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Nocodazole inibitore di Microtubule Depolymerization

Name: Nocodazole
Brand: Selleck Chemicals
SKU: S2775
Rating: 5 (130 reviews)

N. Cat.S2775

Nocodazole è un inibitore rapidamente reversibile della polimerizzazione dei microtubuli, inibisce anche Abl, Abl(E255K) e Abl(T315I) con IC50 di 0,21 μM, 0,53 μM e 0,64 μM in saggi senza cellule, rispettivamente. Nocodazole induce l'apoptosi.

Nocodazole Microtubule Associated inibitore Chemical Structure

Struttura chimica

Peso molecolare: 301.32

Vai a

Controllo Qualità

Lotto: Purezza: 99.80%

99.80

Target correlati	Akt Wnt/beta-catenin PKC HSP ROCK Integrin Bcr-Abl Actin FAK Kinesin
Altro Microtubule Associated Inibitori	MMAF Patupilone (Epothilone B) Lexibulin (CYT997) CW069 Combretastatin A4 Epothilone A ABT-751 (E7010) TAI-1 Cucurbitacin B INH1

Coltura cellulare, trattamento e concentrazione di lavoro

Linee cellulari	Tipo di saggio	Concentrazione	Tempo di incubazione	Descrizione dellattività	PMID
L1210 murine leukemia cell	Growth inhibition assay			In vitro for its inhibitory activity against L1210 murine leukemia cell growth, IC50=38 nM	1738146
LT12	Antiproliferative assay		48 hrs	Antiproliferative activity against rat LT12 cells after 48 hrs by XTT assay, IC50 = 0.006 μM.	19220018
HepG2	Function assay	0.1 to 10 uM	1 hr	Inhibition of TNFalpha-induced NFkappaB (unknown origin)-dependent transcriptional activity expressed in human HepG2 cells at 0.1 to 10 uM incubated for 1 hr prior to TNFalpha induction measured after 6 hrs by dual-luciferase reporter gene assay	25827522
PANC1	Antiproliferative assay		48 hrs	Antiproliferative activity against human PANC1 cells after 48 hrs by SRB assay, GI50 = 0.01 μM.	27688193
HeLa	Antiproliferative assay		48 hrs	Antiproliferative activity against human HeLa cells after 48 hrs by SRB assay, GI50 = 0.01 μM.	27688193
MDA-MB-231	Antiproliferative assay		48 hrs	Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by SRB assay, GI50 = 0.01 μM.	27688193
A549	Antiproliferative assay		48 hrs	Antiproliferative activity against human A549 cells after 48 hrs by SRB cell proliferation assay, GI50 = 0.01 μM.	29089233
HeLa	Antiproliferative assay		48 hrs	Antiproliferative activity against human HeLa cells after 48 hrs by SRB cell proliferation assay, GI50 = 0.01 μM.	29089233
MDA-MB-231	Antiproliferative assay		48 hrs	Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by SRB cell proliferation assay, GI50 = 0.01 μM.	29089233
HeLa	Antiproliferative assay		48 hrs	Antiproliferative activity against human HeLa cells after 48 hrs by SRB assay, GI50 = 0.015 μM.	25827522
MDA-MB-231	Antiproliferative assay		48 hrs	Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by SRB assay, GI50 = 0.017 μM.	25827522
A549	Antiproliferative assay		48 hrs	Antiproliferative activity against human A549 cells after 48 hrs by SRB assay, GI50 = 0.02 μM.	25827522
L1210	Function assay		48 hrs	Inhibitory concentration against proliferation of cultured lymphoid leukemia L1210 cells during 48 hrs, ID50 = 0.027 μM.	7131483
PANC1	Anticancer assay		48 hrs	Anticancer activity against human PANC1 cells after 48 hrs by SRB assay, GI50 = 0.029 μM.	27130357
A549	Cytotoxicity assay		24 hrs	Cytotoxicity against human A549 cells after 24 hrs by MTT assay, IC50 = 0.0366 μM.	20110137
NCI60	Growth inhibition assay		48 hrs	Growth inhibition of human NCI60 cells incubated for 48 hrs by sulforhodamine B assay, GI50 = 0.0389 μM.	27956038
P388	Antiproliferative assay		48 hrs	Antiproliferative activity against mouse P388 cells after 48 hrs by XTT assay, IC50 = 0.04 μM.	19220018
LT12	Antiproliferative assay		48 hrs	Antiproliferative activity against LT12 cells by XTT assay after 48 hrs, IC50 = 0.04 μM.	17181164
LT12	Antiproliferative assay		48 hrs	Antiproliferative activity against rat LT12 cells after 48 hrs by XTT assay, IC50 = 0.04 μM.	20537765
LT12	Antiproliferative assay		48 hrs	Antiproliferative activity against rat LT12 cells after 48 hrs by XTT assay, IC50 = 0.04 μM.	21705223
MDA-MB-231	Anticancer assay		48 hrs	Anticancer activity against human MDA-MB-231 cells after 48 hrs by SRB assay, GI50 = 0.042 μM.	27130357
