Ispinesib (SB-715992)

別名: CK0238273 中文名稱：伊斯平斯

目錄號(hào)：S1452 Purity: 99.97%

Ispinesib (SB-715992, CK0238273)是一種有效的，特異性的，可逆kinesin spindle protein (KSP)抑制劑，無(wú)細(xì)胞試驗(yàn)中K_iapp為1.7 nM，對(duì)CENP-E， RabK6， MCAK， MKLP1，KHC和Kif1A沒有抑制作用。Ispinesib可誘導(dǎo)有絲分裂阻滯和細(xì)胞的凋亡。

Ispinesib (SB-715992) Chemical Structure

CAS: 336113-53-2

規(guī)格	價(jià)格	庫(kù)存
10mM (1mL in DMSO)	2170	現(xiàn)貨
1mg	794.43	現(xiàn)貨
10mg	2621.56	現(xiàn)貨
50mg	7941.69	現(xiàn)貨
200mg	20229.3	現(xiàn)貨
1g	54873	現(xiàn)貨
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產(chǎn)品質(zhì)控

批次：純度： 99.97%

99.97

Ispinesib (SB-715992)相關(guān)產(chǎn)品

相關(guān)靶點(diǎn)	Kinesin-12	點(diǎn)擊展開
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相關(guān)化合物庫(kù)	激酶抑制劑庫(kù) 血管生成相關(guān)化合物庫(kù) TGF-beta/Smad信號(hào)通路庫(kù) 細(xì)胞骨架信號(hào)通路化合物庫(kù) 抗心血管疾病化合物庫(kù)	點(diǎn)擊展開

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系	實(shí)驗(yàn)類型	給藥濃度	孵育時(shí)間	活性描述	文獻(xiàn)信息
LXFS 538	Antitumor assay	6 mg/kg		Antitumor activity against human LXFS 538 cells xenografted in NMRI nu/nu mouse assessed as tumor regression at 6 mg/kg, ip measured on day 13	23394180
HCT116	Growth inhibition assay		72 hrs	Growth inhibition of human HCT116 cells after 72 hrs by MTS assay, IC50=0.0011μM	26396688
MCF7	Antiproliferative assay		48 hrs	Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50=1.3μM	24184776
HeLa	Antiproliferative assay		48 hrs	Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay, IC50=1μM	24184776
NCI-H1299	Growth inhibition assay		72 hrs	Growth inhibition of human NCI-H1299 cells after 72 hrs by Alamar blue assay, GI50=0.082μM	23394180
BxPC3	Growth inhibition assay		72 hrs	Growth inhibition of human BxPC3 cells after 72 hrs by Alamar blue assay, GI50=0.08μM	23394180
PC3	Growth inhibition assay		72 hrs	Growth inhibition of human PC3 cells after 72 hrs by Alamar blue assay, GI50=0.05μM	23394180
HCT116	Growth inhibition assay		72 hrs	Growth inhibition of human HCT116 cells after 72 hrs by Alamar blue assay, GI50=0.025μM	23394180
LNCAP	Growth inhibition assay		72 hrs	Growth inhibition of human LNCAP cells after 72 hrs by Alamar blue assay, GI50=0.022μM	23394180
NCI-H1299	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H1299 cells after 72 hrs by Alamar blue assay, GI50=0.082μM	22248262
BxPC3	Antiproliferative assay		72 hrs	Antiproliferative activity against human BxPC3 cells after 72 hrs by Alamar blue assay, GI50=0.08μM	22248262
K562	Antiproliferative assay		72 hrs	Antiproliferative activity against human K562 cells after 72 hrs by Alamar blue assay, GI50=0.071μM	22248262
hTERT-HME1	Antiproliferative assay		72 hrs	Antiproliferative activity against human hTERT-HME1 cells after 72 hrs by Alamar blue assay, GI50=0.032μM	22248262
HCT116	Antiproliferative assay		72 hrs	Antiproliferative activity against human HCT116 cells after 72 hrs by Alamar blue assay, GI50=0.025μM	22248262
Rh30	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD 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
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 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
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 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-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 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
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 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
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 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
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 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
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
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 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
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 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
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells	29435139
點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù)

