Vinblastine sulfate

Vinblastine sulfate inhibits microtubule formation and suppresses nAChR activity with IC50 of 8.9 μM in a cell-free assay, used to treat certain kinds of cancer. Vinblastine sulfate induces autophagy and apoptosis.

CAS No. 143-67-9

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
5mg	JPY 22000	国内在庫あり
25mg	JPY 55500	国内在庫あり
100mg	JPY 101500	国内在庫あり
1g	JPY 298500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

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製品安全説明書

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Antineoplastic and Immunosuppressive Antibiotics阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
rat REF52 cells	Function assay	0.1 μM	30 mins	Induction of microtubule depolymerization in rat REF52 cells at 0.1 uM after 30 mins by fluorescence assay	23947826
K562 cell	Proliferation assay		48 h	Antiproliferative activity against human K562 cells after 48 hrs, IC50=0.001 μM	19220018
ACHN cells	Cytotoxicity assay		48 h	Cytotoxicity against human ACHN cells after 48 hrs by SRB assay, IC50=22.7 μM	19467877
A375 cells	Cytotoxicity assay		48 h	Cytotoxicity against human A375 cells after 48 hrs by SRB assay, IC50=7.2 μM	19467877
C32 cells	Cytotoxicity assay		48 h	Cytotoxicity against human C32 cells after 48 hrs by SRB assay, IC50=3 μM	19467877
LNCAP cells	Cytotoxicity assay		48 h	Cytotoxicity against human LNCAP cells after 48 hrs by SRB assay, IC50=29.3 μM	19467877
Huh-7D12 cells	Cytotoxicity assay		48 h	Cytotoxicity against human Huh-7D12 cells after 48 hrs by SRB assay, IC50=45.6 μM	19467877
COR-L23 cells	Cytotoxicity assay		48 h	Cytotoxicity against human COR-L23 cells after 48 hrs by SRB assay, IC50=45.5 μM	19467877
142BR cells	Cytotoxicity assay		48 h	Cytotoxicity against human 142BR cells after 48 hrs by SRB assay, IC50=37.6 μM	19467877
HT-29 cells	Cytotoxicity assay		48 h	Cytotoxicity against human HT-29 cells after 48 hrs by MTS assay, IC50=0.55 μM	21920762
A549 cells	Proliferation assay		48 h	Antiproliferative activity against human A549 cells after 48 hrs by MTS assay, IC50=2.36 μM	22546674
DU145 cells	Proliferation assay		48 h	Antiproliferative activity against human DU145 cells after 48 hrs by MTS assay, IC50=4.25 μM	22546674
SK-MEL-5 cells	Proliferation assay		48 h	Antiproliferative activity against human SK-MEL-5 cells after 48 hrs by MTS assay, IC50=1.74 μM	22546674
HepG2 cells	Proliferation assay		48 h	Antiproliferative activity against human HepG2 cells after 48 hrs by MTS assay, IC50=0.16 μM	22546674
HT-29 cells	Proliferation assay		48 h	Antiproliferative activity against human HT-29 cells after 48 hrs by MTS assay, IC50=11.18 μM	22546674
MCF7 cells	Proliferation assay		48 h	Antiproliferative activity against human MCF7 cells after 48 hrs by MTS assay, IC50=24.08 μM	22546674
MDA-MB-231 cells	Proliferation assay		48 h	Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTS assay, IC50=31.52 μM	22546674
HepG2 cells	Cytotoxicity assay		72 h	Cytotoxicity against adriamycin-resistant human HepG2 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=0.056 μM	23708010
HepG2 cells	Cytotoxicity assay		72 h	Cytotoxicity against human HepG2 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=0.019 μM	23708010
K562 cells	Cytotoxicity assay		72 h	Cytotoxicity against human K562 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=0.016 μM	23708010
MDA-MB-231 cells	Cytotoxicity assay		72 h	Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=0.0083 μM	23708010
MCF7 cells	Cytotoxicity assay		72 h	Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=0.007 μM	23708010
UACC903 cells	Cytotoxicity assay		48 h	Cytotoxicity against human UACC903 cells after 48 hrs by MTS assay, IC50=1.65 μM	21920762
BxPC3 cells	Proliferation assay		48 h	Antiproliferative activity against human BxPC3 cells after 48 hrs by MTS assay, IC50=1.13 μM	22546674
COLO 320 human colorectal carcinoma cell line	Function assay			In vitro concentration required to kill 50% of COLO 320 human colorectal carcinoma cell line, EC50=0.08 μM	12361397
LNCaP human prostate cancer cell line	Function assay			In vitro concentration required to kill 50% of LNCaP human prostate cancer cell line, EC50=0.5 μM	12361397
K562 cell	Growth inhibition assay			In vitro inhibitory concentration against human chronic myelogenous leukemia K562 cell growth, IC50=0.001 μM	12852768
T47D cells	Function assay			In vitro concentration required to kill 50% of T47D human breast ductal carcinoma cell line, EC50=0.08 μM	12361397
SCL6 cells	Cytotoxicity assay			Cytotoxicity against human SCL6 cells by MTT assay, ED50=6.1 Μm	12880314
SCL9	Cytotoxicity assay			Cytotoxicity against human SCL9 cells by MTT assay, ED=5.3 μM	12880314
KATO III cells	Cytotoxicity assay			Cytotoxicity against human KATO III cells by MTT assay, ED50=6.1 μM	12880314
NUGC4 cells	Cytotoxicity assay			Cytotoxicity against human NUGC4 cells by MTT assay, ED50=5.3 μM	12880314
K562 cells	Function assay			Inhibition of tubulin polymerization in human K562 cells, IC50=0.13 μM	20546980
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生物活性

