vinorelbine	Antiproliferative activity against human A431 cells after 72 hrs by sulforhodamine B assay Antiproliferative activity against human A431 cells after 72 hrs by sulforhodamine B assay	[PMID: 21480626]
A549	IC₅₀	0.03 μM Compound: 1e	Cytotoxicity against human A549 cells by sulforhodamine B assay Cytotoxicity against human A549 cells by sulforhodamine B assay	[PMID: 19499938]
A549	IC₅₀	0.049 μM Compound: 1e, AVLB	Cytotoxicity against human A549 cells after 72 hrs by SRB assay Cytotoxicity against human A549 cells after 72 hrs by SRB assay	[PMID: 17544278]
A549	IC₅₀	0.6 μM Compound: Vinorelbine	Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay	[PMID: 33588178]
A549	IC₅₀	10 nM Compound: 1d	Cytotoxicity against human A549 cells by MTT assay Cytotoxicity against human A549 cells by MTT assay	[PMID: 22525316]
A549	IC₅₀	26.1 μM Compound: vinorelbine	Cytotoxicity against human A549 cells after 48 hrs by MTT assay Cytotoxicity against human A549 cells after 48 hrs by MTT assay	[PMID: 20462230]
A549	IC₅₀	36.9 nM Compound: 1a	Cytotoxicity against human A549 cells after 72 hrs by SRB assay Cytotoxicity against human A549 cells after 72 hrs by SRB assay	[PMID: 18771244]
A549	IC₅₀	64.6 nM Compound: Vinorelbine	Antiproliferative activity against human A549 cells after 72 hrs by sulforhodamine B assay Antiproliferative activity against human A549 cells after 72 hrs by sulforhodamine B assay	[PMID: 21480626]
A549	IC₅₀	9 nM Compound: 1d, NVB	Cytotoxicity against human A549 cells after 24 to 72 hrs by MTT assay Cytotoxicity against human A549 cells after 24 to 72 hrs by MTT assay	[PMID: 23107481]
HCC1937	IC₅₀	> 10 μM Compound: Vinorelbine	Antiproliferative activity against exponentially growing adherent human HCC1937 cells assessed as inhibition of cell proliferation after 72 hrs by luminescence detection based ATPlite assay Antiproliferative activity against exponentially growing adherent human HCC1937 cells assessed as inhibition of cell proliferation after 72 hrs by luminescence detection based ATPlite assay	[PMID: 25872984]
HCT-116	IC₅₀	0.0149 μM Compound: Vinorelbine	Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 32473523]
HCT-116	IC₅₀	0.015 μM Compound: Vinorelbine	Cytotoxicity against human HCT116 cells after 72 hrs by resazurin-based fluorimetric assay Cytotoxicity against human HCT116 cells after 72 hrs by resazurin-based fluorimetric assay	[PMID: 24901800]
HCT-116	IC₅₀	15 nM Compound: 3, VLN	Cytotoxicity against human HCT116 cells assessed as inhibition of cell proliferation after 72 hrs Cytotoxicity against human HCT116 cells assessed as inhibition of cell proliferation after 72 hrs	[PMID: 25804719]
HCT-116	IC₅₀	35 nM Compound: 7, VLN	Cytotoxicity against human HCT116 cells after 72 hrs by resazurin assay Cytotoxicity against human HCT116 cells after 72 hrs by resazurin assay	[PMID: 23822556]
HCT-116	IC₅₀	35 nM Compound: 4, VLN	Antiproliferative activity against human HCT116 cells after 72 hrs Antiproliferative activity against human HCT116 cells after 72 hrs	[PMID: 24871162]
HCT-116	IC₅₀	75 nM Compound: 22	Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by phosphatase assay Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by phosphatase assay	[PMID: 23252481]
HCT-116/VM46	IC₅₀	600 nM Compound: 22	Cytotoxicity against human vinblastine-resistant HCT116/VM46 cells assessed as growth inhibition after 72 hrs by phosphatase assay Cytotoxicity against human vinblastine-resistant HCT116/VM46 cells assessed as growth inhibition after 72 hrs by phosphatase assay	[PMID: 23252481]
HeLa	IC₅₀	0.026 μM Compound: 1e, AVLB	Cytotoxicity against human HeLa cells after 72 hrs by SRB assay Cytotoxicity against human HeLa cells after 72 hrs by SRB assay	[PMID: 17544278]
HeLa	IC₅₀	0.027 μM Compound: 1e	Cytotoxicity against human HeLa cells by sulforhodamine B assay Cytotoxicity against human HeLa cells by sulforhodamine B assay	[PMID: 19499938]
HeLa	IC₅₀	0.066 μM Compound: Vinorelbine	Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay	[PMID: 29624387]
HeLa	IC₅₀	26.9 nM Compound: 1a	Cytotoxicity against human HeLa cells after 72 hrs by SRB assay Cytotoxicity against human HeLa cells after 72 hrs by SRB assay	[PMID: 18771244]
HeLa	IC₅₀	27 nM Compound: 1f, AVBL	Cytotoxicity against human HeLa cells by MTT assay Cytotoxicity against human HeLa cells by MTT assay	[PMID: 22115594]
HeLa	IC₅₀	9 nM Compound: 1d	Cytotoxicity against human HeLa cells by MTT assay Cytotoxicity against human HeLa cells by MTT assay	[PMID: 22525316]
