AT9283 | Aurora/JAK Inhibitor | AmBeed-信号通路专用抑制剂

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AT9283 {[allProObj[0].p_purity_real_show]}

货号：A335492

AT9283 is a multi-targeted inhibitor with IC50s of 4, 1.2, 1.1 and approximate 3 nM for Bcr-Abl (T315I), JAK2 and JAK3, Aurora A and Aurora B, respectively.

AT9283 化学结构
CAS号：896466-04-9

AT9283 3D分子结构
CAS号：896466-04-9

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AT9283 纯度/质量文件产品仅供科研

货号：A335492 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Cell, 2024, 101755. Ambeed. [ A399663 ]; • EMBO J., 2024. Ambeed. [ A295334 ]; • JMC, 2024, 67(20): 18265-18289. Ambeed. [ A538667 , A341145 , A117430 , A172297 ]; • JMC, 2024. Ambeed. [ A210558 , A1518164 ]; • Cell Death Discov., 2024, 10, 436. Ambeed. [ A384235 ]; 更多 >

转化生长因子-β 亚型比较
Aurora Kinase 亚型比较
JAK 亚型比较
Bcr-Abl 亚型比较

产品名称	ALK1 ↓ ↑	ALK2 ↓ ↑	ALK3 ↓ ↑	ALK4 ↓ ↑	ALK6 ↓ ↑	Smad3 ↓ ↑	TGF-β ↓ ↑	TGFβRI/ALK5 ↓ ↑	TGFβRII ↓ ↑	纯度
LDN193189	++++ ALK1, IC50: 0.8 nM	++++ ALK2, IC50: 0.8 nM	+++ ALK3, IC50: 5.3 nM		+++ ALK6, IC50: 16.7 nM					99%+
LDN-212854	++++ ALK1, IC50: 2.4 nM	++++ ALK2, IC50: 1.3 nM	+ ALK3, IC50: 85.8 nM	+ ALK4, IC50: 2133 nM				+ ALK5, IC50: 9276 nM		99%+
ML347	++ ALK1, IC50: 46 nM	++ ALK2, IC50: 32 nM								98%
K02288	++++ ALK1, IC50: 1.8 nM	++++ ALK2, IC50: 1.1 nM	++ ALK3, IC50: 34.4 nM		+++ ALK6, IC50: 6.4 nM					99%+
LDN-193189 dihydrochloride	++++ ALK1, IC50: 0.8 nM	++++ ALK2, IC50: 0.8 nM	+++ ALK3, IC50: 5.3 nM		+++ ALK6, IC50: 16.7 nM					99%
LDN-214117		++ ALK2, IC50: 24 nM								98%
DMH-1		+ ALK2, IC50: 107.9 nM								99%+
SB-505124				+ ALK4, IC50: 129 nM				++ ALK5, IC50: 47 nM		99%+
Vactosertib				+++ ALK4, IC50: 13 nM				+++ ALK5, IC50: 11 nM		99%+
Alantolactone						✔				98%
SIS3						✔				97%
Pirfenidone							✔			98%
Hesperetin							✔			97%
RepSox								++++ TGFβR1(ALK5), IC50: 4 nM		98%
GW788388								+++ ALK5, IC50: 18 nM		98%
LY364947								++ TGFβRI, IC50: 59 nM	+ TGFβRII, IC50: 0.4 μM	98%
SD-208								++ TGF-βRI (ALK5), IC50: 48 nM		98%
SB-525334								+++ TGFβR1(ALK5), IC50: 14.3 nM		99%+
LY2109761								++ TβRI, Ki: 38 nM	+ TβRII, Ki: 300 nM	99%+
Galunisertib								++ TβRI, IC50: 56 nM		98%
SB 431542								+ ALK5, IC50: 94 nM		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	Aurora A ↓ ↑	Aurora B ↓ ↑	Aurora C ↓ ↑	其他靶点	纯度
BI-847325	++ Aurora A (Human), IC50: 25 nM	++++ Aurora B (Xenopus laevis), IC50: 3 nM	++ Aurora C (Human), IC50: 15 nM		99%+