L1210	Antiproliferative assay		48 hrs	Antiproliferative activity against L1210 cells by XTT assay after 48 hrs, IC50 = 0.05 μM.	17181164
P388	Antiproliferative assay		48 hrs	Antiproliferative activity against mouse adriamycin-resistant P388 cells after 48 hrs by XTT assay, IC50 = 0.05 μM.	17973361
L12	Antiproliferative assay		48 hrs	Antiproliferative activity against rat multidrug-resistant L12 cells after 48 hrs by XTT assay, IC50 = 0.05 μM.	17973361
L1210	Antiproliferative assay		48 hrs	Antiproliferative activity against mouse L1210 cells after 48 hrs by XTT assay, IC50 = 0.05 μM.	20537765
P388	Antiproliferative assay		48 hrs	Antiproliferative activity against ADR-resistant mouse P388 cells after 48 hrs by XTT assay, IC50 = 0.05 μM.	21705223
U2OS	Function assay		72 hrs	Induction of mitotic arrest in human U2OS cells assessed as mitotic index after 72 hrs by microscopic analysis, EC50 = 0.05 μM.	24900887
L1210	Antiproliferative assay		48 hrs	Antiproliferative activity against mouse L1210 cells after 48 hrs by XTT assay, IC50 = 0.06 μM.	17973361
L1210	Antiproliferative assay		48 hrs	Antiproliferative activity against mouse L1210 cells after 48 hrs by XTT assay, IC50 = 0.06 μM.	19220018
L1210	Antiproliferative assay		48 hrs	Antiproliferative activity against mouse L1210 cells after 48 hrs by XTT assay, IC50 = 0.06 μM.	21705223
HeLa	Anticancer assay		48 hrs	Anticancer activity against human HeLa cells after 48 hrs by SRB assay, GI50 = 0.063 μM.	27130357
MDA-MB-231	Cytotoxicity assay		48 hrs	Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 48 hrs by SRB assay, GI50 = 0.065 μM.	28117204
NCI-H460	Antiproliferative assay		48 hrs	Antiproliferative activity against human NCI-H460 cells after 48 hrs by alamar blue assay, IC50 = 0.068 μM.	21563750
BT549	Antiproliferative assay		48 hrs	Antiproliferative activity against human BT549 cells after 48 hrs by alamar blue assay, IC50 = 0.069 μM.	21563750
LT12 MDR	Antiproliferative assay		48 hrs	Antiproliferative activity against LT12 MDR cells by XTT assay after 48 hrs, IC50 = 0.07 μM.	17181164
L1210	Antiproliferative assay		48 hrs	Antiproliferative activity against mouse vincristine-resistant L1210 cells after 48 hrs by XTT assay, IC50 = 0.07 μM.	17973361
P388	Antiproliferative assay		48 hrs	Antiproliferative activity against mouse P388 cells after 48 hrs by XTT assay, IC50 = 0.07 μM.	17973361
LT12	Antiproliferative assay		48 hrs	Antiproliferative activity against multi drug-resistant rat LT12 cells after 48 hrs by XTT assay, IC50 = 0.07 μM.	20537765
P388	Antiproliferative assay		48 hrs	Antiproliferative activity against mouse P388 cells after 48 hrs by XTT proliferation assay, IC50 = 0.07 μM.	21705223
LT12	Antiproliferative assay		48 hrs	Antiproliferative activity against rat multiple drug-resistant LT12 cells after 48 hrs by XTT assay, IC50 = 0.07 μM.	21705223
L1210	Antiproliferative assay		48 hrs	Antiproliferative activity against mouse VCR-resistant L1210 cells after 48 hrs by XTT assay, IC50 = 0.07 μM.	21705223
451LU	Antiproliferative assay		48 hrs	Antiproliferative activity against human 451LU cells after 48 hrs by alamar blue assay, IC50 = 0.072 μM.	21563750
P388	Antiproliferative assay		48 hrs	Antiproliferative activity against P388 cells by XTT assay after 48 hrs, IC50 = 0.08 μM.	17181164
P388	Antiproliferative assay		48 hrs	Antiproliferative activity against mouse P388 cells after 48 hrs by XTT assay, IC50 = 0.08 μM.	20537765
SKOV3	Antiproliferative assay		48 hrs	Antiproliferative activity against human SKOV3 cells after 48 hrs by alamar blue assay, IC50 = 0.08 μM.	21563750
SGC7901	Growth inhibition assay		72 hrs	Growth inhibition of human SGC7901 cells after 72 hrs by MTT assay, IC50 = 0.08 μM.	25262051
A549	Anticancer assay		48 hrs	Anticancer activity against human A549 cells after 48 hrs by SRB assay, GI50 = 0.08 μM.	27130357
K562	Function assay			Effective concentration required to arrest propidium iodide stained K562 cells in G2/M phase, EC50 = 0.082 μM.	12852768