HepG2	IC₅₀	0.11 μM Compound: Vinorelbine	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 32473523]
HepG2	IC₅₀	23.12 μM Compound: Vinorelbine	Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay	[PMID: 26420067]
HL-60	IC₅₀	< 0.06 μM Compound: vinorelbine	Cytotoxicity against human HL60 cells after 48 hrs by MTT assay Cytotoxicity against human HL60 cells after 48 hrs by MTT assay	[PMID: 20462230]
HL-60	IC₅₀	11.47 μM Compound: Vinorelbine	Cytotoxicity against human HL60 cells after 48 hrs by MTT assay Cytotoxicity against human HL60 cells after 48 hrs by MTT assay	[PMID: 26420067]
HT-29	IC₅₀	11.9 nM Compound: Vinorelbine	Antiproliferative activity against human HT-29 cells after 72 hrs by sulforhodamine B assay Antiproliferative activity against human HT-29 cells after 72 hrs by sulforhodamine B assay	[PMID: 21480626]
HUVEC	IC₅₀	2 nM Compound: 7, VLN	Cytotoxicity against HUVEC after 72 hrs by resazurin assay Cytotoxicity against HUVEC after 72 hrs by resazurin assay	[PMID: 23822556]
K562	IC₅₀	0.003 μM Compound: 3; VLN	Cytotoxicity against human K562 cells incubated for 72 hrs by CellTiter 96 aqueous one solution reagent based assay Cytotoxicity against human K562 cells incubated for 72 hrs by CellTiter 96 aqueous one solution reagent based assay	[PMID: 27753480]
K562	IC₅₀	0.006 μM Compound: Vinorelbine	Cytotoxicity against human K562 cells after 72 hrs by resazurin-based fluorimetric assay Cytotoxicity against human K562 cells after 72 hrs by resazurin-based fluorimetric assay	[PMID: 24901800]
K562	IC₅₀	20 nM Compound: 7, VLN	Cytotoxicity against human K562 cells after 72 hrs by resazurin assay Cytotoxicity against human K562 cells after 72 hrs by resazurin assay	[PMID: 23822556]
K562	IC₅₀	3.5 nM Compound: 4, VLN	Antiproliferative activity against human K562 cells after 72 hrs Antiproliferative activity against human K562 cells after 72 hrs	[PMID: 24871162]
K562	IC₅₀	6 nM Compound: 3, VLN	Cytotoxicity against human K562 cells assessed as inhibition of cell proliferation after 72 hrs Cytotoxicity against human K562 cells assessed as inhibition of cell proliferation after 72 hrs	[PMID: 25804719]
K-562R	IC₅₀	0.41 μM Compound: 3; VLN	Cytotoxicity against doxorubicin-resistant human K562R cells incubated for 72 hrs by CellTiter 96 aqueous one solution reagent based assay Cytotoxicity against doxorubicin-resistant human K562R cells incubated for 72 hrs by CellTiter 96 aqueous one solution reagent based assay	[PMID: 27753480]
KB	IC₅₀	0.001 μM Compound: 4, nor-AVLB	Cytotoxicity against human KB cells after 72 hrs Cytotoxicity against human KB cells after 72 hrs	[PMID: 19072542]
KB	IC₅₀	0.04 μM Compound: 3, AVLB	Cytotoxicity against human KB cells after 72 hrs Cytotoxicity against human KB cells after 72 hrs	[PMID: 19072542]
KB	EC₅₀	6 nM Compound: Vinorelbine	Cell cycle arrest in human KB cells assessed as accumulation of cells at G2/M phase after 24 hrs by propidium iodide-based FACScan Cell cycle arrest in human KB cells assessed as accumulation of cells at G2/M phase after 24 hrs by propidium iodide-based FACScan	[PMID: 21480626]
L1210	IC₅₀	65 nM Compound: 22	Cytotoxicity against mouse L1210 cells assessed as growth inhibition after 72 hrs by phosphatase assay Cytotoxicity against mouse L1210 cells assessed as growth inhibition after 72 hrs by phosphatase assay	[PMID: 23252481]
MCF7	IC₅₀	0.07 μM Compound: vinorelbine	Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 19743863]
MCF7	IC₅₀	17.2 μM Compound: vinorelbine	Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay	[PMID: 20462230]
MCF7	IC₅₀	4 nM Compound: 4, VLN	Antiproliferative activity against human MCF7 cells after 72 hrs Antiproliferative activity against human MCF7 cells after 72 hrs	[PMID: 24871162]
MES-SA	IC₅₀	0.21 μM Compound: Vinorelbine	Cytotoxicity against human MES-SA cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay Cytotoxicity against human MES-SA cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay	[PMID: 33588178]
MES-SA/Dx5	IC₅₀	> 32 μM Compound: Vinorelbine	Cytotoxicity against human MES-SA/Dx5 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay Cytotoxicity against human MES-SA/Dx5 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay	[PMID: 33588178]
NCI/ADR-RES	IC₅₀	5000 nM Compound: VRB	Cytotoxicity against Pgp overexpressing human NCI-ADR-RES cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against Pgp overexpressing human NCI-ADR-RES cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 26132075]