CCT 137690	++ Aurora A, IC50: 15 nM	++ Aurora B, IC50: 25 nM	++ Aurora C, IC50: 19 nM		99%+
MK-5108	++++ Aurora A, IC50: 0.064 nM				99%+
KW-2449	+ Aurora A, IC50: 48 nM			FLT3	99%+
Tozasertib	++++ Aurora A, Ki app: 0.6 nM	++ Aurora B, Ki app: 18 nM	+++ Aurora C, Ki app: 4.6 nM	FLT3,Bcr-Abl	99%+
AT9283	++++ Aurora A, IC50: ~3.0 nM	++++ Aurora B, IC50: ~3.0 nM			99%+
MLN8054	+++ Aurora A, IC50: 4 nM	+ Aurora B, IC50: 172 nM			99%+
ZM-447439	+ Aurora A, IC50: 110 nM	+ Aurora B, IC50: 130 nM		Src	99%+
TCS7010	++++ Aurora A, IC50: 3.4 nM				99%+
TAK-901	++ Aurora A-TPX2, IC50: 21 nM	++ Aurora B-INCENP, IC50: 15 nM			99%+
Danusertib	+++ Aurora A, IC50: 13 nM	+ Aurora B, IC50: 79 nM	+ Aurora C, IC50: 61 nM	RET	99%+
MK-8745	++++ Aurora A, IC50: 0.6 nM				99+%
PHA-680632	++ Aurora A, IC50: 27 nM	+ Aurora B, IC50: 135 nM	+ Aurora C, IC50: 120 nM	FLT3	99%+
AMG 900	+++ Aurora A, IC50: 5 nM	+++ Aurora B, IC50: 4 nM	++++ Aurora C, IC50: 1 nM		99%+
Alisertib	++++ Aurora A, IC50: 1.2 nM				99%+
ENMD-2076	+++ Aurora A, IC50: 14 nM	+ Aurora B, IC50: 350 nM		FLT3,RET	98%
JNJ-7706621	+++ Aurora A, IC50: 11 nM	++ Aurora B, IC50: 15 nM			99%+
CYC-116	+++ Aurora A, Ki: 8 nM	+++ Aurora B, Ki: 9 nM		FLT3	99%+
Reversine	+++ Aurora A, IC50: 12 nM	+++ Aurora B, IC50: 13 nM	++ Aurora C, IC50: 20 nM		98%
CCT129202	++ Aurora A, IC50: 42 nM	+ Aurora B, IC50: 198 nM	+ Aurora C, IC50: 227 nM		98%
SNS-314 mesylate	+++ Aurora A, IC50: 9 nM	++ Aurora B, IC50: 31 nM	++++ Aurora C, IC50: 3 nM		99%+
Barasertib-HQPA		++++ Aurora B, IC50: 0.37 nM			99%+
Hesperadin		+ Aurora B (human), IC50: 250 nM			98%
GSK-1070916		++++ Aurora B-INCENP, IC50: 3.5 nM	+++ Aurora C-INCENP, IC50: 6.5 nM	SIK,Tie-2	99%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	JAK1 ↓ ↑	JAK2 ↓ ↑	JAK3 ↓ ↑	Tyk2 ↓ ↑	其他靶点	纯度
Decernotinib	+++ JAK1, Ki: 11 nM JAK1, IC50: 11 nM	+++ JAK2, Ki: 13 nM	++++ JAK3, Ki: 2.5 nM	+++ TYK2, Ki: 13 nM		99%+
ZM39923 HCl	+ JAK1, pIC50: 4.4		+ JAK3, pIC50: 7.1		EGFR	97%
Cerdulatinib	+++ JAK1, IC50: 12 nM	+++ JAK2, IC50: 6 nM	+++ JAK3, IC50: 8 nM	++++ TYK2, IC50: 0.5 nM		99%+
Momelotinib	+++ JAK1, IC50: 11 nM	++ JAK2, IC50: 18 nM	+ JAK3, IC50: 155 nM			99%+
XL019	+ JAK1, IC50: 134.3 nM	++++ JAK2, IC50: 2.2 nM	+ JAK3, IC50: 214.2 nM		FLT3	99%+
Ruxolitinib	+++ JAK1, IC50: 3.3 nM	++++ JAK2, IC50: 2.8 nM				98%
Tofacitinib	+ JAK1, IC50: 112 nM	++ JAK2, IC50: 20 nM	++++ JAK3, IC50: 1 nM			98%
Ruxolitinib (S enantiomer)	+++ JAK1, IC50: 3.3 nM	++++ JAK2, IC50: 2.8 nM		++ TYK2, IC50: 19 nM		98%
