ENMD-2076 | Aurora Kinase Inhibitor | AmBeed-信号通路专用抑制剂

ENMD-2076 {[allProObj[0].p_purity_real_show]}

货号：A283012

ENMD-2076是一种 Aurora A 和 Flt3 激酶抑制剂，IC50 分别为 14 nM 和 1.86 nM，对 Aurora A 的选择性高于 Aurora B，同时对 VEGFR2、FGFR1 等靶点作用较弱，可诱导肿瘤细胞凋亡和 G2/M 阶段停滞。

ENMD-2076 化学结构
CAS号：934353-76-1

ENMD-2076 3D分子结构
CAS号：934353-76-1

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Aurora Kinase 亚型比较

FLT3 亚型比较

VEGFR 亚型比较

Src 亚型比较

PDGFR 亚型比较

FGFR 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	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	FLT3 ↓ ↑	其他靶点	纯度
R406	✔	Syk	98%
Go6976	✔		99%+
Quizartinib	+++ FLT3 (ITD), IC50: 1.1 nM FLT3 (WT), IC50: 4.2 nM		98%
Gilteritinib	++++ FLT3, IC50: 0.29 nM		99%+
Amuvatinib	+ FLT3 (D835Y), IC50: 81 nM		99%+
Pacritinib	++ FLT3, IC50: 22 nM FLT3 (D835Y), IC50: 6 nM		97%
Dovitinib	++++ FLT3, IC50: 1 nM	c-Kit	99%+
Denfivontinib	++++ FLT3 (D835Y), IC50: 0.4 nM FLT3, IC50: 0.4 nM	RET	99%+
TAK-659 HCl	++ FLT3, IC50: 4.6 nM	Syk	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/Flk1, IC50: 3 nM VEGFR2, IC50: 3 nM	+++ VEGFR3, IC50: 6 nM	RET,PDGFR	97%
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	c-Kit,FGFR,PDGFR	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	FLT3,c-Kit	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-Fms/CSF1R,c-Kit	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	FLT3,c-Kit	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	98%
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	+++ hVEGFR2, IC50: 9 nM mVEGF2, IC50: 165 nM	+ hVEGFR3, IC50: 420 nM		99%
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			99%
Cabozantinib S-malate		++++ VEGFR2/KDR, IC50: 0.035 nM			99+%
Ki8751		++++ VEGFR2, IC50: 0.9 nM		c-Kit	99%
SU 5402		++ VEGFR2, IC50: 20 nM			98%
Apatinib 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	99%
Cabozantinib		++++ VEGFR2/KDR, IC50: 0.035 nM			98%
Sorafenib		++ VEGFR2/Flk1, IC50: 90 nM VEGFR2, 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			98%
Semaxinib		+ VEGFR2/Flk1, IC50: 1.23 μM			98%
Vandetanib		++ VEGFR2, IC50: 40 nM	+ VEGFR3, IC50: 110 nM	EGFR	99%
SAR131675			++ VEGFR3, IC50: 23 nM		99%+
ENMD-2076		+ VEGFR2/KDR, IC50: 58.2 nM	++ VEGFR3/FLT4, IC50: 15.9 nM	FLT3,RET	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。

