Monastrol

別名: (±)-Monastrol

此產(chǎn)品請避光密封保存。

目錄號：S8439 Purity: 99.86%

Monastrol ((±)-Monastrol)是一種具有細胞透性的kinesin-5(KIF11)小分子抑制劑，IC50為14μM，kinesin-5(KIF11)可保持半紡錘體的分離狀態(tài)。

Monastrol Chemical Structure

CAS: 329689-23-8

規(guī)格	價格	庫存
10mg	1204.01	現(xiàn)貨
50mg	4070.85	現(xiàn)貨
200mg	12039.31	現(xiàn)貨
1g	32678.74	現(xiàn)貨
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產(chǎn)品質控

批次：純度： 99.86%

99.86

Monastrol相關產(chǎn)品

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細胞實驗數(shù)據(jù)示例

細胞系	實驗類型	給藥濃度	孵育時間	活性描述	文獻信息
C6	Antiproliferative assay	100 uM	24 hrs	Antiproliferative activity against rat C6 cells assessed as reduction in cell viability at 100 uM after 24 hrs by MTS assay relative to control	ChEMBL
C6	Cell cycle assay	100 uM	24 hrs	Cell cycle arrest in rat C6 cells assessed as accumulation at G2/M phase at 100 uM after 24 hrs by propidium iodide staining based flow cytometry	ChEMBL
U138MG	Apoptosis assay	200 uM	48 hrs	Induction of apoptosis in human U138MG cells at 200 uM after 48 hrs by Annexin V/propidium iodide staining based flow cytometry	ChEMBL
U138MG	Necrosis assay	200 uM	48 hrs	Induction of necrosis in human U138MG cells at 200 uM after 48 hrs by Annexin V/propidium iodide staining based flow cytometry	ChEMBL
C6	Apoptosis assay	100 uM	48 hrs	Induction of apoptosis in rat C6 cells at 100 uM after 48 hrs by Annexin V/propidium iodide staining based flow cytometry	ChEMBL
U138MG	Function assay	200 uM	24 hrs	Inhibition of EG5 in human U138MG cells assessed as monopolar spindle formation at 200 uM after 24 hrs by Hoechst staining based immunofluorescence microscopic method	ChEMBL
C6	Function assay	100 uM	24 hrs	Inhibition of EG5 in rat C6 cells assessed as monopolar spindle formation at 100 uM after 24 hrs by Hoechst staining based immunofluorescence microscopic method	ChEMBL
C6	Antiproliferative assay	5 to 50 uM	48 hrs	Antiproliferative activity against rat C6 cells at 5 to 50 uM after 48 hrs by Neubauer chamber method	ChEMBL
MCF7	Antiproliferative assay	25 uM	48 hrs	Antiproliferative activity against human MCF7 cells at 25 uM after 48 hrs by sulforhodamine B assay	ChEMBL
NCI/ADR-RES	Antiproliferative assay	25 uM	48 hrs	Antiproliferative activity against human NCI/ADR-RES cells at 25 uM after 48 hrs by sulforhodamine B assay	ChEMBL
786-0	Antiproliferative assay	25 uM	48 hrs	Antiproliferative activity against human 786-0 cells at 25 uM after 48 hrs by sulforhodamine B assay	ChEMBL
HT-29	Antiproliferative assay	25 uM	48 hrs	Antiproliferative activity against human HT-29 cells at 25 uM after 48 hrs by sulforhodamine B assay	ChEMBL
UACC62	Antiproliferative assay	25 uM	48 hrs	Antiproliferative activity against human UACC62 cells at 25 uM after 48 hrs by sulforhodamine B assay	ChEMBL
PC3	Antiproliferative assay	25 uM	48 hrs	Antiproliferative activity against human PC3 cells at 25 uM after 48 hrs by sulforhodamine B assay	ChEMBL
OVCAR3	Antiproliferative assay	25 uM	48 hrs	Antiproliferative activity against human OVCAR3 cells at 25 uM after 48 hrs by sulforhodamine B assay	ChEMBL
KBV1	Antiproliferative assay		72 hrs	Antiproliferative activity against human KBV1 cells overexpressing MDR1 after 72 hrs by Alamar blue assay in presence of zosuquidar, EC50=45.394μM	20597485
hTERT-HME1	Antiproliferative assay		72 hrs	Antiproliferative activity against human hTERT-HME1 cells after 72 hrs by Alamar blue assay, EC50=45.082μM	20597485
HCT116	Antiproliferative assay		72 hrs	Antiproliferative activity against human HCT116 cells after 72 hrs by Alamar blue assay, EC50=24.155μM	20597485
HeLa	Function assay		12 hrs	Inhibition of Eg5 ATPase activity expressed in HeLa cells after 12 hrs, IC50=6.1μM	17587586
