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Combretastatin A4 Microtubule Associated Inhibitor

Name: Combretastatin A4
Brand: Selleck Chemicals
SKU: S7783
Rating: 5 (7 reviews)

Kat.-Nr.S7783

Combretastatin A4 ist ein microtubule-Targeting-Wirkstoff, der β-Tubulin mit einem K_d von 0,4 μM bindet. Phase 3.

Combretastatin A4 Microtubule Associated Inhibitor Chemical Structure

Chemische Struktur

Molekulargewicht: 316.35

Springe zu

Qualitätskontrolle

Charge: S778301 DMSO]63 mg/mL]false]Ethanol]34 mg/mL]false]Water]Insoluble]false Reinheit: 99.87%

In Nature Medicine für seine erstklassige Qualität zitiert
COA
NMR
SDS
Datenblatt

99.87

Verwandte Ziele	Akt Wnt/beta-catenin PKC HSP ROCK Integrin Bcr-Abl Actin FAK Kinesin
Weitere Microtubule Associated Inhibitoren	Nocodazole MMAF Patupilone (Epothilone B) Lexibulin (CYT997) CW069 Epothilone A ABT-751 (E7010) TAI-1 Cucurbitacin B INH1

Zellkultur, Behandlung & Arbeitskonzentration

Zelllinien	Assay-Typ	Inkubationszeit	Aktivitätsbeschreibung
SKMEL-5	Growth inhibition assay		Cytotoxic concentration required to inhibit 50% cell growth in SKMEL-5 melanoma cell lines, ED50=3.00E-08 μM
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
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
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
MLM melanoma cell	Growth inhibition assay		Cytotoxic concentration required to inhibit 50% cell growth in MLM melanoma cell lines, ED50=1.40E-06 μM
M14	Cytotoxicity assay		In vitro cytotoxic activity was tested against human melanoma cancer (M14) cell line, GI50=0.0001 μM
SK-OV3	Cytotoxicity assay		In vitro cytotoxic activity tested against human ovarian cancer (SK-OV3) cell line, GI50=0.0001 μM
HL60 cells	Cytotoxicity assay	72 h	Cytotoxicity against human HL60 cells after 72 hrs by MTT assay, IC50=0.0001 μM
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
HepG2 cells	Cytotoxicity assay		Cytotoxicity against human HepG2 cells, IC50=0.00014 μM
ZR-75-1	Cytotoxicity assay		Cytotoxicity against ZR-75-1 cell line, IC50=0.00024 μM
HeLa cell	Cytotoxicity assay		Cytotoxicity against HeLa cell line, IC50=0.0003 μM
HCT116 cell	Cytotoxicity assay		Cytotoxicity against HCT116 cell line, IC50=0.00035 μM
KBV1 cells	Cytotoxicity assay	72 h	Cytotoxicity against human vinblastine-resistant KBV1 cells after 72 hrs by MTT assay, IC50=0.0004 μM
SKOV3	Cytotoxicity assay		Cytotoxicity against human SKOV3 cells by SRB assay, GI50=0.00042 μM
SKOV3 cells	Growth inhibition assay		Growth inhibition of human SKOV3 cells by sulforhodamine B assay, GI50=0.00042 μM
HeLa cells	Cytotoxicity assay		Cytotoxicity against human HeLa cells by MTT assay, IC50=0.00051 μM
DU145 cells	Cytotoxicity assay		Cytotoxicity against human DU145 cells by SRB assay, GI50=0.00054 μM
DU145 cells	Growth inhibition assay		Growth inhibition of human DU145 cells by sulforhodamine B assay, GI50=0.00054 μM
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
NCIH460 cells	Cytotoxicity assay	48 h	Cytotoxicity against human NCIH460 cells after 48 hrs by SRB assay, GI50=0.0006 μM
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
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
DU145 cells	Cytotoxicity assay	48 h	Cytotoxicity against human DU145 cells after 48 hrs by SRB assay, GI50=0.0008 μM
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
HCT 116	Growth inhibition assay		Concentration which produces 50% inhibition of growth of human colon tumor HCT 116, IC50=0.0009 μM
HeLa cells	Cytotoxicity assay	72 h	Cytotoxicity against human HeLa cells after 72 hrs by resazurin based fluorescence assay, IC50=0.0009 μM
BNL 1ME A.7R.1 cells	Cytotoxicity assay		Cytotoxicity against mouse BNL 1ME A.7R.1 cells, IC50=0.0009 μM
Calu6	Proliferation assay	48 h	Antiproliferative activity against human Calu6 after 48 hrs by spectrophotometry, IC50=0.00094 μM
melanoma B16 cell	Growth inhibition assay		Concentration which produces 50% inhibition of growth of murine melanoma B16 cell line, IC50=0.001 μM
DU145 cells	Cytotoxicity assay		Cytotoxicity against human DU145 cells by SRB assay, GI50=0.001 μM
HCT116 cells	Proliferation assay	72 h	Antiproliferative activity against human HCT116 cells after 72 hrs by MTS assay, IC50=0.001 μM
HCT15 cells	Proliferation assay	72 h	Antiproliferative activity against human HCT15 cells after 72 hrs by MTS assay, IC50=0.001 μM
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