产品名称	Fyn ↓ ↑	Lck ↓ ↑	Lyn ↓ ↑	Src ↓ ↑	Yes ↓ ↑	其他靶点	纯度
Saracatinib	++ Fyn, IC50: 10 nM	++++ LCK, IC50: <4 nM	+++ Lyn, IC50: 5 nM	++++ c-Src, IC50: 2.7 nM			99%+
SU6656	+ Fyn, IC50: 170 nM		+ Lyn, IC50: 130 nM	+ Src, IC50: 280 nM	++ YES, IC50: 20 nM		98%
PP1	+++ Fyn, IC50: 6 nM	+++ LCK, IC50: 5 nM				EGFR	99%+
PP2	+++ Fyn, IC50: 5 nM	++++ LCK, IC50: 4 nM					98%
WH-4-023		++++ Lck, IC50: 2 nM		+++ Src, IC50: 6 nM			99%+
NVP-BHG 712				+ c-Src, IC50: 1.266 μM			99%+
CCT196969		++ LCK, IC50: 0.02 μM		+ Src, IC50: 0.03 μM			98%
MNS				+ Src, IC50: 29.3 μM		p97,Syk	98%
Tirbanibulin				++ Src (Hep 3B), GI50: 26 nM Src (HuH7), GI50: 13 nM			99%+
PP121				++ Src, IC50: 14 nM		VEGFR,PDGFR	99%+
Bosutinib				++++ Src, IC50: 1.2 nM			99%
Dasatinib monohydrate				++++ Src, IC50: 0.8 nM			98%
Quercetin				✔		Sirtuin,PKC	95%
Dasatinib				++++ Src, IC50: 0.8 nM			98%
Repotrectinib				+++ Src, IC50: 5.3 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	PDGFR ↓ ↑	PDGFRα ↓ ↑	PDGFRβ ↓ ↑	其他靶点	纯度
Tyrphostin A9	+ PDGFR, IC50: 0.5 μM			EGFR	98%
Tyrphostin AG1296					99%+
Motesanib Diphosphate	++ PDGFR, IC50: 84 nM				97%
Pazopanib	++ PDGFR, IC50: 84 nM				99%
Imatinib	+ PDGFR, IC50: 100 nM			c-Kit	98%
Imatinib Mesylate	+ PDGFR, IC50: 100 nM			c-Kit	99%
Sennoside B	✔				99%+
PP121	++++ PDGFR, IC50: 2 nM			mTOR,VEGFR	99%+
Crenolanib		++++ PDGFRα, Kd: 2.1 nM	++++ PDGFRβ, Kd: 3.2 nM		99%+
Masitinib		+ PDGFRα, IC50: 540 nM	+ PDGFRβ, IC50: 800 nM		99%+
Ki8751		++ PDGFRα, IC50: 67 nM		c-Kit	99%
Tivozanib		++ PDGFRα, IC50: 40 nM	++ PDGFRβ, IC50: 49 nM		99%+
Ponatinib		++++ PDGFRα, IC50: 1.1 nM			98%
Amuvatinib		++ PDGFRα (V561D), IC50: 40 nM			99%+
Axitinib		+++ PDGFRα, IC50: 5.0 nM	++++ PDGFRβ, IC50: 1.6 nM		98%
CP-673451		+++ PDGFRα, IC50: 10 nM	++++ PDGFRβ, IC50: 1 nM		99%+
Telatinib		+++ PDGFRα, IC50: 15 nM		c-Kit	99%+
Nintedanib		++ PDGFRα, IC50: 59 nM	++ PDGFRβ, IC50: 65 nM		99+%
