Combretastatin A4

製品コード：S7783 純度：99.87%

Combretastatin A4 is a microtubule-targeting agent that binds β-tubulin with K_d of 0.4 μM.Phase 3.

CAS No. 117048-59-6

サイズ	価格(税別)	在庫状況
10mg	JPY 22000	国内在庫あり
50mg	JPY 59500	国内在庫あり

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

文献中Selleckの製品使用例（5）

製品安全説明書

現在のバッチを見る： S778301 DMSO] 63 mg/mL] false] Ethanol] 34 mg/mL] false] Water] Insoluble] false 純度： 99.87%

99.87

Combretastatin A4関連製品

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シグナル伝達経路

Microtubule Associatedシグナル伝達経路

Microtubule Associated阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Incubation Time	活性情報	PMID
HL60 cells	Cytotoxicity assay	72 h	Cytotoxicity against human HL60 cells after 72 hrs by MTT assay, IC50=0.0001 μM	20731355
SK-OV-3	Growth inhibition assay	48 h	Growth inhibition of human SK-OV-3 after 48 hrs by SRB assay, GI50=0.00013 μM	18722127
KBV1 cells	Cytotoxicity assay	72 h	Cytotoxicity against human vinblastine-resistant KBV1 cells after 72 hrs by MTT assay, IC50=0.0004 μM	20731355
SK-N-BE	Proliferation assay	72 h	Antiproliferative activity in human SK-N-BE cells assessed as cell viability after 72 hrs by MTT assay, IC50=0.00058 μM	22329561
NCIH460 cells	Cytotoxicity assay	48 h	Cytotoxicity against human NCIH460 cells after 48 hrs by SRB assay, GI50=0.0006 μM	18303849
KB-VIN10 cells	Proliferation assay	72 h	Antiproliferative activity against human KB-VIN10 cells over-expressing P-gp 170/MDR1 after 72 hrs by methylene blue assay, IC50=0.0007 μM	21641700
HCT116 cells	Cytotoxicity assay	72 h	Cytotoxicity against human HCT116 cells assessed as reduction of [3H]thymidine incorporation after 72 hrs by scintillation counting, IC50=0.00074 μM	21955454
DU145 cells	Cytotoxicity assay	48 h	Cytotoxicity against human DU145 cells after 48 hrs by SRB assay, GI50=0.0008 μM	18303849
RS4:11 cells	Proliferation assay	72 h	Antiproliferative activity against human RS4:11 cells after 72 hrs by (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide test, IC50=0.0008 μM	25785605
HeLa cells	Cytotoxicity assay	72 h	Cytotoxicity against human HeLa cells after 72 hrs by resazurin based fluorescence assay, IC50=0.0009 μM	24669888
Calu6	Proliferation assay	48 h	Antiproliferative activity against human Calu6 after 48 hrs by spectrophotometry, IC50=0.00094 μM	21774499
HCT116 cells	Proliferation assay	72 h	Antiproliferative activity against human HCT116 cells after 72 hrs by MTS assay, IC50=0.001 μM	21112130
HCT15 cells	Proliferation assay	72 h	Antiproliferative activity against human HCT15 cells after 72 hrs by MTS assay, IC50=0.001 μM	21112130
HL60 cells	Proliferation assay	72 h	Antiproliferative activity against human HL60 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=0.001 μM	21663319
A10 cells	Growth inhibition assay	48 h	Growth inhibition of rat A10 cells after 48 hrs by MTT assay, IC50=0.001 μM	22044164
HUVEC cells	Growth inhibition assay	48 h	Growth inhibition of HUVEC cells after 48 hrs by MTT assay, IC50=0.001 μM	22044164
HL60 cells	Cytotoxicity assay	72 h	Cytotoxicity against human HL60 cells after 72 hrs by MTT assay, IC50=0.001 μM	22136312
HL60 cells	Proliferation assay	72 h	Antiproliferative activity against human HL60 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=0.001 μM	22578111
NCI-H522 cells	Growth inhibition assay	48 h	Growth inhibition of human NCI-H522 cells after 48 hrs by SRB assay, GI50=0.001 μM	22982122
MDA-MB-435 cells	Growth inhibition assay	48 h	Growth inhibition of human MDA-MB-435 cells after 48 hrs by SRB assay, GI50=0.001 μM	22982122
OVCAR3	Growth inhibition assay	48 h	Growth inhibition of human OVCAR3 cells after 48 hrs by SRB assay, GI50=0.001 μM	22982122