SKBR3	Growth inhibition assay		48 hrs	Growth inhibition of human SKBR3 cells after 48 hrs by MTT assay, IC50 = 0.084 μM.	22850214
HeLa	Cytotoxicity assay		48 hrs	Cytotoxicity against human HeLa cells assessed as growth inhibition after 48 hrs by SRB assay, GI50 = 0.086 μM.	28117204
A549	Cytotoxicity assay			Cytotoxicity against human A549 cells by MTT assay, IC50 = 0.087 μM.	21954851
COLO205	Antiproliferative assay		48 hrs	Antiproliferative activity against human COLO205 cells after 48 hrs by alamar blue assay, IC50 = 0.088 μM.	21563750
L1210 VCR	Antiproliferative assay		48 hrs	Antiproliferative activity against L1210 VCR cells by XTT assay after 48 hrs, IC50 = 0.09 μM.	17181164
L1210	Antiproliferative assay		48 hrs	Antiproliferative activity against vincristine-resistant mouse L1210 cells after 48 hrs by XTT assay, IC50 = 0.09 μM.	20537765
A549	Cytotoxicity assay		48 hrs	Cytotoxicity against human A549 cells assessed as growth inhibition after 48 hrs by SRB assay, GI50 = 0.09 μM.	28117204
KB/HeLa	Cell cycle assay			Cell cycle arrest in KB/HeLa cells by accumulation at G2/M phase, EC50 = 0.091 μM.	17181164
KB/HeLa	Cell cycle assay		24 hrs	Cell cycle arrest in KB/HeLa cells assessed as accumulation at G2/M phase after 24 hrs by flow cytometric analysis, EC50 = 0.091 μM.	17973361
KB/HeLa	Cell cycle assay		24 hrs	Cell cycle arrest in human KB/HeLa cells assessed as G2/M phase accumulation after 24 hrs by FACS analysis, EC50 = 0.091 μM.	19220018
KB/HeLa	Cell cycle assay		24 hrs	Cell cycle arrest in human KB/HeLa cells assessed as accumulation at G2/M phase after 24 hrs using propidium iodide staining by FACS analysis, EC50 = 0.091 μM.	20537765
KB/HeLa	Cell cycle assay		24 hrs	Cell cycle arrest in human KB/HeLa cells assessed as accumulation of cells at G2/M phase after 24 hrs by flow cytometry, EC50 = 0.091 μM.	21705223
MiaPaCa	Cytotoxicity assay		48 hrs	Cytotoxicity against human MiaPaCa cells assessed as growth inhibition after 48 hrs by SRB assay, GI50 = 0.091 μM.	28117204
MCF7	Growth inhibition assay			Growth inhibition of human MCF7 cells by Sulforhodamine B assay, GI50 = 0.1 μM.	21106458
MCF7	Growth inhibition assay			Growth inhibition of human MCF7 cells by Sulforhodamine B assay, LC50 = 0.1 μM.	21106458
A549	Growth inhibition assay			Growth inhibition of human A549 cells by Sulforhodamine B assay, GI50 = 0.1 μM.	21106458
A549	Growth inhibition assay			Growth inhibition of human A549 cells by Sulforhodamine B assay, LC50 = 0.1 μM.	21106458
A549	Cell cycle assay		24 hrs	Cell cycle arrest in human A549 cells assessed as accumulation at G2/M phase after 24 hrs using propidium iodide staining by flow cytometry, EC50 = 0.1065 μM.	20110137
RKO	Cytotoxicity assay			Cytotoxic activity against human colon adenocarcinoma RKO cells without ectopic inducible expression of cyclin-dependent kinase inhibitor p27kip1, IC50 = 0.11 μM.	12852768
RKO	Antiproliferative assay		48 hrs	Antiproliferative activity against RKO cells by XTT assay after 48 hrs, IC50 = 0.11 μM.	17181164
RKO	Cytotoxicity assay		48 hrs	Cytotoxicity against human RKO cells after 48 hrs by XTT assay, IC50 = 0.11 μM.	17973361
RKO	Antiproliferative assay			Antiproliferative activity against human RKO cells by XTT assay, IC50 = 0.11 μM.	19220018
RKO	Antiproliferative assay		48 hrs	Antiproliferative activity against human RKO cells after 48 hrs by XTT assay, IC50 = 0.11 μM.	20537765
RKOp27	Cytotoxicity assay		48 hrs	Cytotoxicity against non induced human RKOp27 cells after 48 hrs by XTT assay, IC50 = 0.11 μM.	21705223
SW480	Antiproliferative assay		48 hrs	Antiproliferative activity against human SW480 cells after 48 hrs by alamar blue assay, IC50 = 0.12 μM.	21563750
A549	Growth inhibition assay		72 hrs	Growth inhibition of human A549 cells after 72 hrs by MTT assay, IC50 = 0.12 μM.	25262051
KB/HeLa	Antiproliferative assay			Antiproliferative activity against human KB/HeLa cells by XTT assay, IC50 = 0.14 μM.	19220018
KB/HeLa	Antiproliferative assay		48 hrs	Antiproliferative activity against KB/HeLa cells by XTT assay after 48 hrs, IC50 = 0.14 μM.	17181164
KB/HeLa	Cytotoxicity assay		48 hrs	Cytotoxicity against human KB/HeLa cells after 48 hrs by XTT assay, IC50 = 0.14 μM.	17973361