Avapritinib		++++ PDGFRα (D842V), IC50: 0.5 nM			99%+
MK-2461			+++ PDGFRβ, IC50: 22 nM		98%+
Lactate			+++ PDGFRβ, IC50: 27 nM	FLT3,c-Kit	85%
Linifanib			++ PDGFRβ, IC50: 66 nM		99%+
AZD2932			+++ PDGFRβ, IC50: 4 nM	c-Kit	99%
Dovitinib			+++ PDGFRβ, IC50: 27 nM	FLT3,c-Kit	99%+
Sorafenib			++ mPDGFRβ, IC50: 57 nM PDGFRβ, IC50: 57 nM		99%
Sunitinib			++++ PDGFRβ , IC50: 2 nM	FLT3	98%
Orantinib			+++ PDGFRβ, Ki: 8 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	FGFR ↓ ↑	FGFR1 ↓ ↑	FGFR2 ↓ ↑	FGFR3 ↓ ↑	FGFR4 ↓ ↑	其他靶点	纯度
Tyrphostin AG1296	+ FGFR (Swiss 3T3), IC50: 12.3 μM					PDGFR	99%+
Pazopanib	+ FGFR, IC50: 140 nM						99%
Erdafitinib	✔					RET	99%+
Gambogenic acid	✔						98+%
Sulfatinib		+++ FGFR1, IC50: 15 nM					99+%
Nintedanib esylate		+ FGFR1, IC50: 69 nM	++ FGFR2, IC50: 37 nM	+ FGFR3, IC50: 108 nM			98%
Zoligratinib		+++ FGFR1, IC50: 9.3 nM	+++ FGFR2, IC50: 7.6 nM	++ FGFR3, IC50: 22 nM	+ FGFR4, IC50: 290 nM		99%+
MK-2461		+ FGFR1, IC50: 65 nM	++ FGFR2, IC50: 39 nM	++ FGFR3, IC50: 50 nM			98%+
SU 5402		++ FGFR1, IC50: 30 nM					98%
Brivanib		+ FGFR1, IC50: 148 nM					99%+
Lucitanib		++ FGFR1, IC50: 17.5 nM	+ FGFR2, IC50: 82.5 nM				99%+
Ponatinib		++++ FGFR1, IC50: 2.2 nM					98%
PD-166866		+ FGFR1, IC50: 52.4 nM					99%
Narazaciclib		++ FGFR1, IC50: 26 nM				RET	99%+
Lactate		+++ FGFR1, IC50: 8 nM		+++ FGFR3, IC50: 9 nM		FLT3,c-Kit	85%
Lenvatinib mesylate		++ FGFR1, IC50: 46 nM				c-RET	99%
LY2874455		++++ FGFR1, IC50: 2.8 nM	++++ FGFR2, IC50: 2.6 nM	+++ FGFR3, IC50: 6.4 nM	+++ FGFR4, IC50: 6 nM		99%+
FIIN-2		+++ FGFR1, IC50: 3.09 nM	+++ FGFR2, IC50: 4.3 nM	++ FGFR3, IC50: 27 nM	++ FGFR4, IC50: 45.3 nM		99%
FIIN-3		+++ FGFR1, IC50: 13.1 nM	++ FGFR2, IC50: 21 nM	++ FGFR3, IC50: 31.4 nM	++ FGFR4, IC50: 35.3 nM		98%
Infigratinib		++++ FGFR1, IC50: 0.9 nM	++++ FGFR2, IC50: 1.4 nM	++++ FGFR3, IC50: 1.0 nM FGFR3 (K650E), IC50: 4.9 nM	+ FGFR4, IC50: 60 nM		99%+