NCI/ADR-RES	IC₅₀	5000 nM Compound: VRB	Growth inhibition of human NCI/ADR-RES cells after 96 hrs by trypan blue exclusion assay Growth inhibition of human NCI/ADR-RES cells after 96 hrs by trypan blue exclusion assay	[PMID: 29730191]
NCI/ADR-RES	IC₅₀	5000 nM Compound: VRB	Cytotoxicity against human NCI/ADR-RES cells assessed as growth inhibition by trypan blue exclusion assay Cytotoxicity against human NCI/ADR-RES cells assessed as growth inhibition by trypan blue exclusion assay	[PMID: 23214452]
NCI/ADR-RES	IC₅₀	5000 nM Compound: VRB	Cytotoxicity against human NCI/ADR-RES cells assessed as growth inhibition after 96 hrs by Giemsa staining-based light microscopy Cytotoxicity against human NCI/ADR-RES cells assessed as growth inhibition after 96 hrs by Giemsa staining-based light microscopy	[PMID: 25025991]
NCI/ADR-RES	IC₅₀	5000 nM Compound: VRB	Growth inhibition of doxorubicin-resistant human NCI-ADR-RES cells overexpressing P-glycoprotein after 96 hrs Growth inhibition of doxorubicin-resistant human NCI-ADR-RES cells overexpressing P-glycoprotein after 96 hrs	[PMID: 22044164]
NCI-H1299	IC₅₀	0.23 μM Compound: Vinorelbine	Cytotoxicity against human NCI-H1299 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay Cytotoxicity against human NCI-H1299 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay	[PMID: 33588178]
NCI-H1975	IC₅₀	0.008 μM Compound: Vinorelbine	Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 32473523]
NCI-H460	IC₅₀	43.7 nM Compound: Vinorelbine	Antiproliferative activity against human NCI-H460 cells after 72 hrs by sulforhodamine B assay Antiproliferative activity against human NCI-H460 cells after 72 hrs by sulforhodamine B assay	[PMID: 21480626]
NCI-H661	IC₅₀	0.12 μM Compound: Vinorelbine	Cytotoxicity against human NCI-H661 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay Cytotoxicity against human NCI-H661 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay	[PMID: 33588178]
OVCAR-8	IC₅₀	300 nM Compound: VRB	Cytotoxicity against human OVCAR8 cells assessed as growth inhibition after 48 hrs by SRB assay Cytotoxicity against human OVCAR8 cells assessed as growth inhibition after 48 hrs by SRB assay	[PMID: 26132075]
OVCAR-8	IC₅₀	300 nM Compound: VRB	Growth inhibition of human OVCAR8 cells after 96 hrs by trypan blue exclusion assay Growth inhibition of human OVCAR8 cells after 96 hrs by trypan blue exclusion assay	[PMID: 29730191]
OVCAR-8	IC₅₀	300 nM Compound: VRB	Cytotoxicity against human OVCAR8 cells assessed as growth inhibition by trypan blue exclusion assay Cytotoxicity against human OVCAR8 cells assessed as growth inhibition by trypan blue exclusion assay	[PMID: 23214452]
OVCAR-8	IC₅₀	300 nM Compound: VRB	Cytotoxicity against human OVCAR8 cells assessed as growth inhibition after 96 hrs by Giemsa staining-based light microscopy Cytotoxicity against human OVCAR8 cells assessed as growth inhibition after 96 hrs by Giemsa staining-based light microscopy	[PMID: 25025991]
OVCAR-8	IC₅₀	300 nM Compound: VRB	Growth inhibition of human OVCAR8 cells overexpressing P-glycoprotein after 96 hrs Growth inhibition of human OVCAR8 cells overexpressing P-glycoprotein after 96 hrs	[PMID: 22044164]
SK-OV-3	IC₅₀	26.7 nM Compound: Vinorelbine	Antiproliferative activity against human SKOV3 cells after 72 hrs by sulforhodamine B assay Antiproliferative activity against human SKOV3 cells after 72 hrs by sulforhodamine B assay	[PMID: 21480626]
SMMC-7721	IC₅₀	4.7 μM Compound: vinorelbine	Cytotoxicity against human SMMC7721 cells after 48 hrs by MTT assay Cytotoxicity against human SMMC7721 cells after 48 hrs by MTT assay	[PMID: 20462230]
SW480	IC₅₀	> 40 μM Compound: vinorelbine	Cytotoxicity against human SW480 cells after 48 hrs by MTT assay Cytotoxicity against human SW480 cells after 48 hrs by MTT assay	[PMID: 20462230]
U-87MG ATCC	IC₅₀	2 nM Compound: 7, VLN	Cytotoxicity against human U87MG cells after 72 hrs by resazurin assay Cytotoxicity against human U87MG cells after 72 hrs by resazurin assay	[PMID: 23822556]
U-87MG ATCC	IC₅₀	2 nM Compound: 4, VLN	Antiproliferative activity against human U87 cells after 72 hrs Antiproliferative activity against human U87 cells after 72 hrs	[PMID: 24871162]
U-87MG ATCC	IC₅₀	3.5 nM Compound: 3, VLN	Cytotoxicity against human U87 cells assessed as inhibition of cell proliferation after 72 hrs Cytotoxicity against human U87 cells assessed as inhibition of cell proliferation after 72 hrs	[PMID: 25804719]