KB/HeLa	Antiproliferative assay		48 hrs	Antiproliferative activity against human KB/HeLa cells after 48 hrs by XTT assay, IC50 = 0.14 μM.	20537765
KB/HeLa	Cytotoxicity assay		48 hrs	Cytotoxicity against human KB/HeLa cells after 48 hrs by XTT assay, IC50 = 0.14 μM.	21705223
HT1080	Growth inhibition assay		72 hrs	Growth inhibition of human HT1080 cells after 72 hrs by MTT assay, IC50 = 0.14 μM.	25262051
NCI-H460	Antiproliferative assay		48 hrs	Antiproliferative activity against NCI-H460 cells by XTT assay after 48 hrs, IC50 = 0.15 μM.	17181164
NCI-H460	Cytotoxicity assay		48 hrs	Cytotoxicity against human NCI-H460 cells after 48 hrs by XTT assay, IC50 = 0.15 μM.	17973361
NCI-H460	Antiproliferative assay			Antiproliferative activity against human NCI-H460 cells by XTT assay, IC50 = 0.15 μM.	19220018
NCI-H460	Antiproliferative assay		48 hrs	Antiproliferative activity against human NCI-H460 cells after 48 hrs by XTT assay, IC50 = 0.15 μM.	20537765
NCI-H460	Cytotoxicity assay		48 hrs	Cytotoxicity against human NCI-H460 cells after 48 hrs by XTT assay, IC50 = 0.15 μM.	21705223
SKOV3	Antiproliferative assay		48 hrs	Antiproliferative activity against SKOV3 cells by XTT assay after 48 hrs, IC50 = 0.17 μM.	17181164
P388 ADR	Antiproliferative assay		48 hrs	Antiproliferative activity against P388 ADR cells by XTT assay after 48 hrs, IC50 = 0.17 μM.	17181164
SKOV3	Cytotoxicity assay		48 hrs	Cytotoxicity against human SKOV3 cells after 48 hrs by XTT assay, IC50 = 0.17 μM.	17973361
SKOV3	Antiproliferative assay			Antiproliferative activity against human SKOV3 cells by XTT assay, IC50 = 0.17 μM.	19220018
SKOV3	Antiproliferative assay		48 hrs	Antiproliferative activity against human SKOV3 cells after 48 hrs by XTT assay, IC50 = 0.17 μM.	20537765
P388	Antiproliferative assay		48 hrs	Antiproliferative activity against adriamycin-resistant mouse P388 cells after 48 hrs by XTT assay, IC50 = 0.17 μM.	20537765
SKOV3	Cytotoxicity assay		48 hrs	Cytotoxicity against human SKOV3 cells after 48 hrs by XTT assay, IC50 = 0.17 μM.	21705223
HCT116	Cytotoxicity assay			Cytotoxicity against human HCT116 cells by SRB assay, IC50 = 0.173 μM.	21954851
HeLa	Cytotoxicity assay		24 to 48 hrs	Cytotoxicity against human HeLa cells after 24 to 48 hrs by trypan blue assay, IC50 = 0.178 μM.	23445405
L1210	Function assay	0.3 uM	24 hrs	Fraction of cell population of cultured lymphoid leukemia L1210 cells in mitosis at a dose of 0.3 uM after 24 hr, Mitotic index = 0.19 μM.	7131483
DLD1	Antiproliferative assay		48 hrs	Antiproliferative activity against human DLD1 cells after 48 hrs by alamar blue assay, IC50 = 0.19 μM.	21563750
SF268	Antiproliferative assay		48 hrs	Antiproliferative activity against SF268 cells by XTT assay after 48 hrs, IC50 = 0.3 μM.	17181164
SF268	Cytotoxicity assay		48 hrs	Cytotoxicity against human SF268 cells after 48 hrs by XTT assay, IC50 = 0.3 μM.	17973361
SF268	Antiproliferative assay			Antiproliferative activity against human SF268 cells by XTT assay, IC50 = 0.3 μM.	19220018
L12	Antiproliferative assay		48 hrs	Antiproliferative activity against rat L12 cells after 48 hrs by XTT assay, IC50 = 0.3 μM.	17973361
SF268	Antiproliferative assay		48 hrs	Antiproliferative activity against human SF268 cells after 48 hrs by XTT assay, IC50 = 0.3 μM.	20537765
SF268	Cytotoxicity assay		48 hrs	Cytotoxicity against human SF268 cells after 48 hrs by XTT assay, IC50 = 0.3 μM.	21705223
LT12	Antiproliferative assay		48 hrs	Antiproliferative activity against rat LT12 cells ectopic expression of human MDR1 after 48 hrs by XTT assay, IC50 = 0.4 μM.	19220018
A549	Cytotoxicity assay		48 hrs	Cytotoxicity against human A549 cells after 48 hrs by SRB assay, GI50 = 0.5 μM.	20529689
SK-N-SH	Cytotoxicity assay		48 hrs	Cytotoxicity against human SK-N-SH cells after 48 hrs by SRB assay, GI50 = 0.65 μM.	20529689
SK-N-SH	Growth inhibition assay			Growth inhibition of human SK-N-SH cells by Sulforhodamine B assay, GI50 = 0.66 μM.	21106458
HeLa	Cytotoxicity assay		48 hrs	Cytotoxicity against human HeLa cells after 48 hrs by MTT assay, IC50 = 0.71 μM.	23748152
