CYC-116 | Aurora Kinase | VEGFR | AmBeed-信号通路专用抑制剂

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CYC-116 99%+

货号：A199103 产品仅供科研

CYC116 is a potent inhibitor of Aurora with Ki of 8.0 nM/9.2 nM for Aurora A/B.

CYC-116 化学结构
CAS号：693228-63-6

CYC-116 3D分子结构
CAS号：693228-63-6

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CYC-116 纯度/质量文件

货号：A199103 标准纯度：99%+ 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: • Mar. Drugs, 2024, 22(5): 194. Ambeed. [ A104599 ]; • Pharmaceuticals, 2024, 17(5): 570. Ambeed. [ A224421 ]; 更多 >

Aurora Kinase 亚型比较
VEGFR 亚型比较

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	Bcr-Abl,FLT3	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		RET,FLT3	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			99%+
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	VEGFR1 ↓ ↑	VEGFR2 ↓ ↑	VEGFR3 ↓ ↑	其他靶点	纯度
Motesanib Diphosphate	++++ VEGFR1, IC50: 2 nM	++++ VEGFR2, IC50: 3 nM VEGFR2/Flk1, IC50: 3 nM	+++ VEGFR3, IC50: 6 nM	PDGFR,RET	99%+
Tivozanib	++ VEGFR1, IC50: 30 nM	+++ VEGFR2, IC50: 6.5 nM	++ VEGFR3, IC50: 15 nM		99%+
Brivanib	+ VEGFR1, IC50: 380 nM	++ Flk1, IC50: 25 nM VEGFR2, IC50: 25 nM			99%+
Regorafenib	+++ VEGFR1, IC50: 13 nM	+++ VEGFR2, IC50: 4.2 nM	+ VEGFR3, IC50: 46 nM	RET	98%
Pazopanib	+++ VEGFR1, IC50: 10 nM	++ VEGFR2, IC50: 30 nM	+ VEGFR3, IC50: 47 nM	PDGFR,c-Kit,FGFR	99%
Sitravatinib	+++ VEGFR1 (FLT1), IC50: 6 nM	+++ VEGFR2 (KDR), IC50: 5 nM	++++ VEGFR3 (FLT4), IC50: 2 nM		99%+
Foretinib	+++ VEGFR1/FLT1, IC50: 6.8 nM	++++ KDR, IC50: 0.86 nM	++++ VEGFR3/FLT4, IC50: 2.8 nM	Tie-2	99%+
MGCD-265 analog	++++ VEGFR1, IC50: 3 nM	++++ VEGFR2, IC50: 3 nM	++++ VEGFR3, IC50: 4 nM	Tie-2	99%+
Lactate	+++ VEGFR1/FLT1, IC50: 10 nM	+++ VEGFR2/Flk1, IC50: 13 nM	+++ VEGFR3/FLT4, IC50: 8 nM	c-Kit,FLT3	85%
AEE788	+ FLT1, IC50: 59 nM	+ KDR, IC50: 77 nM		EGFR	98+%
Linifanib	++++ VEGFR1/FLT1, IC50: 3 nM	++++ VEGFR2/KDR, IC50: 4 nM	+ VEGFR3/FLT4, IC50: 190 nM	FLT3	99%+
Vatalanib 2HCl	+ VEGFR1/FLT1, IC50: 77 nM	++ VEGFR2/KDR, IC50: 37 nM VEGFR2/Flk1, IC50: 270 nM	+ VEGFR3/FLT4, IC50: 660 nM	c-Kit,c-Fms	99%+