NCI/ADR-RES cells	Growth inhibition assay	48 h	Growth inhibition of human NCI/ADR-RES cells after 48 hrs by SRB assay, GI50=0.001 μM	22982122
PC3 cells	Growth inhibition assay	48 h	Growth inhibition of human PC3 cells after 48 hrs by SRB assay, GI50=0.001 μM	22982122
DU145 cells	Growth inhibition assay	48 h	Growth inhibition of human DU145 cells after 48 hrs by SRB assay, GI50=0.001 μM	22982122
MDA-MB-231 cells	Growth inhibition assay	48 h	Growth inhibition of human MDA-MB-231 cells after 48 hrs by SRB assay, GI50=0.001 μM	22982122
CEM cells	Cytotoxicity assay	72 h	Cytotoxicity against human CEM cells after 72 hrs by MTT assay, IC50=0.001 μM	22676247
HCT116 cells	Cytotoxicity assay	72 h	Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay, IC50=0.001 μM	22676247
MDA-MB-435 cells	Cytotoxicity assay	72 h	Cytotoxicity against human MDA-MB-435 cells after 72 hrs by MTT assay, IC50=0.001 μM	22676247
HL60 cells	Proliferation assay	72 h	Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay, IC50=0.001 μM	23117171
HL60 cells	Proliferation assay	72 h	Antiproliferative activity against human HL60 cells after 72 hrs by (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide test, IC50=0.001 μM	25785605
HL60 cells	Proliferation assay	72 h	Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay, IC50=0.001 μM	20420439
Hs578T cells	Growth inhibition assay	48 h	Growth inhibition of human Hs578T cells after 48 hrs by SRB assay, GI50=0.001 μM	22982122
HL60 cells	Cytotoxicity assay	72 h	Cytotoxicity against human HL60 cells after 72 hrs by MTT assay, IC50=0.001 μM	23445496
MDA-MB-468 cells	Cytotoxicity assay	4 days	Cytotoxicity against human MDA-MB-468 cells assessed as cell viability after 4 days by MTS assay, IC50=0.0011 μM	24210503
MCF7 cells	Proliferation assay	72 h	Antiproliferative activity in human MCF7 cells assessed as cell viability after 72 hrs by MTT assay, IC50=0.00111 μM	22329561
NCI-H460 cells	Cytotoxicity assay	72 h	Cytotoxic activity against human NCI-H460 cells after 72 hrs by sulforhodamine B test, IC50=0.0013 μM	18396857
OVCAR8 cells	Growth inhibition assay	96 h	Growth inhibition of human OVCAR8 cells overexpressing P-glycoprotein after 96 hrs, IC50=0.0013 μM	22044164
OVCAR8 cells	Cytotoxicity assay	96 h	Cytotoxicity against human OVCAR8 cells assessed as growth inhibition after 96 hrs by Giemsa staining-based light microscopy, IC50=0.0013 μM	25025991
NCI/ADR-RES cells	Cytotoxicity assay	96 h	Cytotoxicity against human NCI/ADR-RES cells assessed as growth inhibition after 96 hrs by Giemsa staining-based light microscopy, IC50=0.0013 μM	25025991
HuTu 80 cells	Proliferation assay	72 h	Antiproliferative activity in human HuTu 80 cells assessed as cell viability after 72 hrs by MTT assay, IC50=0.00137 μM	22329561
SW620 cells	Proliferation assay	72 h	Antiproliferative activity in human SW620 cells assessed as cell viability after 72 hrs by MTT assay, IC50=0.00152 μM	22329561
Molt4/C8 cells	Proliferation assay	3 days	Antiproliferative effect against human Molt4/C8 cells after 3 days, IC50=0.0016 μM	17419607
SKMEL-5	Growth inhibition assay		Cytotoxic concentration required to inhibit 50% cell growth in SKMEL-5 melanoma cell lines, ED50=3.00E-08 μM	1875350
A-549	Growth inhibition assay		Cytotoxic concentration required to inhibit 50% cell growth in A-549 lung carcinoma cell lines, ED50=1.20E-06 μM	1875350
MCF-7	Growth inhibition assay		Cytotoxic concentration required to inhibit 50% cell growth in MCF-7 breast carcinoma cell lines, ED50=3.80E-06 μM	1875350
HT-29	Growth inhibition assay		Cytotoxic concentration required to inhibit 50% cell growth in HT-29 colon adenocarcinoma cell lines, ED50=1.20E-06 μM	1875350
MLM melanoma cell	Growth inhibition assay		Cytotoxic concentration required to inhibit 50% cell growth in MLM melanoma cell lines, ED50=1.40E-06 μM	1875350