HeLa	Growth inhibition assay			Growth inhibition of human HeLa cells by Sulforhodamine B assay, GI50 = 0.75 μM.	21106458
SK-N-SH	Growth inhibition assay			Growth inhibition of human SK-N-SH cells by Sulforhodamine B assay, LC50 = 0.75 μM.	21106458
K562	Function assay			Inhibition of tubulin polymerization in human K562 cells, IC50 = 0.76 μM.	20546980
HeLa	Antiproliferative assay		48 hrs	Antiproliferative activity against human HeLa cells assessed as growth inhibition after 48 hrs by SRB assay, GI50 = 0.81 μM.	25131956
HeLa	Antiproliferative assay		48 hrs	Antiproliferative activity against human HeLa cells after 48 hrs by SRB assay, GI50 = 0.81 μM.	27344493
A549	Cytotoxicity assay		48 hrs	Cytotoxicity against human A549 cells assessed as cell viability after 48 hrs by MTT assay, IC50 = 0.89 μM.	25599948
HeLa	Growth inhibition assay			Growth inhibition of human HeLa cells by Sulforhodamine B assay, LC50 = 0.9 μM.	21106458
A549	Antiproliferative assay		48 hrs	Antiproliferative activity against human A549 cells after 48 hrs by SRB assay, IC50 = 0.9 μM.	28988624
MDA-MB-453	Cytotoxicity assay		48 hrs	Cytotoxicity in human MDA-MB-453 cells incubated for 48 hrs by MTT assay, IC50 = 0.91 μM.	28923381
MCF7	Antiproliferative assay		48 hrs	Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 48 hrs by SRB assay, GI50 = 0.94 μM.	25131956
MCF7	Antiproliferative assay		48 hrs	Antiproliferative activity against human MCF7 cells after 48 hrs by SRB assay, GI50 = 0.94 μM.	27344493
MIAPaCa2	Antiproliferative assay		48 hrs	Antiproliferative activity against human MIAPaCa2 cells assessed as growth inhibition after 48 hrs by SRB assay, GI50 = 0.95 μM.	25131956
MIAPaCa2	Antiproliferative assay		48 hrs	Antiproliferative activity against human MIAPaCa2 cells after 48 hrs by SRB assay, GI50 = 0.95 μM.	27344493
A549	Cytotoxicity assay		48 hrs	Cytotoxicity against human A549 cells after 48 hrs by SRB assay, LC50 = 1 μM.	20529689
HCT116	Cytotoxicity assay		48 hrs	Cytotoxicity in human HCT116 cells incubated for 48 hrs by MTT assay, IC50 = 1.06 μM.	28923381
HeLa	Cytotoxicity assay		48 hrs	Cytotoxicity against human HeLa cells assessed as cell viability after 48 hrs by MTT assay, IC50 = 1.1 μM.	25599948
DU145	Cytotoxicity assay		48 hrs	Cytotoxicity in human DU145 cells incubated for 48 hrs by MTT assay, IC50 = 1.14 μM.	28923381
HeLa	Antiproliferative assay		48 hrs	Antiproliferative activity against human HeLa cells after 48 hrs by SRB assay, IC50 = 1.2 μM.	28988624
MCF7	Antiproliferative assay		48 hrs	Antiproliferative activity against human MCF7 cells after 48 hrs by SRB assay, IC50 = 1.25 μM.	28988624
HCT116	Anticancer assay		48 hrs	Anticancer activity against human HCT116 cells after 48 hrs by MTT assay, IC50 = 1.262 μM.	28789894
IMR32	Antiproliferative assay		48 hrs	Antiproliferative activity against human IMR32 cells after 48 hrs by SRB assay, IC50 = 1.3 μM.	28988624
A549	Anticancer assay		48 hrs	Anticancer activity against human A549 cells after 48 hrs by MTT assay, IC50 = 1.513 μM.	28789894
MCF7	Anticancer assay		48 hrs	Anticancer activity against human MCF7 cells assessed as reduction in cell growth incubated for 48 hrs by MTT assay, IC50 = 1.6 μM.	26231080
DU145	Anticancer assay		48 hrs	Anticancer activity against human DU145 cells after 48 hrs by MTT assay, IC50 = 1.698 μM.	28789894
MCF7	Cytotoxicity assay		48 hrs	Cytotoxicity against human MCF7 cells assessed as cell viability after 48 hrs by MTT assay, IC50 = 1.7 μM.	25599948
PC3	Cytotoxicity assay		48 hrs	Cytotoxicity in human PC3 cells incubated for 48 hrs by MTT assay, IC50 = 1.84 μM.	28923381
MDA-MB-231	Anticancer assay		48 hrs	Anticancer activity against human MDA-MB-231 cells after 48 hrs by MTT assay, IC50 = 1.862 μM.	28789894
A549	Anticancer assay		48 hrs	Anticancer activity against human A549 cells assessed as reduction in cell growth incubated for 48 hrs by MTT assay, IC50 = 1.87 μM.	26231080
A549	Cytotoxicity assay		48 hrs	Cytotoxicity against human A549 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50 = 1.87 μM.	28668476