HL-60(TB)	Growth inhibition assay		24 hrs	Growth inhibition of human HL-60(TB) cells incubated for 24 hrs by MTT assay, IC50=0.147μM	28667871
MOLT4	Growth inhibition assay		24 hrs	Growth inhibition of human MOLT4 cells incubated for 24 hrs by MTT assay, IC50=0.215μM	28667871
McCoy	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse McCoy cells assessed as decrease in cell viability after 72 hrs by MTT assay, IC50=26.8μM	29908443
MM1S	Antiproliferative assay		72 hrs	Antiproliferative activity against human MM1S cells incubated for 72 hrs by MTT assay, IC50=8.7μM	ChEMBL
HCT116	Antiproliferative assay		72 hrs	Antiproliferative activity against human HCT116 cells incubated for 72 hrs by MTT assay, IC50=9μM	ChEMBL
CCRF-CEM	Growth inhibition assay			Growth inhibition of human CCRF-CEM cells, GI50=31.6μM	21855351
M14	Growth inhibition assay			Growth inhibition of human M14 cells, GI50=25.1μM	21855351
HL-60(TB)	Growth inhibition assay			Growth inhibition of human HL-60(TB) cells, GI50=25.1μM	21855351
KBV1/KB3-1	Function assay			Drug resistant ratio of EC50 for human KBV1 cells overexpressing MDR1 to EC50 for KB3-1 cells, EC50=0.0012μM	20597485
HCT116	Cell cycle assay			Effect on cell cycle progression in human HCT116 cells assessed as increase in phospho-histone H3 by fluorescence microscopy, EC50=1.5μM	18793847
HCT116	Cell cycle assay			Effect on cell cycle progression in human HCT116 cells assessed as mitotic arrest measured by doubling DNA content by fluorescence microscopy, EC50=1.2μM	18793847
K562	Growth inhibition assay			Growth inhibition of human K562 cells, GI50=31.6μM	21855351
MOLT4	Growth inhibition assay			Growth inhibition of human MOLT4 cells, GI50=31.6μM	21855351
SR	Growth inhibition assay			Growth inhibition of human SR cells, GI50=31.6μM	21855351
NCI-H522	Growth inhibition assay			Growth inhibition of human NCI-H522 cells, GI50=31.6μM	21855351
COLO205	Growth inhibition assay			Growth inhibition of human COLO205 cells, GI50=31.6μM	21855351
HCT116	Growth inhibition assay			Growth inhibition of human HCT116 cells, GI50=31.6μM	21855351
KM12	Growth inhibition assay			Growth inhibition of human KM12 cells, GI50=31.6μM	21855351
SF295	Growth inhibition assay			Growth inhibition of human SF295 cells, GI50=31.6μM	21855351
U251	Growth inhibition assay			Growth inhibition of human U251 cells, GI50=31.6μM	21855351
SK-MEL-2	Growth inhibition assay			Growth inhibition of human SK-MEL-2 cells, GI50=31.6μM	21855351
RPMI8266	Growth inhibition assay			Growth inhibition of human RPMI8266 cells, GI50=31.6μM	21855351
NCI-H322M	Growth inhibition assay			Growth inhibition of human NCI-H322M cells, GI50=39.8μM	21855351
HCC2998	Growth inhibition assay			Growth inhibition of human HCC2998 cells, GI50=39.8μM	21855351
HCT15	Growth inhibition assay			Growth inhibition of human HCT15 cells, GI50=39.8μM	21855351
SW620	Growth inhibition assay			Growth inhibition of human SW620 cells, GI50=39.8μM	21855351
SNB75	Growth inhibition assay			Growth inhibition of human SNB75 cells, GI50=39.8μM	21855351
SK-MEL-5	Growth inhibition assay			Growth inhibition of human SK-MEL-5 cells, GI50=39.8μM	21855351
UACC62	Growth inhibition assay			Growth inhibition of human UACC62 cells, GI50=39.8μM	21855351
SN12C	Growth inhibition assay			Growth inhibition of human SN12C cells, GI50=39.8μM	21855351
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
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 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
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
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 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
點擊查看更多細胞系數(shù)據(jù)

生物活性

產(chǎn)品描述

Monastrol ((±)-Monastrol)是一種具有細胞透性的kinesin-5(KIF11)小分子抑制劑，IC50為14μM，kinesin-5(KIF11)可保持半紡錘體的分離狀態(tài)。