Filgotinib	+++ JAK1, IC50: 10 nM	++ JAK2, IC50: 28 nM	+ JAK3, IC50: 810 nM	+ TYK2, IC50: 116 nM		99%
Baricitinib	+++ JAK1, IC50: 5.9 nM	+++ JAK2, IC50: 5.7 nM		++ TYK2, IC50: 53 nM		99%
Gandotinib	++ JAK1, IC50: 19.8 nM	++++ JAK2, IC50: 0.288 nM JAK2 (V617F), Ki: 0.245 nM	++ JAK3, IC50: 48.0 nM	++ TYK2, IC50: 44 nM	FLT3	99%+
Oclacitinib maleate	+++ JAK1, IC50: 10nM	++ JAK2, IC50: 18nM	+ JAK3, IC50: 99nM	+ TYK2, IC50: 84nM		98+%
NVP-BSK805 2HCl	++ JAK1, IC50: 31.63 nM	++++ JAK2, IC50: ~0.5 nM	++ JAK3, IC50: 18.68 nM	+++ TYK2, IC50: 10.76 nM		99+%
Peficitinib		✔				98%
Go6976		✔			FLT3	99%+
AZD-1480		++++ JAK2, IC50: 0.26 nM				99%+
Fedratinib		+++ JAK2 (V617F), IC50: 3 nM JAK2, IC50: 3 nM			FLT3,RET	99%+
WP1066		+ JAK2, IC50: 2.3 μM				98%
Curcumol		✔				98%
AZ960		++++ JAK2, Ki: 0.45 nM JAK2, IC50: <3 nM				97%
GLPG0634 analog		✔				99%+
CEP-33779		++++ JAK2, IC50: 1.8 nM				99%+
FLLL32		+ JAK2, IC50: <5 μM				99%+
WHI-P154			+ JAK3, IC50: 1.8 μM		EGFR,Src,VEGFR	98%
BMS-911543		++++ JAK2, IC50: 1.1 nM	+ JAK3, IC50: 75 nM	++ TYK2, IC50: 66 nM		98%
TG101209		+++ JAK2, IC50: 6 nM	+ JAK3, IC50: 169 nM		FLT3,RET	99%+
AT9283		++++ JAK2, IC50: 1.2 nM	++++ JAK3, IC50: 1.1 nM			99%+
Pacritinib		++ JAK2 (V617F), IC50: 19 nM JAK2, IC50: 23 nM	+ JAK3, IC50: 520 nM	++ TYK2, IC50: 50 nM	FLT3	97%
Tofacitinib citrate		++ JAK2, IC50: 20 nM	++++ JAK3, IC50: 1 nM			99%
FM-381			++++ JAK3, IC50: 127 pM			98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	Abl ↓ ↑	Bcr-Abl ↓ ↑	其他靶点	纯度
NVP-BHG 712	+ c-Abl, IC50: 1.667 μM			99%+
KW-2449	+++ Abl, IC50: 14 nM Abl (T315I), IC50: 4 nM		FLT3	99%+
Ponatinib	++++ Abl, IC50: 0.37 nM			98%
AT9283				99%+
Imatinib Mesylate	+ v-Abl, IC50: 600 nM		c-Kit,PDGFR	99%
Danusertib	++ Abl, IC50: 25 nM		RET	99%+
Rebastinib	++++ p-Abl1 (native), IC50: 0.75 nM u-Abl1 (T315I), IC50: 5 nM		FLT3,Tie-2	99%+
PP121	++ Abl, IC50: 18 nM		PDGFR,VEGFR	99%+
GNF-7	+++ M351T, IC50: 133 nM E255V, IC50: 122 nM			99%+
Olverembatinib dimesylate	++++ Abl, IC50: 0.34 nM Abl (G250E), IC50: 0.35 nM			99%
Dasatinib monohydrate	++++ Abl , IC50: 0.6 nM		Src	98%
Dasatinib	++++ Abl, IC50: 0.6 nM		Src	98%
Bafetinib	+++ Abl, IC50: 5.8 nM			98+%
GNF-2		+ Bcr-Abl (SUP-B15 cell line), IC50: 268 nM Bcr-Abl (K562 cell line), IC50: 273 nM		98%+
Degrasyn		+ Bcr-Abl, IC50: 1.8 μM	DUB	98+%
GNF-5		++ Bcr-Abl, IC50: 220 nM		98%
Radotinib		++ BCR-ABL1, IC50: 34 nM		98+%
PD173955			Src	99%+
Nilotinib		++ Bcr-Abl, IC50: <30 nM		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