Danusertib		++ FGFR1, IC50: 47 nM				RET	99%+
R1530		++ FGFR1, IC50: 28 nM					98%
ENMD-2076		+ FGFR1, IC50: 92.7 nM	+ FGFR2, IC50: 70.8 nM			FLT3,RET	98%
Dovitinib		+++ FGFR1, IC50: 8 nM		+++ FGFR3, IC50: 9 nM		FLT3,c-Kit	99%+
Sorafenib		+ FGFR1, IC50: 580 nM					99%
SSR128129E		+ FGFR1, IC50: 1.9 μM					99%+
AZD-4547		++++ FGFR1, IC50: 0.2 nM	++++ FGFR2, IC50: 2.5 nM	++++ FGFR3, IC50: 1.8 nM			98%
Lenvatinib		++ FGFR1, IC50: 46 nM				RET	98%
PD173074		++ FGFR1, IC50: ~25 nM					99%+
S49076		++ FGFR1, IC50: 18 nM	+++ FGFR2, IC50: 17 nM	+++ FGFR3, IC50: 15 nM			98%
Futibatinib		++++ FGFR1, IC50: 1.8 nM	++++ FGFR2, IC50: 1.4 nM	++++ FGFR3, IC50: 1.6 nM	+++ FGFR4, IC50: 3.7 nM		99%+
Ferulic Acid		+ FGFR1, IC50: 3.78 μM	+ FGFR2, IC50: 12.5 μM				98%
Nintedanib		+ FGFR1, IC50: 69 nM	++ FGFR2, IC50: 37 nM	+ FGFR3, IC50: 108 nM	+ FGFR4, IC50: 610 nM		99+%
ASP5878		++++ FGFR1, IC50: 0.47 nM	++++ FGFR2, IC50: 0.6 nM	++++ FGFR3, IC50: 0.74 nM	+++ FGFR4, IC50: 3.5 nM		99%
PRN1371		++++ FGFR1, IC50: 0.6 nM	++++ FGFR2, IC50: 1.3 nM	+++ FGFR3, IC50: 4.1 nM	++ FGFR4, IC50: 19.3 nM		99%
Derazantinib		+++ FGFR1, IC50: 4.5 nM	++++ FGFR2, IC50: 1.8 nM	+++ FGFR3, IC50: 4.5 nM	++ FGFR4, IC50: 34 nM	RET	99%+
ODM-203		+++ FGFR1, IC50: 11 nM	+++ FGFR2, IC50: 16 nM	+++ FGFR3, IC50: 6 nM	++ FGFR4, IC50: 35 nM		99%+
Pemigatinib		++++ FGFR1, IC50: 0.4 nM	++++ FGFR2, IC50: 0.5 nM	++++ FGFR3, IC50: 1.2 nM	++ FGFR4, IC50: 30 nM		99%+
SKLB 610			✔			PDGFR	99%+
Alofanib			✔				99%+
Lirafugratinib			✔				99%
Masitinib mesylate				✔		FAK	99%+
BLU9931				+ FGFR3, IC50: 150 nM	+++ FGFR4, IC50: 3 nM		99%+
BO-264				✔			99%+
Fisogatinib					+++ FGFR4, IC50: 5 nM		99%+
H3B-6527					++++ FGFR4, IC50: <1.2 nM		99%+
Roblitinib					++++ FGFR4, IC50: 1.9 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。

