|(6-(噻吩-2-羰基)-1H-苯并[d]咪唑-2-基)氨基甲酸甲酯|CsnPharm

CAS No.: 31430-18-9

Nocodazole/诺考达唑 Catalog No. CSN11569

Synonyms: Oncodazole;R17934;NSC-238159

Nocodazole is a rapidly-reversible inhibitor of microtubule polymerization, also inhibits Abl, Abl (E255K) and Abl (T315I) with IC50 of 0.21 μM, 0.53 μM and 0.64 μM, respectively.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Abl

IC50:0.21μM Abl (E255K)

IC50:0.53μM Abl (T315I)

IC50:0.64μM
描述Microtubules, part of the cytoskeleton that provides structure and shape to the cytoplasm of cells, are tubular polymers of tubulin formed by polymerization. Nocodazole is a standard anti-microtubule agent that interferes with the polymerization and now be mostly used as depolymerizing drug in basic cell biology research^[8]. Nocodazole can be used as a high-affinity ligand for the cancer-related kinases including Abl phosphorylated, c-Kit, BRAF, and MEK. Furthermore, Nocodazole induces apoptosis in chronic lymphocytic leukemia cells, inhibits insulin-stimulated glucose transport and decreases apoptosis in some human colon carcinoma cells^[9]. In vitro Tubulin Polymerization Assays, Nocodazole inhibited tumor cell lines including NCIH460, SKOV3, BT549,451LU, COLO-205 at 48h with IC50 values 68nM, 80nM, 69nM, 72nM, 88nM respectively, which was reflected by a decreased level of steady state turbidity in a dose-dependent manner^[5]. To learn how the spindle assembly checkpoint (SAC) inhibitory is extinguished, 9A-Hec1-expressing cells exhibited a robust mitotic arrest after incubation in 5 mM nocodazole for 5 h. As comparison, WT-Hec1 was treated with a moderately low dose (300 nM) of nocodazole, which resulted in the loss of all non-kinetochore spindle microtubules but retention of kinetochore–microtubule^[6]. In addition, nocodazole can also improve the CRISPR-mediated HDR efficiency, a 600-bp homology in both arms leads to high-level genome knock in, with 97–100% of the donor insertion events being mediated by HDR. The combined use of CCND1, a cyclin that functions in G1/S transition, and nocodazole, a G2/M phase synchronizer, doubles HDR efficiency to up to 30% in iPSCs, the results showed an additive effect on enhancing precise genome editing^[7].
作用机制Nocodazole will bind to β-Tb and block polymerization, arrest mammalian cells in mitosis and release them into cytokinesis and G1 as well as mis-regulate mitotic kinases^[8].
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
human 451LU cells	-	Proliferation assay	48 h	Antiproliferative activity against human 451LU cells after 48 hrs by alamar blue assay, IC50=72 nM	21563750
human A549 cells	-	Proliferation assay	48 h	Antiproliferative activity against human A549 cells after 48 hrs by SRB assay, GI50=20 nM	25827522
human A549 cells	-	Cytotoxic assay	24 h	Cytotoxicity against human A549 cells after 24 hrs by MTT assay, IC50=36.6 nM	20110137

更多
动物研究
剂量
Mice: 15 mg/kg - 60 mg/kg^[3] (i.p.), 5 mg/kg^[4] (i.p.)

给药途径
i.p.

动物研究
剂量	Mice: 15 mg/kg - 60 mg/kg^[3] (i.p.), 5 mg/kg^[4] (i.p.)
给药途径	i.p.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.3187 mL
- 16.5937 mL
- 33.1873 mL
- 5 mM
- 0.6637 mL
- 3.3187 mL
- 6.6375 mL
- 10 mM
- 0.3319 mL
- 1.6594 mL
- 3.3187 mL

技术信息

CAS号

31430-18-9

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C14H11N3O3S

运输

蓝冰

分子量

301.32

别名

Oncodazole;R17934;NSC-238159;R 17,934;诺考达唑

溶解度

DMSO	20.0 mg/mL (66.4 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+30% PEG300+water	0.4 mg/mL	clear
PO	0.5% CMC-Na	65 mg/mL	suspension