AT9283 生物活性

靶点	JAK3 JAK3, IC50:1.1 nM Tyk2 TYK2, IC50:1 nM-10 nM JAK2 JAK2, IC50:1.2 nM Aurora A Aurora A, IC50:~3.0 nM
描述	The Aurora family of serine/threonine kinases, which consists of Aurora A, B and C, plays an important role in chromosome alignment, segregation, and cytokinesis during mitosis. AT9283 is a multiple target inhibitor, most potent to JAK2/3 as well as Aurora A/B and Abl(T315I) with IC50 values of 1.2nM, 1.1nM, 3nM, 3nM and 4nM (measure by kinase assays), respectively, less potent to GSK-3β, FGFR2, VEGFR3/FLT4, Mer, RET, RSK2, RSK3, TYK2 and YES with IC50 ranging in 1-10nM^[1]. Treatment with AT9283 at concentration of 100nM for 2h resulted in endoreduplication, as well as a decrease in levels of phosphorylated histone H3 in HCT116 cells, indicating inhibition of Aurora B kinase. p53 induction and increased cleavage of PARP can be observed, followed ultimately by cell death by 14 days. The colony formation can be inhibited at dose of 7.7-20nM in a panel of tumor cell lines of different origins, including HCT116, HT-29, SW620, A2780, A549, MCF7 and MIA-Pa-Ca-2. Consistent with the in vitro study, a single of 10 mg/kg dose of AT9283 significantly decreased the level of phosphorylated histone H3 for up to 3h in tumor samples from HCT116 tumor bearing mice^[2]. Exposure to 1μM AT9283 caused a decrease in p-Stat5 1 h after the start of treatment, confirming inhibition of Jak2, as well as showed anti-proliferation with IC50 values ranging in 16-110nM in a number of Jak2-dependent cell lines, HEL, TF-1 and Ba/F3 ETV6-JAK2. AT9283 at dose of 10 mg/kg, bid, was efficacious in a Jak2-dependent murine leukemic model^[3]. Injection with AT9283 interperitoneally at dose of 15 and 20 mg/kg for 16 days produced a significant tumor growth inhibition of 67% (% T/C ) 33%) and 76% (% T/C ) 24%), respectively, in immunocompromised BALB/c nude mice bearing early stage HCT116 human colon carcinoma xenografts^[1].
作用机制	For Aurora A, AT9283 can sit deeply in the ATP-binding site of Aurora A^[1]. For JAK2, AT9283 can bound to the active site of the Jak2 kinase domain^[3].

AT9283 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
A549 cells		Function assay	72 h	Antitumor activity against human A549 cells after 72 hrs by MTT assay, IC50=0.512 μM	23664099
HCT116 cells		Cytotoxic assay	10-14 days	Cytotoxicity against human HCT116 cells assessed as number of colonies after 10 to 14 days by colony forming assay, IC50=0.012 μM	19143567
HT-29 cells		Function assay	72 h	Antitumor activity against human HT-29 cells after 72 hrs by MTT assay, IC50=0.383 μM	23664099
K562 cells		Function assay	72 h	Antitumor activity against human K562 cells after 72 hrs by MTT assay, IC50=1.6 μM	23664099

AT9283 动物研究

Dose	Mice: min = 15 mg/kg, max = 20 mg/kg^[4]
Administration	i.p.