A10 cells	Growth inhibition assay	48 h	Growth inhibition of rat A10 cells after 48 hrs by MTT assay, IC50=0.001 μM
HUVEC cells	Growth inhibition assay	48 h	Growth inhibition of HUVEC cells after 48 hrs by MTT assay, IC50=0.001 μM
HL60 cells	Cytotoxicity assay	72 h	Cytotoxicity against human HL60 cells after 72 hrs by MTT assay, IC50=0.001 μM
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
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
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
OVCAR3	Growth inhibition assay	48 h	Growth inhibition of human OVCAR3 cells after 48 hrs by SRB assay, GI50=0.001 μM
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
PC3 cells	Growth inhibition assay	48 h	Growth inhibition of human PC3 cells after 48 hrs by SRB assay, GI50=0.001 μM
DU145 cells	Growth inhibition assay	48 h	Growth inhibition of human DU145 cells after 48 hrs by SRB assay, GI50=0.001 μM
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
CEM cells	Cytotoxicity assay	72 h	Cytotoxicity against human CEM cells after 72 hrs by MTT assay, IC50=0.001 μM
HCT116 cells	Cytotoxicity assay	72 h	Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay, IC50=0.001 μM
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
HaCaT cells	Proliferation assay		Antiproliferative activity against human HaCaT cells assessed as cell viability by MTT assay, IC50=0.001 μM
HL60 cells	Proliferation assay	72 h	Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay, IC50=0.001 μM
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
HT-29	Growth inhibition assay		Growth inhibition of human HT-29 cells by MTT assay, IC50=0.001 μM
HL60 cells	Proliferation assay	72 h	Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay, IC50=0.001 μM
Hs578T cells	Growth inhibition assay	48 h	Growth inhibition of human Hs578T cells after 48 hrs by SRB assay, GI50=0.001 μM
HL60 cells	Cytotoxicity assay	72 h	Cytotoxicity against human HL60 cells after 72 hrs by MTT assay, IC50=0.001 μM
SKOV3 cells	Growth inhibition assay		Growth inhibition of human SKOV3 cells by MTT assay, IC50=0.001 μM
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
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
H460	Cytotoxicity assay		Cytotoxicity against human H460 cells by sulforhodamine B test, IC50=0.0012 μM
H460	Proliferation assay		Antiproliferative activity against human H460 cells, IC50=0.00124 μM
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
OVCAR8 cells	Growth inhibition assay	96 h	Growth inhibition of human OVCAR8 cells overexpressing P-glycoprotein after 96 hrs, IC50=0.0013 μM
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
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
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
OVCAR8 cells	Cytotoxicity assay		Cytotoxicity against human OVCAR8 cells assessed as growth inhibition by trypan blue exclusion assay, IC50=0.0013 μM
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
K562 cells	Cytotoxicity assay		Cytotoxicity against human K562 cells, IC50=0.0014 μM
NCI/ADR (MDR) cells	Function assay		Cell cycle arrest in NCI/ADR (MDR) cells by accumulation at G2/M phase, IC50=0.0015 μM
HUVEC	Proliferation assay		Antiproliferative activity against human HUVEC, IC50=0.0015 μM
KB cell	Proliferation assay		Antiproliferative activity against human KB cell line by methylene blue dye assay, IC50=0.0015 μM
KB-VIN10 cell	Proliferation assay		Antiproliferative activity against human KB-VIN10 cell line by methylene blue dye assay, IC50=0.0015 μM
Human SH-SY5Y neuroblastoma cells	Function assay		Inhibitory concentration against Human SH-SY5Y neuroblastoma cells, IC50=0.0015 μM
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
Molt4/C8 cells	Proliferation assay		Antiproliferative activity against human Molt4/C8 cells, IC50=0.0016 μM
ACHN cell	Proliferation assay		Antiproliferative activity against drug resistant ACHN cell line expressing MDR1 by Alamar Blue assay, IC50=0.0016 μM
Molt4/C8 cells	Proliferation assay	3 days	Antiproliferative effect against human Molt4/C8 cells after 3 days, IC50=0.0016 μM
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Chemische Informationen, Lagerung & Stabilität

Molekulargewicht	316.35	Formel	C₁₈H₂₀O₅	Lagerung (Ab dem Eingangsdatum)	3 Jahre-20°CPulver
CAS-Nr.	117048-59-6	SDF herunterladen		Lagerung von Stammlösungen	1 Jahr-80°Cin Lösungsmittel 1 Monat-20°Cin Lösungsmittel
Synonyme	N/A			Smiles	COC1=C(C=C(C=C1)C=CC2=CC(=C(C(=C2)OC)OC)OC)O