靶點

KIF11(Eg5) ^[4]
(Cell-based assay)

14 μM

體外研究(In Vitro)
體外研究活性	Monastrol并不是通過細胞周期的S期和G2期或中心體復制抑制細胞周期進程。monastrol的有絲分裂阻滯作用快速可逆。它還能在爪蟾卵提取物中抑制雙極紡錘體的形成。Monastrol將細胞阻滯在有絲分裂期，但在體外不影響處于有絲分裂間期細胞的微管或是微管聚合^[1]。將交感神經(jīng)元細胞暴露于monastrol幾小時，將會增加軸突數(shù)量及生長速率。但時間延長，軸突的總體長度則與對照組無異。感覺神經(jīng)元同樣也有這種軸突生長速率短期升高的效果，然而，進一步延長暴露時間將導致軸突變短，說明感覺神經(jīng)元細胞對藥物的毒性作用更為敏感。但是，細胞整體培養(yǎng)狀況比taxol處理組要更為強健，taxol是一種常用于治療癌癥的藥物^[2]。在HeLa細胞中，monastrol激活紡錘體檢驗點，導致有絲分裂受到阻滯，引起凋亡^[3]。
細胞實驗	細胞系	BS-C-1 (猴腎臟上皮)細胞
	濃度	100 μM
	孵育時間	4 h
	方法	在胸腺嘧啶脫氧核苷雙重阻滯實驗中，處于生長對數(shù)期的BS-C-1細胞在含2 mM胸苷的正常培養(yǎng)基中培養(yǎng)。然后將細胞置于含24 μM deoxycytidine的培養(yǎng)基中培養(yǎng)9小時。第二次阻滯時，將細胞至于要含2 mM 胸苷的無血清培養(yǎng)基中16小時。最后，將細胞重新置于含24 μM deoxycytidine的培養(yǎng)基中，加入100 μM monastrol或0.1% DMSO。為了檢測monastrol和nocodazole的作用是否具有可逆性。將BS-C-1鋪于蓋玻片上，用含2 μM nocodazole或是100 μM monastrol的正常生長培養(yǎng)基處理4小時，然后將細胞置于正常培養(yǎng)基。在不同的時間節(jié)點，將蓋玻片進行免疫熒光染色，對處于有絲分裂間期或有絲分裂期的細胞進行計數(shù)。
實驗圖片	檢測方法	檢測指標	實驗圖片	PMID
	Growth inhibition assay	Cell viability		26035434
	Western blot	Cyclin B / Survivin		26035434

參考文獻
[1] Kapoor TM, et al. J Cell Biol. 2000, 150(5):975-88. [2] Haque SA, et al. Cell Motil Cytoskeleton. 2004, 58(1):10-6. [3] Chin GM, et al. Mol Cancer Ther. 2006, 5(10):2580-91. [4] Mayer TU, et al. Science. 1999, 286(5441):971-4. + 展開

參考文獻

[1] Kapoor TM, et al. J Cell Biol. 2000, 150(5):975-88.
[2] Haque SA, et al. Cell Motil Cytoskeleton. 2004, 58(1):10-6.
[3] Chin GM, et al. Mol Cancer Ther. 2006, 5(10):2580-91.

[4] Mayer TU, et al. Science. 1999, 286(5441):971-4.

+ 展開

化學信息&溶解度

分子量	292.35	分子式	C₁₄H₁₆N₂O₃S
CAS號	329689-23-8	SDF	Download Monastrol SDF
Smiles	CCOC(=O)C1=C(NC(=S)NC1C2=CC(=CC=C2)O)C
儲存條件(自收到貨起)	3年 -20°C(避光) 粉狀	儲備液保存和期限建議分裝儲備液，避免反復凍融！	1年-80°C溶于溶劑
儲存條件(自收到貨起)	3年 -20°C(避光) 粉狀	儲備液保存和期限建議分裝儲備液，避免反復凍融！	1個月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 58 mg/mL ( (198.39 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Ethanol : 58 mg/mL (198.39 mM)

Water : Insoluble

DMSO : 69 mg/mL ( (236.01 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Ethanol : 15 mg/mL (51.3 mM)

Water : Insoluble

摩爾濃度計算器

體內溶解度
批次：

現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑

動物體內配方計算器

實驗計算

摩爾濃度計算器

質量	濃度	體積	分子量
=	×	×

稀釋計算器分子量計算器

動物體內配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

給藥劑量 mg/kg 動物平均體重 g 每只動物給藥體積 μL 動物數(shù)量只

第二步：請輸入動物體內配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計算結果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH₂O，混勻澄清。

體內配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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* 必填項

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):

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