AT9283

目錄號：S1134 Purity: 99.82%

AT9283是一種有效的JAK2/3抑制劑，無細(xì)胞試驗(yàn)中IC50為1.2 nM/1.1 nM；對Aurora A/B，Abl1(T315I)也有效。

AT9283 Chemical Structure

CAS: 896466-04-9

規(guī)格	價格	庫存
10mM (1mL in DMSO)	2444.92	現(xiàn)貨
2mg	818.33	現(xiàn)貨
5mg	1380.26	現(xiàn)貨
50mg	6298.93	現(xiàn)貨
1g	24488.1	現(xiàn)貨
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產(chǎn)品質(zhì)控

批次：純度： 99.82%

99.82

AT9283相關(guān)產(chǎn)品

相關(guān)靶點(diǎn)	JAK1 JAK2 JAK3 Tyk2	點(diǎn)擊展開
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相關(guān)化合物庫	激酶抑制劑庫 FDA藥物庫天然產(chǎn)物庫酪氨酸激酶抑制劑分子庫 JAK-STAT信號通路庫	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	孵育時間	活性描述	文獻(xiàn)信息
Sf9	Function assay	10 uM	60 mins	Displacement of BODIPY-ATP from C-terminal thrombin-cleavable hexa-histidine tagged human JAK2 JH2 pseudokinase domain (536 to 812 residues) W659A/W777A/F794H mutant expressed in baculovirus-infected Sf9 cells at 10 uM after 60 mins by high-throughput flu	28626521
HCT116	Function assay	20 mg/kg		Cmax in BALB/c mouse bearing human HCT116 cells at 20 mg/kg, ip, Cmax=8.4μM	19143567
HCT116	Function assay	5 mg/kg		Cmax in BALB/c mouse bearing human HCT116 cells at 5 mg/kg, iv, Cmax=4.9μM	19143567
HCT116	Function assay	10 mg/kg		Cmax in BALB/c mouse bearing human HCT116 cells at 10 mg/kg, po, Cmax=0.45μM	19143567
HCT116	Cytotoxicity assay		10 to 14 days	Cytotoxicity against human HCT116 cells assessed as number of colonies after 10 to 14 days by colony forming assay, IC50=0.012μM	19143567
HT-29	Antitumor assay		72 hrs	Antitumor activity against human HT-29 cells after 72 hrs by MTT assay, IC50=0.383μM	23664099
A549	Antitumor assay		72 hrs	Antitumor activity against human A549 cells after 72 hrs by MTT assay, IC50=0.512μM	23664099
LoVo	Antitumor assay		72 hrs	Antitumor activity against human LoVo cells after 72 hrs by MTT assay, IC50=0.553μM	23664099
K562	Antitumor assay		72 hrs	Antitumor activity against human K562 cells after 72 hrs by MTT assay, IC50=1.6μM	23664099
U937	Antitumor assay		72 hrs	Antitumor activity against human U937 cells after 72 hrs by MTT assay, IC50=6.7μM	23664099
BL21 (DE3)	Function assay		30 mins	Inhibition of His6-tagged MELK catalytic domain (1 to 340 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) cells using Bcl-GL as substrate measured after 30 mins in presence of [gamma32P]ATP by liquid scintillation counting method, IC50=0.685μM	28351607
Sf9	Function assay			Binding affinity to N-terminal TEV-cleavable hexa-histidine tagged human JAK2 JH1 domain (840 to 1132 residues) expressed in baculovirus-infected Sf9 cells by ITC assay, Kd=0.011μM	28626521
Sf9	Function assay			Binding affinity to C-terminal thrombin-cleavable hexa-histidine tagged human JAK2 JH2 pseudokinase domain (536 to 812 residues) W659A/W777A/F794H mutant expressed in baculovirus-infected Sf9 cells by ITC assay, Kd=1.323μM	28626521
HCT116	Function assay			Inhibition of Aurora B kinase in human HCT116 cells assessed as reduction in polyploid phenotype, IC50=0.03μM	28918096
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
U-2 OS	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS 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
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH 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
Rh18	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 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
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
fibroblast cells	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 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
點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù)

生物活性

產(chǎn)品描述

AT9283是一種有效的JAK2/3抑制劑，無細(xì)胞試驗(yàn)中IC50為1.2 nM/1.1 nM；對Aurora A/B，Abl1(T315I)也有效。

特性

AT9283是有效的pan-aurora 抑制劑。

靶點(diǎn)

JAK3 ^[1] (Cell-free assay)	JAK2 ^[1] (Cell-free assay)	Aurora A ^[1] (Cell-free assay)	Aurora B ^[1] (Cell-free assay)	Abl1 (T315I) ^[1] (Cell-free assay)	點(diǎn)擊更多
1.1 nM	1.2 nM	~3.0 nM	~3.0 nM	4 nM	點(diǎn)擊更多