Löslichkeit

In vitro
Charge:

DMSO : 63 mg/mL (199.14 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Ethanol : 34 mg/mL

Water : Insoluble

Molaritätsrechner

Masse	Konzentration	Volumen	Molekulargewicht
=	×	×

Verdünnungsrechner Molekulargewichtsrechner

In vivo Charge:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In-vivo-Formulierungsrechner (Klare Lösung)

Schritt 1: Geben Sie die untenstehenden Informationen ein (Empfohlen: Ein zusätzliches Tier zur Berücksichtigung von Verlusten während des Experiments)

Dosierung: mg/kg Durchschnittsgewicht der Tiere: g Dosiervolumen pro Tier:μL Anzahl der Tiere:

Schritt 2: Geben Sie die In-vivo-Formulierung ein (Dies ist nur der Rechner, keine Formulierung. Bitte kontaktieren Sie uns zuerst, wenn es im Abschnitt "Löslichkeit" keine In-vivo-Formulierung gibt.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berechnungsergebnisse:

Arbeitskonzentration: mg/ml;

Methode zur Herstellung der DMSO-Stammlösung: mg Wirkstoff vorgelöst in μL DMSO ( Konzentration der Stammlösung mg/mL, Bitte kontaktieren Sie uns zuerst, wenn die Konzentration die DMSO-Löslichkeit der Wirkstoffcharge überschreitet. )

Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügenμL PEG300, mischen und klären, dann hinzufügenμL Tween 80, mischen und klären, dann hinzufügen μL ddH₂O, mischen und klären.

Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügen μL Maisöl, mischen und klären.

Hinweis: 1. Bitte stellen Sie sicher, dass die Flüssigkeit klar ist, bevor Sie das nächste Lösungsmittel hinzufügen.
2. Achten Sie darauf, das/die Lösungsmittel der Reihe nach hinzuzufügen. Sie müssen sicherstellen, dass die bei der vorherigen Zugabe erhaltene Lösung eine klare Lösung ist, bevor Sie mit der Zugabe des nächsten Lösungsmittels fortfahren. Physikalische Methoden wie Vortex, Ultraschall oder ein heißes Wasserbad können zur Unterstützung des Lösens verwendet werden.

Wirkmechanismus

Targets/IC₅₀/Ki	β-tubulin 0.4 μM(Kd)
In vitro	Combretastatin A4 hemmt das Wachstum von MDA-MB-231-, A549-, Hela-, HL-60-, SF295-, HCT-8-, MDA-MB435-, PC3M-, OVCAR-8-, NCI-H358M- und Lymphozytenzellen mit IC50-Werten von 2,8, 3,8, 0,9, 2,1, 6,2, 5,3, 7,9, 4,7, 0,37, 8 bzw. 3,2 nM. 1 μM dieser Verbindung hemmt die Tubulinpolymerisation um 35 %, und 10 μM blockieren die Tubulinpolymerisation nahezu vollständig. Diese Chemikalie zeigt eine große relative Bindungskapazität, die 78 % der Colchicinbindung erreicht.
Kinase-Assay	Kompetitiver Bindungsassay mittels LC-MS/MS
Kinase-Assay	Colchicin (1,2 μM) wird mit Tubulin (1,3 mg/mL) in Inkubationspuffer (80 mM PIPES, 2,0 mM MgCl2, 0,5 mM EGTA, pH 6,9) bei 37 °C für 1 h inkubiert. Unterschiedliche Konzentrationen (0,1 − 125 μM) dieser Verbindung werden verwendet, um mit Colchicin zu konkurrieren, das ursprünglich an Tubulin gebunden war. Nach der Inkubation wird das Filtrat erhalten. Die Fähigkeit des Analogons, die Bindung von Colchicin zu hemmen, wird als Prozentsatz der Kontrollbindung in Abwesenheit eines beliebigen Konkurrenten ausgedrückt.
In vivo	Im NT2- und MDA-MB-231-Mammakarzinommodell induziert die Verabreichung von Combretastatin A4 (100 mg/kg, i.p.) eine signifikante Abnahme der Lipide R1 und eine Reduktion des Tumor-pO2, gemessen mittels Elektronenparamagnetischer Resonanz (EPR)-Oximetrie. Diese Verbindung (100 mg/kg, i.p.) verringert signifikant das K^trans bei männlichen NMRI-Mäusen.
Literatur	[1] https://pubmed.ncbi.nlm.nih.gov/24669888/ [2] https://pubmed.ncbi.nlm.nih.gov/25765253/ [3] https://pubmed.ncbi.nlm.nih.gov/25323069/

Technischer Support

Handhabungshinweise

Tel: +1-832-582-8158 Ext:3

Wenn Sie weitere Fragen haben, hinterlassen Sie bitte eine Nachricht.

Häufig gestellte Fragen

Frage 1:
How to make solution for in vivo IP injection of it?

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

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