生物活性

產(chǎn)品描述

特性

Ispinesib是一種有效可逆的特定有絲分裂驅(qū)動(dòng)蛋白(KSP)變構(gòu)抑制劑。

靶點(diǎn)

KSP (HsEg5) ^[1]
(Cell-free assay)

1.7 nM(Ki app)

體外研究(In Vitro)
體外研究活性	Ispinesib 是有效可逆的特定KSP變構(gòu)抑制劑，KSP與微管的結(jié)合性能，通過抑制ADP釋放而不改變微管中KSP-ADP復(fù)合體的釋放，而擾亂KSP的運(yùn)動(dòng)。^[1] Ispinesib作用于一系列腫瘤細(xì)胞系, 包括Colo205, Colo201, HT-29, M5076, Madison-109,和MX-1, IC50為1.2 nM 到 9.5 nM，具有很強(qiáng)細(xì)胞毒性。^[2] 15 nM 和 30 nM Ispinesib作用于PC-3前列腺癌細(xì)胞, 通過調(diào)節(jié)控制凋亡，細(xì)胞增殖，細(xì)胞周期，和信號(hào)的基因表達(dá)水平，如EGFR, p27, p15, 和IL-11，而抑制細(xì)胞增殖和誘導(dǎo)凋亡。^[3] 7.4 nM–600 nM Ispinesib 作用于一組53種乳腺癌細(xì)胞系,具有廣譜抑制活性。150 nM Ispinesib 作用于BT-474 和MDA-MB-468細(xì)胞,誘導(dǎo)凋亡, 提高凋亡細(xì)胞比例，降低抗凋亡的Bcl-XL水平,和提高促凋亡的Bax和Bid 水平。^[4]
激酶實(shí)驗(yàn)	人類KSP ATP酶活性和Ispinesib抑制的穩(wěn)定動(dòng)力學(xué)分析
激酶實(shí)驗(yàn)	使用丙酮酸激酶-乳酸脫氫酶檢測(cè)體系進(jìn)行驅(qū)動(dòng)蛋白的特異性分析，伴隨著NADH氧化產(chǎn)生ADP。在340 nm處檢測(cè)吸光度的變化。使用納摩爾濃度KSP進(jìn)行穩(wěn)態(tài)研究，使用一個(gè)敏感的熒光為基礎(chǔ)的檢測(cè)系統(tǒng)，利用丙酮酸激酶，丙酮酸氧化酶，辣根過氧化物酶（HRP）耦合的檢測(cè)體系，伴隨著Amplex紅色熒光試劑氧化為試鹵靈而生成ADP。通過熒光檢測(cè)產(chǎn)生的試鹵靈。在含10 μM 紫杉醇的PEM25 buffer [25 mM Pipes-K⁺ (pH 6.8), 2 mM MgCl₂, 1 mM EGTA]中進(jìn)行穩(wěn)態(tài)生化試驗(yàn)。在含500 μM ATP, 5 μM 微管,和1 nM KSP的PEM25 buffer中測(cè)定抑制穩(wěn)定的IC50值。通過劑量-反應(yīng)曲線獲得Ispinesib的K_i?app(明顯的抑制劑解離常數(shù))值, 通過使用Morrison方程明確糾正酶濃度。在穩(wěn)態(tài)情況下測(cè)定抑制劑形態(tài)（競(jìng)爭(zhēng)性，非競(jìng)爭(zhēng)性，無(wú)競(jìng)爭(zhēng)力的，或者混合生物）。
細(xì)胞實(shí)驗(yàn)	細(xì)胞系	Breast 乳腺癌細(xì)胞，包括MCF-7, HCC1954, MDA-MB-468,和KPL4
	濃度	0.085 nM-33 μM
	孵育時(shí)間	72小時(shí)
	方法	指數(shù)生長(zhǎng)期細(xì)胞接種在96孔板上，用Ispinesib處理72小時(shí)。然后使用CellTiter-Glo測(cè)量細(xì)胞生長(zhǎng), 并使用BioTek FLx800測(cè)定熒光值。分析數(shù)據(jù)，計(jì)算IC50值。