M14	Cytotoxicity assay		In vitro cytotoxic activity was tested against human melanoma cancer (M14) cell line, GI50=0.0001 μM	12729640
SK-OV3	Cytotoxicity assay		In vitro cytotoxic activity tested against human ovarian cancer (SK-OV3) cell line, GI50=0.0001 μM	12729640
HepG2 cells	Cytotoxicity assay		Cytotoxicity against human HepG2 cells, IC50=0.00014 μM	17127061
ZR-75-1	Cytotoxicity assay		Cytotoxicity against ZR-75-1 cell line, IC50=0.00024 μM	17249649
HeLa cell	Cytotoxicity assay		Cytotoxicity against HeLa cell line, IC50=0.0003 μM	17249649
HCT116 cell	Cytotoxicity assay		Cytotoxicity against HCT116 cell line, IC50=0.00035 μM	17249649
SKOV3	Cytotoxicity assay		Cytotoxicity against human SKOV3 cells by SRB assay, GI50=0.00042 μM	24016002
SKOV3 cells	Growth inhibition assay		Growth inhibition of human SKOV3 cells by sulforhodamine B assay, GI50=0.00042 μM	23772309
HeLa cells	Cytotoxicity assay		Cytotoxicity against human HeLa cells by MTT assay, IC50=0.00051 μM	19879758
DU145 cells	Cytotoxicity assay		Cytotoxicity against human DU145 cells by SRB assay, GI50=0.00054 μM	24016002
DU145 cells	Growth inhibition assay		Growth inhibition of human DU145 cells by sulforhodamine B assay, GI50=0.00054 μM	23772309
HCT 116	Growth inhibition assay		Concentration which produces 50% inhibition of growth of human colon tumor HCT 116, IC50=0.0009 μM	11714613
BNL 1ME A.7R.1 cells	Cytotoxicity assay		Cytotoxicity against mouse BNL 1ME A.7R.1 cells, IC50=0.0009 μM	25785605
melanoma B16 cell	Growth inhibition assay		Concentration which produces 50% inhibition of growth of murine melanoma B16 cell line, IC50=0.001 μM	11714613
DU145 cells	Cytotoxicity assay		Cytotoxicity against human DU145 cells by SRB assay, GI50=0.001 μM	20496923
HaCaT cells	Proliferation assay		Antiproliferative activity against human HaCaT cells assessed as cell viability by MTT assay, IC50=0.001 μM	23063401
HT-29	Growth inhibition assay		Growth inhibition of human HT-29 cells by MTT assay, IC50=0.001 μM	25689111
SKOV3 cells	Growth inhibition assay		Growth inhibition of human SKOV3 cells by MTT assay, IC50=0.001 μM	25689111
H460	Cytotoxicity assay		Cytotoxicity against human H460 cells by sulforhodamine B test, IC50=0.0012 μM	18783207
H460	Proliferation assay		Antiproliferative activity against human H460 cells, IC50=0.00124 μM	16722633
NCI/ADR-RES cells	Cytotoxicity assay		Cytotoxicity against human NCI/ADR-RES cells assessed as growth inhibition by trypan blue exclusion assay, IC50=0.0013 μM	23214452
OVCAR8 cells	Cytotoxicity assay		Cytotoxicity against human OVCAR8 cells assessed as growth inhibition by trypan blue exclusion assay, IC50=0.0013 μM	23214452
K562 cells	Cytotoxicity assay		Cytotoxicity against human K562 cells, IC50=0.0014 μM	19837594
NCI/ADR (MDR) cells	Function assay		Cell cycle arrest in NCI/ADR (MDR) cells by accumulation at G2/M phase, IC50=0.0015 μM	16377187
HUVEC	Proliferation assay		Antiproliferative activity against human HUVEC, IC50=0.0015 μM	16722633
KB cell	Proliferation assay		Antiproliferative activity against human KB cell line by methylene blue dye assay, IC50=0.0015 μM	17034147
KB-VIN10 cell	Proliferation assay		Antiproliferative activity against human KB-VIN10 cell line by methylene blue dye assay, IC50=0.0015 μM	17034147
Human SH-SY5Y neuroblastoma cells	Function assay		Inhibitory concentration against Human SH-SY5Y neuroblastoma cells, IC50=0.0015 μM	15963722
Molt4/C8 cells	Proliferation assay		Antiproliferative activity against human Molt4/C8 cells, IC50=0.0016 μM	17034150
ACHN cell	Proliferation assay		Antiproliferative activity against drug resistant ACHN cell line expressing MDR1 by Alamar Blue assay, IC50=0.0016 μM	17286393
他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