ENMD-2076 生物活性

靶点

Aurora A

Aurora A, IC50:14 nM
Aurora B

Aurora B, IC50:350 nM
VEGFR3

VEGFR3/FLT4, IC50:15.9 nM
VEGFR2

VEGFR2/KDR, IC50:58.2 nM

描述

ENMD-2076 has selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold selective for Aurora A than over Aurora B and less potent to VEGFR2/KDR and VEGFR3, FGFR1 and FGFR2 and PDGFRα.

ENMD-2076 细胞实验

Cell Line HL-7702 MDA-MB-468 C6 U251 U87 T98G LN18 HCC1143 VI-MC1 CM-MC1 CoMS	Concentration	Treated Time	Description	References
HL-7702	0.5, 1, 5μM	24, 48, 72 h	ENMD-2076 possessed limited toxicity to normal cells	Aging (Albany NY). 2019 Nov 9;11(21):9738-9766.
MDA-MB-468	0 – 5 μM	96 h	To evaluate the effect of ENMD-2076 on DNA synthesis	Clin Cancer Res. 2013 Jan 1;19(1):291-303.
C6	0, 0.5, 1, 2, 4, 8μM	24, 48, 72 h	ENMD-2076 inhibited the proliferation of glioblastoma cells in a dose dependent manner and time dependent manner	Aging (Albany NY). 2019 Nov 9;11(21):9738-9766.
U251	0, 0.5, 1, 2, 4, 8μM	24, 48, 72 h	ENMD-2076 inhibited the proliferation of glioblastoma cells in a dose dependent manner and time dependent manner	Aging (Albany NY). 2019 Nov 9;11(21):9738-9766.
U87	0, 0.5, 1, 2, 4, 8μM	24, 48, 72 h	ENMD-2076 inhibited the proliferation of glioblastoma cells in a dose dependent manner and time dependent manner	Aging (Albany NY). 2019 Nov 9;11(21):9738-9766.
T98G	0, 0.5, 1, 2, 4, 8μM	24, 48, 72 h	ENMD-2076 inhibited the proliferation of glioblastoma cells in a dose dependent manner and time dependent manner	Aging (Albany NY). 2019 Nov 9;11(21):9738-9766.
LN18	0, 0.5, 1, 2, 4, 8μM	24, 48, 72 h	ENMD-2076 inhibited the proliferation of glioblastoma cells in a dose dependent manner and time dependent manner	Aging (Albany NY). 2019 Nov 9;11(21):9738-9766.
HCC1143	0 – 20 μM	24 -96 h	To evaluate the antiproliferative activity of ENMD-2076 against breast cancer cell lines	Clin Cancer Res. 2013 Jan 1;19(1):291-303.
VI-MC1	291 nM (IC10), 539 nM (IC50)	48 h	Evaluate the cytotoxic effect of ENMD-2076 on canine mast cell tumor cells, showing dose-dependent cytotoxicity and selective killing of G2/M phase cells	Vet Comp Oncol. 2016 Mar;14(1):13-27.
CM-MC1	17.5 nM (IC10), 404 nM (IC50)	48 h	Evaluate the cytotoxic effect of ENMD-2076 on canine mast cell tumor cells, showing dose-dependent cytotoxicity	Vet Comp Oncol. 2016 Mar;14(1):13-27.
CoMS	117 nM (IC10), 360 nM (IC50)	48 h	Evaluate the cytotoxic effect of ENMD-2076 on canine mast cell tumor cells, showing dose-dependent cytotoxicity and selective killing of G2/M phase cells	Vet Comp Oncol. 2016 Mar;14(1):13-27.

Cell Line

Concentration

Treated Time

Description

References

HL-7702

0.5, 1, 5μM

24, 48, 72 h

ENMD-2076 possessed limited toxicity to normal cells

Aging (Albany NY). 2019 Nov 9;11(21):9738-9766.

MDA-MB-468

0 – 5 μM

96 h

To evaluate the effect of ENMD-2076 on DNA synthesis

Clin Cancer Res. 2013 Jan 1;19(1):291-303.

0, 0.5, 1, 2, 4, 8μM

24, 48, 72 h

ENMD-2076 inhibited the proliferation of glioblastoma cells in a dose dependent manner and time dependent manner

Aging (Albany NY). 2019 Nov 9;11(21):9738-9766.

U251

0, 0.5, 1, 2, 4, 8μM

24, 48, 72 h

ENMD-2076 inhibited the proliferation of glioblastoma cells in a dose dependent manner and time dependent manner

Aging (Albany NY). 2019 Nov 9;11(21):9738-9766.

U87

0, 0.5, 1, 2, 4, 8μM

24, 48, 72 h

ENMD-2076 inhibited the proliferation of glioblastoma cells in a dose dependent manner and time dependent manner

Aging (Albany NY). 2019 Nov 9;11(21):9738-9766.

T98G

0, 0.5, 1, 2, 4, 8μM

24, 48, 72 h

ENMD-2076 inhibited the proliferation of glioblastoma cells in a dose dependent manner and time dependent manner

Aging (Albany NY). 2019 Nov 9;11(21):9738-9766.

LN18

0, 0.5, 1, 2, 4, 8μM

24, 48, 72 h

ENMD-2076 inhibited the proliferation of glioblastoma cells in a dose dependent manner and time dependent manner

Aging (Albany NY). 2019 Nov 9;11(21):9738-9766.

HCC1143

0 – 20 μM

24 -96 h

To evaluate the antiproliferative activity of ENMD-2076 against breast cancer cell lines

Clin Cancer Res. 2013 Jan 1;19(1):291-303.