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Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources

human 451LU cells	-	Proliferation assay	48 h	Antiproliferative activity against human 451LU cells after 48 hrs by alamar blue assay, IC50=72 nM	21563750
human A549 cells	-	Proliferation assay	48 h	Antiproliferative activity against human A549 cells after 48 hrs by SRB assay, GI50=20 nM	25827522
human A549 cells	-	Cytotoxic assay	24 h	Cytotoxicity against human A549 cells after 24 hrs by MTT assay, IC50=36.6 nM	20110137
human A549 cells	-	Growth inhibition assay	-	Growth inhibition of human A549 cells by Sulforhodamine B assay, GI50=0.1 μM	21106458
human BT549 cells	-	Proliferation assay	48 h	Antiproliferative activity against human BT549 cells after 48 hrs by alamar blue assay, IC50=69 nM	21563750
human COLO205 cells	-	Proliferation assay	48 h	Antiproliferative activity against human COLO205 cells after 48 hrs by alamar blue assay , IC50=88 nM	21563750
human HaCaT cells	-	Cytotoxic assay	48 h	Cytotoxic activity against human HaCaT cells assessed as reduction in cell growth incubated for 48 hrs by MTT assay, IC50=8.9 μM	26231080
human HeLa cells	-	Proliferation assay	48 h	Antiproliferative activity against human HeLa cells after 48 hrs by SRB assay, GI50=15 nM	25827522
human Jurkat T cells	-	Function assay	36 h	Induction of microtubule damage in human Jurkat T cells overexpressing Bcl2 after 36 hrs by immunostaining method	22197393
human KB/HeLa cells	-	Function assay	24 h	Cell cycle arrest in human KB/HeLa cells assessed as G2/M phase accumulation after 24 hrs by FACS analysis, EC50=91 nM	19220018
human MCF7 cells	-	Growth inhibition assay	-	Growth inhibition of human MCF7 cells by Sulforhodamine B assay, GI50=0.1 μM	21106458
human MDA-MB-231 cells	-	Proliferation assay	48 h	Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by SRB assay, GI50=17 nM	25827522
human MIAPaCa2 cells	-	Proliferation assay	48 h	Antiproliferative activity against human MIAPaCa2 cells assessed as growth inhibition after 48 hrs by SRB assay, GI50=0.95 μM	25131956
human NCI-H460 cells	-	Proliferation assay	48 h	Antiproliferative activity against human NCI-H460 cells after 48 hrs by alamar blue assay, IC50=68 nM	21563750
human NCI-H460 cells	-	Proliferation assay	48 h	Antiproliferative activity against human NCI-H460 cells after 48 hrs by XTT assay, IC50=0.15 μM	20537765
human PANC1 cells	-	Proliferation assay	48 h	Antiproliferative activity against human PANC1 cells after 48 hrs by SRB assay, GI50=10 nM	25827522
human PC3M cells	0.5 ug/ml	Function assay	24 h	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
human RKO cells	-	Proliferation assay	-	Antiproliferative activity against human RKO cells by XTT assay, IC50=0.11 μM	19220018
human SF268 cells	-	Cytotoxic assay	48 h	Cytotoxicity against human SF268 cells after 48 hrs by XTT assay, IC50=0.3 μM	21705223
human SGC7901 cells	-	Function assay	48 h	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
human SKBR3 cells	-	Growth inhibition assay	48 h	Growth inhibition of human SKBR3 cells after 48 hrs by MTT assay	22850214
human SK-N-SH cells	-	Growth inhibition assay	-	Growth inhibition of human SK-N-SH cells by Sulforhodamine B assay, GI50=0.66 μM	21106458
human SKOV3 cells	-	Proliferation assay	48 h	Antiproliferative activity against human SKOV3 cells after 48 hrs by alamar blue assay, IC50=80 nM	21563750
human SW480 cells	-	Proliferation assay	48 h	Antiproliferative activity against human SW480 cells after 48 hrs by alamar blue assay, IC50=0.12 μM	21563750
human U2OS cells	-	Function assay	72 h	Induction of mitotic arrest in human U2OS cells assessed as mitotic index after 72 hrs by microscopic analysis, EC50=50 nM	24900887
K562 cells	-	Function assay	-	Effective concentration required to arrest propidium iodide stained K562 cells in G2/M phase, EC50=82 nM	12852768
L1210 murine leukemia cell	-	Growth inhibition assay	-	In vitro for its inhibitory activity against L1210 murine leukemia cell growth, IC50=38 nM	1738146
LT12 cells	-	Proliferation assay	48 h	Antiproliferative activity against LT12 cells by XTT assay after 48 hrs, IC50=40 nM	17181164
lymphoid leukemia L1210 cells	-	Proliferation assay	48 h	Inhibitory concentration against proliferation of cultured lymphoid leukemia L1210 cells during 48 hrs, ID50=27 nM	7131483
mouse NIH3T3 cells	0.5 ug/ml	Function assay	24 h	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
mouse P388 cells	-	Proliferation assay	48 h	Antiproliferative activity against mouse P388 cells after 48 hrs by XTT assay, IC50=40 nM	19220018
rat LT12 cells	-	Proliferation assay	48 h	Antiproliferative activity against rat LT12 cells after 48 hrs by XTT assay, IC50=6 nM	19220018

靶点	Description	IC50
Abl		IC50:0.21μM
Abl (E255K)		IC50:0.53μM
Abl (T315I)		IC50:0.64μM

Nocodazole/诺考达唑 Catalog No. CSN11569

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