生物活性

製品説明

Combretastatin A4 is a microtubule-targeting agent that binds β-tubulin with K_d of 0.4 μM.Phase 3.

Targets

β-tubulin ^[1]

0.4 μM(Kd)

In Vitro
In vitro	Combretastatin A4 inhibits the growth of MDA-MB-231, A549, Hela, HL-60, SF295, HCT-8, MDA-MB435, PC3M, OVCAR-8, NCI-H358M, and lymphocyte cells with IC50 of 2.8, 3.8, 0.9, 2.1, 6.2, 5.3, 7.9, 4.7, 0.37, 8, and 3.2 nM, respectively.^[1] ^[2] 1 μM Combretastatin A4 inhibits tubulin polymerization by 35%, and 10 μM nearly completely blocks tubulin polymerization. Combretastatin A4 demonstrates great relative binding capacity, reaching 78% of colchicine binding.^[1]
Kinase Assay	Competitive binding assay using LC-MS/MS
Kinase Assay	Colchicine (1.2 μ M) is incubated with tubulin (1.3 mg/mL) in the incubation buﬀer (80 mM PIPES, 2.0 mM MgCl2, 0.5 mM EGTA, pH 6.9) at 37℃ for 1 h. Varying concentrations (0.1 − 125 μ M) of Combretastatin A4 are used to compete with colchicine originally bound to tubulin. After incubation, the ﬁltrate is obtained. The ability of the analogue to inhibit the binding of colchicine is expressed as a percentage of control binding in the absence of any competitor.
細胞実験	細胞株	MDA-MB-231, A549, and Hela cells
	濃度	~3.8 nM
	反応時間	72 h
	実験の流れ	MDA-MB-231, A549, and HeLa cells are grown in DMEM medium (115 units/mL of penicillin G, 115 μg/mL of streptomycin, and 10% fetal bovine serum). Cells are seeded in 96-well plates (5000 cells/well) containing 50 μL of growth medium for 24 h. After medium removal, 100 μL of fresh medium containing individual analogue compounds at diﬀerent concentrations is added to each well and incubated at 37 ℃ for 72 h. After 24 h of culture, the cells are supplemented with 50 μL of analogue compounds dissolved in DMSO (less than 0.25% in each preparation). After 72 h of incubation, 20 μL of resazurin is added for 2 h before recording ﬂuorescence at 560 nm (excitation) and 590 nm (emission) using a Victor microtiter plate ﬂuorimeter. The IC50 is deﬁned as the compound concentration required to inhibit cell proliferation by 50% in comparison with cells treated with the maximum amount of DMSO (0.25%) and considered as 100% viability.

In Vivo
In Vivo	In NT2 and MDA-MB-231 mammary tumor model, administration of Combretastatin A4 (100 mg/kg, i.p.) induces a significant decrease in lipids R1 and a reduction in tumor pO2 measured by electron paramagnetic resonance (EPR) oximetry.^[2] Combretastatin A4 (100 mg/kg, i.p.) significant decreases the K^trans in male NMRI mice.^[3]
動物実験	動物モデル	FVB/N or nude NMRI female mice bearing NT2 and MDA-MB-231 tumors
	投与量	100 mg/kg
	投与経路	i.p.

参考
[1] Zheng S, et al. J Med Chem. 2014, 57(8), 3369-3381. [2] Colliez F, et al. Magn Reson Med. 2015, doi: 10.1002/mrm.25642. [3] Fruytier AC, et al. NMR Biomed. 2014, 27(11), 1403-1412.

参考

化学情報

分子量	316.35	化学式	C₁₈H₂₀O₅
CAS No.	117048-59-6	SDF	Download Combretastatin A4 SDFをダウンロードする
Smiles	COC1=C(C=C(C=C1)C=CC2=CC(=C(C(=C2)OC)OC)OC)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ケ月-20°Cin solvent

In vitro
Batch:

DMSO : 63 mg/mL ( (199.14 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。)

Ethanol : 34 mg/mL

Water : 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。

技術サポート

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Handling Instructions

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よくある質問（FAQ）

質問1:
How to make solution for in vivo IP injection?

回答
We've tested some vehicles for S7783 Combretastatin A4, and found it can be dissolved in 5% DMSO+50% PEG 300+ddH2O at 30mg/ml clearly. When prepare the solution, please dissolve the compound in DMSO clearly first. The add PEG, after they mixed well, then dilute with water.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
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):