A549	Cytotoxicity assay		48 hrs	Cytotoxicity against human A549 cells after 48 hrs by MTT assay, IC50 = 2.31 μM.	23748152
SK-N-SH	Cytotoxicity assay		48 hrs	Cytotoxicity against human SK-N-SH cells after 48 hrs by SRB assay, LC50 = 2.8 μM.	20529689
DU145	Cytotoxicity assay		48 hrs	Cytotoxicity against human DU145 cells after 48 hrs by MTT assay, IC50 = 2.8 μM.	23748152
HeLa	Anticancer assay		48 hrs	Anticancer activity against human HeLa cells assessed as reduction in cell growth incubated for 48 hrs by MTT assay, IC50 = 2.83 μM.	26231080
HeLa	Cytotoxicity assay		48 hrs	Cytotoxicity against human HeLa cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50 = 2.83 μM.	28668476
DU145	Cytotoxicity assay		48 hrs	Cytotoxicity against human DU145 cells assessed as cell viability after 48 hrs by MTT assay, IC50 = 3.2 μM.	25599948
HaCaT	Cytotoxicity assay		48 hrs	Cytotoxic activity against human HaCaT cells assessed as reduction in cell growth incubated for 48 hrs by MTT assay, IC50 = 8.9 μM.	26231080
NIH3T3	Apoptosis assay	0.5 ug/ml	24 hrs	Induction of apoptosis in mouse NIH3T3 cells assessed as accumulation at subG1 phase at 0.5 ug/ml after 24 hrs by flow cytometry	18247573
PC3M	Apoptosis assay	0.5 ug/ml	24 hrs	Induction of apoptosis in human PC3M cells assessed as accumulation at subG1 phase at 0.5 ug/ml after 24 hrs by flow cytometry	18247573
NRK	Function assay	30 uM	60 mins	Golgi-disturbing activity in golgi apparatus of rat NRK cells assessed as microtubule depolymerization-associated golgi fragmentation at 30 uM after 60 mins by Hoechst 3342 staining-based immunofluorescence microscopy	20189813
Vero	Function assay	5 ug/ml	30 mins	Effect on disruption of microtubules in african green monkey Vero cells at 5 ug/ml after 30 mins by immunofluorescence method	19182783
MCF7	Apoptosis assay	2.5 uM	48 hrs	Induction of apoptosis in human MCF7 cells assessed as nuclear fragmentation at 2.5 uM after 48 hrs by DAPI staining	21194809
MCF7	Function assay	2.5 uM	48 hrs	Inhibition of tubulin polymerization in human MCF7 cells assessed as disrupted microtubule organization at 2.5 uM after 48 hrs by microscopic analysis	21194809
A549	Cell cycle assay		24 hrs	Cell cycle arrest in human A549 cells assessed as accumulation of cells in G2 phase after 24 hrs measured using propidium iodide staining by FACS analysis	21863853
A549	Apoptosis assay	10 to 100 nM	48 hrs	Induction of apoptosis in human A549 cells assessed as early apoptotic cells at 10 to 100 nM after 48 hrs by annexin-V FITC/7-ADD staining-based flow cytometric analysis	21916509
A549	Apoptosis assay	10 to 100 nM	48 hrs	Induction of apoptosis in human A549 cells assessed as necrotic cells at 10 to 100 nM after 48 hrs by annexin-V FITC/7-ADD staining-based flow cytometric analysis	21916509
A549	Cell cycle assay	1 uM	48 hrs	Cell cycle arrest in human A549 cells assessed as accumulation at G2/M phase at 1 uM after 48 hrs by propidium iodide staining-based flow cytometric analysis relative to control	22361684
SKBR3	Function assay	50 to 100 nM	24 hrs	Induction of Hsp27 phosphorylation in human SKBR3 cells at 50 to 100 nM after 24 hrs by SDS-PAGE analysis	22435708
SKBR3	Function assay	0.2 to 1 uM	24 hrs	Induction of Hsp27 phosphorylation in human SKBR3 cells at 0.2 to 1 uM after 24 hrs by SDS-PAGE analysis	22435708
MCF7	Function assay	4 uM	24 hrs	Inhibition of microtubule organization in human MCF7 cells at 4 uM after 24 hrs by immunofluorescence analysis	22982122
Jurkat T	Function assay		36 hrs	Induction of microtubule damage in human Jurkat T cells overexpressing Bcl2 after 36 hrs by immunostaining method	22197393
Jurkat T	Function assay		36 hrs	Induction of microtubule damage in human Jurkat T cells overexpressing Neo after 36 hrs by immunostaining method	22197393
Jurkat T	Apoptosis assay		36 hrs	Induction of apoptosis in human Jurkat T cells overexpressing Bcl2 assessed as cellular protrusions after 36 hrs by light microscopy	22197393
Jurkat T	Apoptosis assay		36 hrs	Induction of apoptosis in human Jurkat T cells overexpressing Neo after 36 hrs by flow cytometry	22197393