體外研究(In Vitro)
體外研究活性	在體外, AT9283有效抑制多種激酶，包括 Aurora A, Aurora B, JAK3, JAK2和 Abl，IC50分別為3 nM, 3 nM, 1.1 nM, 1.2 nM 和 4 nM。AT9283 作用于HCT116 細(xì)胞，通過抑制Aurora B 激酶活性，產(chǎn)生明顯的多倍體表現(xiàn)型，IC50為30 nM。而且, AT9283也有效抑制HCT116形成集落。^[1]
激酶實(shí)驗(yàn)	Aurora A和 Aurora B激酶實(shí)驗(yàn)
激酶實(shí)驗(yàn)	在DELFIA格式中進(jìn)行Aurora A 和 B實(shí)驗(yàn)。Aurora A 酶和AT9283 及 3 μM 肽底物 (生物素-CGPKGPGRRGRRRTSSFAEG)在 10 mM MOPS, pH 7, 0.1 mg/mL BSA, 0.001% Brij-35, 0.5% 甘油, 0.2 mM EDTA, 10 mM MgCl₂, 0.01% β-巰基乙醇, 15 μM ATP,和2.5% DMSO混合物中溫育。Aurora B 酶和AT9283,及3 μM 以上底物在25 mM Tris, pH 8.5, 5 mM MgCl₂, 0.1 mg/mL BSA, 0.025% Tween-20, 1 mM DTT, 15 μM ATP, 和 2.5% DMSO的混合物中溫育。Aurora A 和 Aurora B反應(yīng)分別進(jìn)行60分鐘和45-90分鐘,然后使用 EDTA進(jìn)行淬火。反應(yīng)混合物轉(zhuǎn)移到親和素包被的實(shí)驗(yàn)板上，通過時間分辨熒光技術(shù)(激發(fā)波長, 337 nm;發(fā)射波長, 620 nm)，使用特定磷酸抗體和銪標(biāo)記的二抗測量磷酸化的肽。
細(xì)胞實(shí)驗(yàn)	細(xì)胞系	HCT 116 細(xì)胞
	濃度	1 nM 到10 μM
	孵育時間	72 小時
	方法	HCT 116細(xì)胞培養(yǎng)在DMEM +10% FBS + GLUTAMAX I 中。細(xì)胞接種在黑色96孔平底組織培養(yǎng)板中，孔中含200 μL 培養(yǎng)基，在37^oC 下溫育約16小時，在濕潤且含5% CO₂ 的環(huán)境下溫育約16小時。使用9種不同濃度AT9283 (為 1 nM到 10 μM, 對照組為DMSO) 處理細(xì)胞，然后再溫育72小時。標(biāo)記對細(xì)胞多倍體形態(tài)學(xué)的觀察。記錄產(chǎn)生明顯多倍體所需AT9283的濃度。細(xì)胞按75−100個細(xì)胞/mL接種在有關(guān)培養(yǎng)基中，然后轉(zhuǎn)移到6-或24-孔組織培養(yǎng)板上，然后覆蓋培養(yǎng)16小時。AT9283(11 種濃度，0.1 nM 到 10 μM) 或?qū)φ战M(DMSO) 加到復(fù)制孔中，DMSO終濃度為0.1%。隨后加入AT9283，集落生長10和14天，計算最佳離散菌落數(shù)。集落在2 mL Carnoys 固定液(25% 乙酸,75% MeOH)中固定，然后在2 mL 0.4% w/v 結(jié)晶紫中染色。計算每孔中集落數(shù)。使用Prism Graphpad 軟件繪制IC50曲線，通過S形劑量反應(yīng)曲線計算IC50值。
實(shí)驗(yàn)圖片	檢測方法	檢測指標(biāo)	實(shí)驗(yàn)圖片	PMID
實(shí)驗(yàn)圖片	Growth inhibition assay	Cell viability		21430070

體內(nèi)研究(In Vivo)
體內(nèi)研究活性	AT9283 按15 mg/kg和 20 mg/kg劑量作用于攜帶HCT116人結(jié)腸癌移植瘤的小鼠，持續(xù)16天，顯著抑制腫瘤生長，抑制分別達(dá)67%和76%。此外, 與血漿(半衰期為0.5小時)相比，AT9283口服給藥小鼠，也具有顯著較長的半衰期。^[1]
動物實(shí)驗(yàn)	Animal Models	后腿側(cè)皮下注射HCT116細(xì)胞的雄性BALB/c小鼠
	Dosages	15 mg/kg 和 20 mg/kg
	Administration	腹腔注射

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)
NCT01145989	Completed	Multiple Myeloma	NCIC Clinical Trials Group\|Astex Pharmaceuticals Inc.\|Canadian Cancer Trials Group	February 15 2011	Phase 2
NCT00443976	Completed	Non-Hodgkins Lymphoma\|Unspecified Adult Solid Tumor Protocol Specific	NCIC Clinical Trials Group\|Astex Pharmaceuticals Inc.\|Canadian Cancer Trials Group	January 30 2007	Phase 1

參考文獻(xiàn)
[1] Howard S, et al. J Med Chem, 2009, 52(2), 379-388. [2] Qi W, et al. Int J Cancer. 2012, 130(12), 2997-3005. [3] Santo L, et al. Clin Cancer Res. 2011, 17(10), 3259-3271.

參考文獻(xiàn)

[1] Howard S, et al. J Med Chem, 2009, 52(2), 379-388.
[2] Qi W, et al. Int J Cancer. 2012, 130(12), 2997-3005.
[3] Santo L, et al. Clin Cancer Res. 2011, 17(10), 3259-3271.

化學(xué)信息&溶解度

分子量	381.43	分子式	C₁₉H₂₃N₇O₂
CAS號	896466-04-9	SDF	Download AT9283 SDF
Smiles	C1CC1NC(=O)NC2=C(NN=C2)C3=NC4=C(N3)C=C(C=C4)CN5CCOCC5
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復(fù)凍融！	1年-80°C溶于溶劑
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復(fù)凍融！	1個月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 76 mg/mL ( (199.25 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Ethanol : 25 mg/mL (65.54 mM)

Water : Insoluble

DMSO : 76 mg/mL ( (199.25 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Ethanol : 76 mg/mL (199.25 mM)

Water : Insoluble

摩爾濃度計算器

體內(nèi)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(nèi)配方計算器

實(shí)驗(yàn)計算

摩爾濃度計算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計算器分子量計算器

動物體內(nèi)配方計算器（澄清溶液）

第一步：請輸入基本實(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(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(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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