Axitinib	++++ VEGFR1/FLT1, IC50: 0.1 nM	++++ VEGFR2/KDR, IC50: 0.2 nM VEGFR2/Flk1, IC50: 0.18 nM			98%
Dovitinib	+++ VEGFR1/FLT1, IC50: 10 nM	+++ VEGFR2/Flk1, IC50: 13 nM	+++ VEGFR3/FLT4, IC50: 8 nM	c-Kit,FLT3	99%+
ZM 306416	+ VEGFR1, IC50: 0.33 μM			Src	99%+
KRN-633	+ VEGFR1, IC50: 170 nM	+ VEGFR2, IC50: 160 nM	+ VEGFR3, IC50: 125 nM	BTK,c-Kit	99%+
OSI-930	+++ FLT1, IC50: 8 nM	+++ KDR, IC50: 9 nM			99%+
Lenvatinib	++ VEGFR1/FLT1, IC50: 22 nM	++++ VEGFR2/KDR, IC50: 4.0 nM	+++ VEGFR3/FLT4, IC50: 5.2 nM		98%
NVP-BAW2881	+ hVEGFR1, IC50: 820 nM	+++ mVEGF2, IC50: 165 nM hVEGFR2, IC50: 9 nM	+ hVEGFR3, IC50: 420 nM		98%
Cediranib	+++ VEGFR1/FLT1, IC50: 5 nM	++++ VEGFR2/KDR, IC50: 0.5 nM		c-Kit	99%+
Nintedanib	++ VEGFR1, IC50: 34 nM	+++ VEGFR2, IC50: 13 nM	+++ VEGFR3, IC50: 13 nM	FLT3	99+%
BMS-794833		++ VEGFR2, IC50: 15 nM			99%+
SKLB1002		++ VEGFR2, IC50: 32 nM			98%
Cabozantinib S-malate		++++ VEGFR2/KDR, IC50: 0.035 nM			99+%
Ki8751		++++ VEGFR2, IC50: 0.9 nM		c-Kit	98+%
SU 5402		++ VEGFR2, IC50: 20 nM			98%
Rivoceranib Mesylate		++++ VEGFR2, IC50: 1 nM		RET	98+%
Ponatinib		++++ VEGFR2, IC50: 1.5 nM			98%
LY2874455		+++ VEGFR2, IC50: 7 nM			99%+
ZM323881 HCl		++++ VEGFR2, IC50: <2 nM			98%
AZD2932		+++ VEGFR-2, IC50: 8 nM		c-Kit	98%
Cabozantinib		++++ VEGFR2/KDR, IC50: 0.035 nM			98%
Sorafenib		++ VEGFR2, IC50: 90 nM VEGFR2/Flk1, IC50: 90 nM			99%
CYC-116		++ VEGFR2, Ki: 44 nM		FLT3	99%+
Golvatinib		++ VEGFR2, IC50: 16 nM			99%+
Sunitinib		+ VEGFR2 , IC50: 80 nM		FLT3	98%
RAF265		++ VEGFR2, EC50: 30 nM			99%+
PD173074					99%+
BFH772		++++ VEGFR2, IC50: 3 nM			99%+
Semaxinib		+ VEGFR2/Flk1, IC50: 1.23 μM			98%
Vandetanib		++ VEGFR2, IC50: 40 nM	+ VEGFR3, IC50: 110 nM	EGFR	98%
SAR131675			++ VEGFR3, IC50: 23 nM		99%+
ENMD-2076		+ VEGFR2/KDR, IC50: 58.2 nM	++ VEGFR3/FLT4, IC50: 15.9 nM	RET,FLT3	98%
Telatinib		+++ VEGFR2, IC50: 6 nM	++++ VEGFR3, IC50: 4 nM	c-Kit	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。