製品説明

Vinblastine sulfate inhibits microtubule formation and suppresses nAChR activity with IC50 of 8.9 μM in a cell-free assay, used to treat certain kinds of cancer. Vinblastine sulfate induces autophagy and apoptosis.

Targets

nAChR ^[1]
(Adrenal Chromaffin Cells)

8.9 μM

In Vitro
In vitro	The average terminal half-lives of Vinblastine is 14.3 h. When incubated in freshly isolated rat hepatocytes, VLB penetrates rapidly and intensely into the cells, probably through a passive diffusion mechanism followed by tight cellular binding^[3]. Vinblastine inhibits the angiogenic response induced by adrenomedullin and is also positive for mitotic slippage, causing micronuclei in mononucleate cells with cytokinesis block^[4]. vinblastine gives significant increase in micronucleated mononucleated cells at concentrations that produced approximately 50% cell death and cytostasis or less as calculated using RPD, RICC and RCC^[2].
細胞実験	細胞株	Chinese hamster ovary (CHO) cells
	濃度	1% (v/v) (dissolved in DMSO)
	反応時間	3h
	実験の流れ	Six-well treatment plates are set up that contained 5 × 10⁴ cells/mL in each well, suspended in 3 mL culture medium, and these are treated with vinblastine for 3 h followed by 21 h growth.
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	GRP78 p-eIF2 p-JNK / c-Caspase-7 / c-PARP ERK / p-ERK / Mcl-1 / Bad / Bid / Noxa		19674193
	Immunofluorescence	α-tubulin / Acetyl tubulin		30120268
	Growth inhibition assay	Cell viability		27114800

In Vivo
In Vivo	Vinblastine is a widely used anticancer drug with undesired side effects ^[6]. A combination of VBL and RAP at very low doses against human HCC gets a satisfactory antiangiogenic effect in vivo^[4]. The clinically relevant dose of vinblastine inhibits palmitoylation of tubulin in vivo in CEM cells (effect on depalmitoylation of tubulin)^[5].

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT02840409	Recruiting	Low Grade Glioma	The Hospital for Sick Children\|Hoffmann-La Roche	August 2016	Phase 2

参考
[1] McKay DB, et al. Proc Soc Exp Biol Med. 1993, 203(3):372-376. [2] George E. Johnson, et al. Mutat Res. 2010, 702(2):189-192. [3] Zhou XJ, et al. Eur J Drug Metab Pharmacokinet. 1990, 15(4):323-332. [4] Ribatti D, et al. Oncogene. 2003, 22(41):6458-6461. [5] Joan M. Caron, et al. Chemotherapy. 2007, 53:51-58. + 展開

参考

+ 展開

化学情報

分子量	909.05	化学式	C₄₆H₅₈N₄O₉.H₂SO₄
CAS No.	143-67-9	SDF	Download Vinblastine sulfate SDFをダウンロードする
Smiles	CCC1(CC2CC(C3=C(CCN(C2)C1)C4=CC=CC=C4N3)(C5=C(C=C6C(=C5)C78CCN9C7C(C=CC9)(C(C(C8N6C)(C(=O)OC)O)OC(=O)C)CC)OC)C(=O)OC)O.OS(=O)(=O)O
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 100 mg/mL ( (110.0 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : 50 mg/mL

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

C1=C0/X	C1:	LOG(C1):
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C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):