體內(nèi)研究(In Vivo)
體內(nèi)研究活性	Ispinesib按4.5 mg/kg-15 mg/kg劑量作用于攜帶移植瘤的小鼠模型，有效抑制Colo205, Colo201, HT-29細(xì)胞，但是不抑制MX-1細(xì)胞。SB-715992按6 mg/kg-10 mg/kg劑量處理，也抑制小鼠實(shí)體瘤，包括 Madison 109 肺癌, M5076肉瘤,及L1210和P388白血病。^[2] Ispinesib 按8 mg/kg-10 mg/kg劑量作用于攜帶乳腺癌細(xì)胞MCF-7, HCC1954, MDA-MB-468,和KPL4移植瘤的小鼠,抑制腫瘤生長(zhǎng)。^[4]
動(dòng)物實(shí)驗(yàn)	Animal Models	攜帶MCF7, KPL4,和HCC1954細(xì)胞的(nu/nu)裸鼠模型，攜帶MDA-MB-468 細(xì)胞的SCID小鼠模型
	Dosages	10 mg/kg作用于裸鼠，8 mg/kg作用于SCID 鼠
	Administration	3倍劑量腹腔注射，每隔四天進(jìn)行一次

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試驗(yàn)信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT00607841	Terminated	Breast Neoplasms	Cytokinetics	December 2007	Phase 1
NCT00354250	Completed	Recurrent Renal Cell Cancer\|Stage III Renal Cell Cancer\|Stage IV Renal Cell Cancer	National Cancer Institute (NCI)	May 2006	Phase 2
NCT00097409	Completed	Ovarian Cancer	GlaxoSmithKline	December 2004	Phase 2
NCT00119171	Completed	Solid Tumor Cancer	GlaxoSmithKline	November 2004	Phase 1

參考文獻(xiàn)
[1] Lad L, et al. Biochemistry, 2008, 47(11), 3576-3585. [2] Johnson RK, et al. Proc Am Assoc Cancer Res, 2002, 43, 269. [3] Davis DA, et al. BMC Cancer, 2006, 6, 22. [4] Purcell JW, et al. Clin Cancer Res, 2010, 16(2), 566-576. + 展開

參考文獻(xiàn)

[1] Lad L, et al. Biochemistry, 2008, 47(11), 3576-3585.
[2] Johnson RK, et al. Proc Am Assoc Cancer Res, 2002, 43, 269.
[3] Davis DA, et al. BMC Cancer, 2006, 6, 22.

[4] Purcell JW, et al. Clin Cancer Res, 2010, 16(2), 566-576.

+ 展開

化學(xué)信息&溶解度

分子量	517.06	分子式	C₃₀H₃₃ClN₄O₂
CAS號(hào)	336113-53-2	SDF	Download Ispinesib (SB-715992) SDF
Smiles	CC1=CC=C(C=C1)C(=O)N(CCCN)C(C2=NC3=C(C=CC(=C3)Cl)C(=O)N2CC4=CC=CC=C4)C(C)C
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1年-80°C溶于溶劑
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1個(gè)月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 103 mg/mL ( (199.2 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Ethanol : 103 mg/mL (199.2 mM)

Water : Insoluble

DMSO : 103 mg/mL ( (199.2 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Ethanol : 103 mg/mL (199.2 mM)

Water : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

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

動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計(jì)算器分子量計(jì)算器

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動(dòng)物的藥量）

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

第二步：請(qǐng)輸入動(dòng)物體內(nèi)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(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計(jì)算結(jié)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(qǐng)先聯(lián)系Selleck）；

體內(nèi)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(nèi)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(jìn)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(xiàng)

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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