CYC-116 生物活性

靶点	Aurora A Aurora A, Ki:8 nM Aurora A Aurora A, Ki:8 nM VEGFR2 VEGFR2, Ki:44 nM VEGFR2 VEGFR2, Ki:44 nM
描述	The aurora kinases, consisting of aurora A, B, and C, are a family of serine-threonine kinases that regulate centrosome maturation, bipolar spindle assembly, chromosome segregation, and cytokinesis. CYC-116 is a potent inhibitor for both aurora A and B with K_i values of 8.0 and 9.2nM, respectively. CYC-116 also inhibited CDK2/cyclin E, CDK4/cyclin D, CDK9/cyclin T, Flt-3, p70 S6, Src, Lck and VEGFR2 with K_i values of 0.39, 1.09, 0.48, 0.044, 0.54, 0.82, 2.80, and 0.044μM, respectively. iIn an MTT assay, CYC-116 inhibited A2780 and MiaPaCa-2 cell growth with IC50 values of 170 and 278nM, respectively. CYC-116 also exhibited anti-proliferative activity against MCF-7, Hela, Colo205, K562, NCI-H460, Saos-2, and Messa cell lines with IC50 values of 0.599, 0.590, 0.241, 1.375, 0.681, 0.110, and 0.090μM, respectively. In a murine P388/D1 leukemia model, oral administration of CYC-116 at 45 and 67mg/kg twice daily resulted in a significant increase in lifespan of 172% and 183%, respectively, as compared to the vehicle control group. In mice bearing subcutaneous NCI-H460 xenografts, oral dosing of CYC-116 at 75 and 100mg/kg/day caused tumor growth delays of 2.3 and 5.8 days, respectively.^[3]
作用机制	CYC-116 is an inhibitor for aurora A and B that possesses anticancer activity.^[3]

CYC-116 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
A2780 cells		Cytotoxicity assay	96 h	Cytotoxicity against human A2780 cells after 96 hrs by MTT assay	20462263
A549 cells	0.5-2 μM	Function assay	7 h	Cell cycle arrest in asynchronous human A549 cells assessed as accumulation of cyclin B1-negative tetraploid cells at G1 phase at 0.5 to 2 uM after 7 hrs by FACS analysis	20462263
A549 cells		Function assay	7 h	Inhibition of Aurora kinase in human A549 cells assessed as concentration required for half-maximal inhibition of histone H3 serine-10 phosphorylation after 7 hrs immunofluorescence microscopy	20462263
BxPC3 cells		Cytotoxicity assay	96 h	Cytotoxicity against human BxPC3 cells after 96 hrs by MTT assay	20462263

CYC-116 参考文献

[1]Kamei H, Jackson RC, et al. An integrated pharmacokinetic-pharmacodynamic model for an Aurora kinase inhibitor. J Pharmacokinet Pharmacodyn. 2010 Aug;37(4):407-34.

[2]Wang S, Midgley CA, et al. Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors. J Med Chem. 2010 Jun 10;53(11):4367-78.

[3]Wang S, Midgley CA, Scaërou F, et al. Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors. J Med Chem. 2010;53(11):4367-4378. doi:10.1021/jm901913s

CYC-116 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.71mL

0.54mL

0.27mL

13.57mL

2.71mL

1.36mL

27.14mL

5.43mL

2.71mL

CYC-116 技术信息

CAS号	693228-63-6
分子式	C₁₈H₂₀N₆OS
分子量	368.456

别名
运输	蓝冰

存储条件

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 14 mg/mL(38 mM)，配合低频超声助溶，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

IP 2% DMSO+water 0.1 mg/mL clear

PO 0.5% CMC-Na 71 mg/mL suspension

CYC-116 99%+

CYC-116 纯度/质量文件

全球学术期刊中引用的产品

CYC-116 生物活性

CYC-116 细胞研究

CYC-116 参考文献

CYC-116 实验方案

CYC-116 技术信息

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Aurora A	Aurora A, Ki:8 nM
Aurora A	Aurora A, Ki:8 nM
VEGFR2	VEGFR2, Ki:44 nM
VEGFR2	VEGFR2, Ki:44 nM
Aurora B	Aurora B, Ki:9 nM
Aurora B	Aurora B, Ki:9 nM

CYC-116 99%+

CYC-116 纯度/质量文件

全球学术期刊中引用的产品

CYC-116 生物活性

CYC-116 细胞研究

CYC-116 参考文献

CYC-116 实验方案

CYC-116 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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