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 p21^WAFI/CIP1 expression in androgen-dependent (AD) and- independent (AI) prostate cancer cell lines. Vinorelbine stimulates reporter genes in a concentration-dependent manner^[2].

MCE 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

778.93

Formula

C₄₅H₅₄N₄O₈

CAS 号

71486-22-1

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.

纯度 & 产品资料

产品使用指南 (1538 KB)

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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

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 at the owner's expense. MCE 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. [Content Brief] [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. [Content Brief] [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. [Content Brief] [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. [Content Brief]

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 at the owner's expense.

MCE 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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

Vinorelbine 相关分类

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Vinorelbine71486-22-1KW-2307 baseMicrotubule/TubulinAutophagyInhibitorinhibitorinhibit

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Vinorelbine (Synonyms: 长春瑞滨; KW-2307 base)

Other Forms of Vinorelbine:

MCE 顾客使用本产品发表的 14 篇科研文献

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参考文献

Vinorelbine 相关分类

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Vinorelbine (Synonyms: 长春瑞滨; KW-2307 base)

Other Forms of Vinorelbine:

Vinorelbine 相关抗体

MCE 顾客使用本产品发表的 14 篇科研文献

Vinorelbine 相关产品

•同靶点产品:

•同靶点蛋白产品:

生物活性

实验参考方法

纯度 & 产品资料

参考文献

Vinorelbine 相关抗体:

Vinorelbine 相关分类

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