AT9283 临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00985868	Unspecified Childhood Solid Tu... 展开 >>mor, Protocol Specific 收起 <<	Phase 1	Active, not recruiting	December 2018	United Kingdom ... 展开 >> Birmingham Children's Hospital Birmingham, England, United Kingdom, B4 6NH Leeds General Infirmary Leeds, England, United Kingdom, LS9 7TF Royal Manchester Children's Hospital Manchester, England, United Kingdom, M27 4HA Great North Children's Hospital, Royal Victoria Infirmary Newcastle-Upon-Tyne, England, United Kingdom, NE1 4LP Royal Marsden - Surrey Sutton, England, United Kingdom, SM2 5PT 收起 <<
NCT01431664	Leukemia	Phase 1	Completed	-	United Kingdom ... 展开 >> Royal Marsden Hospital Surrey, London, United Kingdom, SM2 5PT Birmingham Children's Hospital Birmingham,, United Kingdom, B4 6NH Leeds General Infirmary Leeds, United Kingdom, LS1 3EX Royal Manchester Children's Hospital Manchester, United Kingdom, M13 9WL Great North Children's Hospital, Royal Victoria Infirmary Newcastle upon Tyne, United Kingdom, NE1 4LP 收起 <<
NCT00522990	Acute Myeloid Leukemia ... 展开 >> Acute Lymphoblastic Leukemia Chronic Myeloid Leukemia Myelodysplastic Syndromes Myelofibrosis 收起 <<	Phase 1 Phase 2	Terminated(Recommended Phase I... 展开 >>I dose determined) 收起 <<	-	United States, Alabama ... 展开 >> University of Alabama at Birmingham Birmingham, Alabama, United States, 35294 United States, Texas The University of Texas, MD Anderson Cancer Center Houston, Texas, United States, 77030 收起 <<

AT9283 参考文献

[1]Howard S, Berdini V, et al. Fragment-based discovery of the pyrazol-4-yl urea (AT9283), a multitargeted kinase inhibitor with potent aurora kinase activity. J Med Chem. 2009 Jan 22;52(2):379-88.

[2]Curry J, Angove H, et al. Aurora B kinase inhibition in mitosis: strategies for optimising the use of aurora kinase inhibitors such as AT9283. Cell Cycle. 2009 Jun 15;8(12):1921-9. Epub 2009 Jun 15.

[3]Dawson MA, Curry JE, et al. AT9283, a potent inhibitor of the Aurora kinases and Jak2, has therapeutic potential in myeloproliferative disorders. Br J Haematol. 2010 Jul;150(1):46-57.

[4]Qi W, Liu X, et al. AT9283, a novel aurora kinase inhibitor, suppresses tumor growth in aggressive B-cell lymphomas. Int J Cancer. 2012;130(12):2997-3005.

AT9283 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.62mL

0.52mL

0.26mL

13.11mL

2.62mL

1.31mL

26.22mL

5.24mL

2.62mL

AT9283 技术信息

CAS号	896466-04-9
分子式	C₁₉H₂₃N₇O₂
分子量	381.432

别名
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,2-8°C

溶解度

DMSO: 105 mg/mL(275.28 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

2% DMSO+30% PEG 300+water 5 mg/mL

AT9283 {[allProObj[0].p_purity_real_show]}

AT9283 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

AT9283 质控信息

AT9283 生物活性

AT9283 细胞研究

AT9283 动物研究

AT9283 临床研究

AT9283 参考文献

AT9283 实验方案

AT9283 技术信息

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靶点

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细胞研究

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JAK3	JAK3, IC50:1.1 nM
Tyk2	TYK2, IC50:1 nM-10 nM
JAK2	JAK2, IC50:1.2 nM
Aurora A	Aurora A, IC50:~3.0 nM
Aurora B	Aurora B, IC50:~3.0 nM
Abl	Abl (Q252H), IC50:10 nM-30 nM Abl1 (T315I), IC50:4 nM

AT9283 {[allProObj[0].p_purity_real_show]}

AT9283 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

AT9283 质控信息

AT9283 生物活性

AT9283 细胞研究

AT9283 动物研究

AT9283 临床研究

AT9283 参考文献

AT9283 实验方案

AT9283 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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AT9283 纯度/质量文件产品仅供科研