Jurkat T	Apoptosis assay		36 hrs	Induction of apoptosis in human Jurkat T cells overexpressing Neo assessed as cellular protrusions after 36 hrs by light microscopy	22197393
HeLa	Function assay	1 uM	24 hrs	Inhibition of tubulin polymerization in human HeLa cells assessed as tubulin soluble fraction at 1 uM after 24 hrs by immunohistochemistry analysis	23313639
HeLa	Function assay	1 uM	24 hrs	Mitotic arrest in human HeLa cells assessed as increase in accumulation at G2/M phase at 1 uM for 24 hrs by PI staining/FACS analysis	24530033
HeLa	Cell cycle assay	2 uM	24 hrs	Cell cycle arrest at G2/M phase in human HeLa cells assessed as increase in cyclin B1 expression at 2 uM after 24 hrs by immunoblot analysis relative to control	25499929
HeLa	Cell cycle assay	2 uM	24 hrs	Cell cycle arrest at G2/M phase in human HeLa cells assessed as soluble form of tubulin at 2 uM after 24 hrs by immunoblot analysis relative to control	25499929
DU145	Function assay	50 uM	48 hrs	Disruption of microtubule network in human DU145 cells at 50 uM after 48 hrs by immunohistochemistry analysis	25615796
HeLa	Function assay	25 uM	24 hrs	Effect on PCM1 protein in human HeLa cells assessed as accumulation of pericentriolar material at 25 uM after 24 hrs by immunofluorescence microscopy	25050880
SGC7901	Function assay		48 hrs	Induction of distortions in tubulin assembly in human SGC7901 cells assessed as abnormal mitotic spindle formation at 2 fold IC50 level incubated for 48 hrs by immunofluorescence staining based fluorescence microscopy	25262051
HT1080	Function assay		48 hrs	Induction of distortions in tubulin assembly in human HT1080 cells assessed as abnormal mitotic spindle formation at 2 fold IC50 level incubated for 48 hrs by immunofluorescence staining based fluorescence microscopy	25262051
MCF7	Function assay	1 uM	4 hrs	Induction of tubulin depolymerization in human MCF7 cells at 1 uM after 4 hrs by sedimentation assay and Western blotting method	25369367
DU145	Function assay	1.5 uM	48 hrs	Reduction in mitochondrial membrane potential in human DU145 cells at 1.5 uM incubated for 48 hrs by JC1 dye staining based flow cytometry	26330077
SKBR3	Function assay	2.5 uM	24 hrs	Induction of microtubule destabilization in human SKBR3 cells assessed as soluble fraction of protein at 2.5 uM after 24 hrs by Western blot analysis	26599530
HeLa	Function assay	100 nM	4 hrs	Inhibition of tubulin polymerization in human HeLa cells assessed as microtubule disruption in mitotic phase at 100 nM after 4 hrs by indirect immunofluorescence analysis	26641132
HeLa	Function assay	100 nM	4 hrs	Inhibition of tubulin polymerization in human HeLa cells assessed as microtubule disruption in interphase at 100 nM after 4 hrs by indirect immunofluorescence analysis	26641132
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	29435139
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells	29435139
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells	29435139
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells	29435139
U-2 OS	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells	29435139
HeLa	Function assay		24 hrs	Inhibition of tubulin polymerization in human HeLa cells assessed as increase in soluble tubulin fraction after 24 hrs by Western blot analysis	28818768
HeLa	Function assay	0.1 uM	24 hrs	Inhibition of tubulin polymerization in human HeLa cells assessed as shift of tubulin protein to soluble fraction at 0.1 uM after 24 hrs by Western blot analysis	29501940
PC3MLN4	Function assay	1 uM	24 hrs	Upregulation of Cyclin-B1 protein expression in human PC3MLN4 cells at 1 uM after 24 hrs by Western blot method	29288939
PC3MLN4	Function assay	1 uM	48 hrs	Disruption of microtubule dynamics in human PC3MLN4 cells at 1 uM after 48 hrs by immunofluorescence microscopic method	29288939
MCF7	Function assay	1 uM	4 hrs	Induction of tubulin depolymerization in human MCF7 cells at 1 uM after 4 hrs by Western blot method	27689728
Jurkat	Function assay	1 uM	4 hrs	Induction of tubulin depolymerization in human Jurkat cells at 1 uM after 4 hrs by Western blot method	27689728
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Informazioni chimiche, conservazione e stabilità

