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Combretastatin A4 Microtubule Associated inibitore

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

N. Cat.S7783

Combretastatin A4 è un agente che mira ai microtubulei e si lega alla β-tubulina con un K_d di 0,4 μM. Fase 3.

Combretastatin A4 Microtubule Associated inibitore Chemical Structure

Struttura chimica

Peso molecolare: 316.35

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Controllo Qualità

Lotto: S778301 DMSO]63 mg/mL]false]Ethanol]34 mg/mL]false]Water]Insoluble]false Purezza: 99.87%

Citato in Nature Medicine per la sua qualità superiore
COA
NMR
SDS
Scheda tecnica

99.87

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

Coltura cellulare, trattamento e concentrazione di lavoro

Linee cellulari	Tipo di saggio	Tempo di incubazione	Descrizione dellattività
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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Informazioni chimiche, conservazione e stabilità

Peso molecolare	316.35	Formula	C₁₈H₂₀O₅	Conservazione (Dalla data di ricezione)	3 anni-20°Cpolvere
N. CAS	117048-59-6	Scarica SDF		Conservazione delle soluzioni stock	1 anno-80°Cin solvente 1 mese-20°Cin solvente
Sinonimi	N/A			Smiles	COC1=C(C=C(C=C1)C=CC2=CC(=C(C(=C2)OC)OC)OC)O

Solubilità

In vitro
Lotto:

DMSO : 63 mg/mL (199.14 mM)
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

Ethanol : 34 mg/mL

Water : Insoluble

Calcolatore di Molarità

Massa	Concentrazione	Volume	Peso molecolare
=	×	×

Calcolatore di Diluizione Calcolatore del Peso Molecolare

In vivo Lotto:
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.

Calcolatore di formulazione in vivo (Soluzione chiara)

Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante lesperimento)

Dosaggio: mg/kg Peso medio degli animali: g Volume di dosaggio per animale:μL Numero di animali:

Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non cè una formulazione in vivo nella sezione Solubilità.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Risultati del calcolo:

Concentrazione di lavoro: mg/ml;

Metodo per preparare il liquido master di DMSO: mg farmaco predissolto in μL DMSO ( Concentrazione del liquido master mg/mL, Vi preghiamo di contattarci prima se la concentrazione supera la solubilità del DMSO del lotto del farmaco. )

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungereμL PEG300, mescolare e chiarire, quindi aggiungereμL Tween 80, mescolare e chiarire, quindi aggiungere μL ddH₂O, mescolare e chiarire.

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungere μL Olio di mais, mescolare e chiarire.

Nota: 1. Si prega di assicurarsi che il liquido sia limpido prima di aggiungere il solvente successivo.
2. Assicurarsi di aggiungere il/i solvente/i in ordine. È necessario assicurarsi che la soluzione ottenuta, nellaggiunta precedente, sia una soluzione limpida prima di procedere allaggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno dacqua calda possono essere utilizzati per facilitare la dissoluzione.

Meccanismo dazione

Targets/IC₅₀/Ki	β-tubulin 0.4 μM(Kd)
In vitro	Combretastatin A4 inibisce la crescita delle cellule MDA-MB-231, A549, Hela, HL-60, SF295, HCT-8, MDA-MB435, PC3M, OVCAR-8, NCI-H358M e linfocitarie con IC50 di 2,8, 3,8, 0,9, 2,1, 6,2, 5,3, 7,9, 4,7, 0,37, 8 e 3,2 nM, rispettivamente. 1 μM di questo composto inibisce la polimerizzazione della tubulina del 35%, e 10 μM bloccano quasi completamente la polimerizzazione della tubulina. Questa sostanza chimica dimostra una grande capacità di legame relativa, raggiungendo il 78% del legame della colchicina.
Saggio chinasico	Saggio di legame competitivo mediante LC-MS/MS
Saggio chinasico	La colchicina (1,2 μM) viene incubata con tubulina (1,3 mg/mL) nel tampone di incubazione (80 mM PIPES, 2,0 mM MgCl2, 0,5 mM EGTA, pH 6,9) a 37 °C per 1 h. Diverse concentrazioni (0,1 − 125 μM) di questo composto vengono utilizzate per competere con la colchicina originariamente legata alla tubulina. Dopo l'incubazione, si ottiene il filtrato. La capacità dell'analogo di inibire il legame della colchicina è espressa come percentuale del legame di controllo in assenza di qualsiasi competitore.
In vivo	Nel modello di tumore mammario NT2 e MDA-MB-231, la somministrazione di Combretastatin A4 (100 mg/kg, i.p.) induce una diminuzione significativa dei lipidi R1 e una riduzione della pO2 tumorale misurata mediante ossimetria a risonanza paramagnetica elettronica (EPR). Questo composto (100 mg/kg, i.p.) diminuisce significativamente la K^trans nei topi NMRI maschi.
Riferimenti	[1] https://pubmed.ncbi.nlm.nih.gov/24669888/ [2] https://pubmed.ncbi.nlm.nih.gov/25765253/ [3] https://pubmed.ncbi.nlm.nih.gov/25323069/

Supporto tecnico

Istruzioni per la manipolazione

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

Per qualsiasi altra domanda, si prega di lasciare un messaggio.

Domande Frequenti

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

Risposta:
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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