Peso molecolare	301.32	Formula	C₁₄H₁₁N₃O₃S	Conservazione (Dalla data di ricezione)	3 anni-20°Cpolvere
N. CAS	31430-18-9	Scarica SDF		Conservazione delle soluzioni stock	1 anno-80°Cin solvente 1 mese-20°Cin solvente
Sinonimi	R17934, Oncodazole, NSC238159			Smiles	COC(=O)NC1=NC2=C(N1)C=C(C=C2)C(=O)C3=CC=CS3

Solubilità

In vitro
Lotto:

DMSO : 7.5 mg/mL (24.89 mM)
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

Water : Insoluble

Ethanol : 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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	0.380mg/ml (1.26mM)	Taking the 1 mL working solution as an example, add 50 μL 7.5 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to make it clear. Volume up to 1 mL. The mixed solution should be used immediately for optimal results.
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.
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	Microtubules (Cell-free assay) Abl (Cell-free assay) 0.21 μM Abl (E255K) (Cell-free assay) 0.53 μM Abl (T315I) (Cell-free assay) 0.64 μM
In vitro	Nocodazole è un ligando ad alta affinità per le chinasi correlate al cancro, tra cui Abl fosforilata, c-Kit, BRAF e MEK con K_d di 0,091 μM, 1,6 μM, 1,8 μM e 1,6 μM, rispettivamente. Inoltre, il K_d di questo composto per Abl(E255K) fosforilata, Abl(T315I) fosforilata, BRAF(V600E) e PI3Kγ è di 0,12 μM, 0,17 μM, 1,1 μM e 1,5 μM, rispettivamente. Induce apoptosi nelle cellule di leucemia linfatica cronica. Questa sostanza chimica inibisce il trasporto di glucosio stimolato dall'insulina. Diminuisce l'apoptosi in alcune cellule di carcinoma del colon umano. Compromette la morfologia e la direzionalità delle cellule migranti dell'eminenza gangliare mediale. A concentrazioni elevate, questo composto depolimerizza rapidamente i microtubuli nelle cellule, mentre a basse concentrazioni inibisce l'instabilità dinamica dei microtubuli. Le cellule mitotiche incubate con diverse concentrazioni sono inibite dal progredire alla fase G₁ 6 ore dopo il rilascio dal blocco di Nocodazole, con una concentrazione inibitoria mediana di 4 nM. Le cellule pretrattate con Nocodazole esposte in assenza di questa sostanza chimica formano solo microtubuli liberi, mentre le cellule pretrattate esposte in sua presenza assemblano microtubuli organizzati dal centrosoma. Interrompe i microtubuli legandosi alla β-tubulina. Questo composto previene la formazione di uno dei due legami disolfuro intercatena. Compromette il trasporto di vescicole. Sopprime la morte cellulare e la disfunzione lisosomiale indotte da METH. La morte cellulare indotta da METH è significativamente ridotta dal pretrattamento con questo composto rispetto al solo METH. Raddoppia l'efficienza di HDR fino al 30% nelle iPSC. Migliora l'efficienza di HDR mediata da CRISPR e ha un effetto additivo sul miglioramento dell'editing genomico preciso.
In vivo	Il volume e il peso del tumore dei topi trattati con Nocodazole sono significativamente ridotti rispetto a quelli trattati solo con questo composto. Il trattamento combinato con questa sostanza chimica aumenta fortemente l'apoptosi degli xenotrapianti tumorali COLO 205 trattati solo con essa.
Riferimenti	[1] https://pubmed.ncbi.nlm.nih.gov/22002881/ [2] http://onlinelibrary.wiley.com/doi/10.1002/ddr.10023/abstract [3] https://pubmed.ncbi.nlm.nih.gov/7913875/ [4] https://pubmed.ncbi.nlm.nih.gov/22613348/ [5] https://pubmed.ncbi.nlm.nih.gov/12203371/ [6] https://pubmed.ncbi.nlm.nih.gov/28219395/ [7] https://pubmed.ncbi.nlm.nih.gov/34388376/

Applicazioni

Metodi	Biomarcatori	PMID
Western blot	Cdc2 / cyclin B1 / MAD2 / Cdc20	21918689
Immunofluorescence	Tubulin / LC8 Brd4 / α-tubulin	23038268
Growth inhibition assay	Cell viability	21918689

Supporto tecnico

Istruzioni per la manipolazione

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

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