VI-MC1

291 nM (IC10), 539 nM (IC50)

48 h

Evaluate the cytotoxic effect of ENMD-2076 on canine mast cell tumor cells, showing dose-dependent cytotoxicity and selective killing of G2/M phase cells

Vet Comp Oncol. 2016 Mar;14(1):13-27.

CM-MC1

17.5 nM (IC10), 404 nM (IC50)

48 h

Evaluate the cytotoxic effect of ENMD-2076 on canine mast cell tumor cells, showing dose-dependent cytotoxicity

Vet Comp Oncol. 2016 Mar;14(1):13-27.

CoMS

117 nM (IC10), 360 nM (IC50)

48 h

Evaluate the cytotoxic effect of ENMD-2076 on canine mast cell tumor cells, showing dose-dependent cytotoxicity and selective killing of G2/M phase cells

Vet Comp Oncol. 2016 Mar;14(1):13-27.

ENMD-2076 动物实验

Species Wistar rats Nude mice Nude mice	Animal Model Intracranial tumor model MDA-MB-468 and MDA-MB-231 triple-negative breast cancer xenografts HT-29 CRC cell line xenograft model	Administration	Dosage	Frequency	Description	References
Wistar rats	Intracranial tumor model	Oral	50 mg/kg, 200 mg/kg	28 days	ENMD-2076 significantly prolonged the survival time of tumor-bearing rats as well as inhibiting tumor growth (p<0.01)	Aging (Albany NY). 2019 Nov 9;11(21):9738-9766.
Nude mice	MDA-MB-468 and MDA-MB-231 triple-negative breast cancer xenografts	Oral gavage	100 mg/kg	Once daily for 16 days (MDA-MB-231) or 40 days (MDA-MB-468)	To evaluate the antitumor activity of ENMD-2076 in triple-negative breast cancer xenograft models	Clin Cancer Res. 2013 Jan 1;19(1):291-303.
Nude mice	HT-29 CRC cell line xenograft model	Oral	100 or 200 mg/kg	Daily for 28 days	To evaluate the antitumor effects of ENMD-2076 on HT-29 CRC xenograft models. Results showed that ENMD-2076 at doses of 100 and 200 mg/kg significantly inhibited tumor growth and reduced tumor vascularity and metabolic activity.	Clin Cancer Res. 2010 Jun 1;16(11):2989-2998

Species

Wistar rats Nude mice Nude mice

Animal Model

Intracranial tumor model MDA-MB-468 and MDA-MB-231 triple-negative breast cancer xenografts HT-29 CRC cell line xenograft model

Administration

Dosage

Frequency

Description

References

Wistar rats

Intracranial tumor model

Oral

50 mg/kg, 200 mg/kg

28 days

ENMD-2076 significantly prolonged the survival time of tumor-bearing rats as well as inhibiting tumor growth (p<0.01)

Aging (Albany NY). 2019 Nov 9;11(21):9738-9766.

Nude mice

MDA-MB-468 and MDA-MB-231 triple-negative breast cancer xenografts

Oral gavage

100 mg/kg

Once daily for 16 days (MDA-MB-231) or 40 days (MDA-MB-468)

To evaluate the antitumor activity of ENMD-2076 in triple-negative breast cancer xenograft models

Clin Cancer Res. 2013 Jan 1;19(1):291-303.

Nude mice

HT-29 CRC cell line xenograft model

Oral

100 or 200 mg/kg

Daily for 28 days

To evaluate the antitumor effects of ENMD-2076 on HT-29 CRC xenograft models. Results showed that ENMD-2076 at doses of 100 and 200 mg/kg significantly inhibited tumor growth and reduced tumor vascularity and metabolic activity.

Clin Cancer Res. 2010 Jun 1;16(11):2989-2998

ENMD-2076 参考文献

ENMD-2076 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.66mL

0.53mL

0.27mL

13.32mL

2.66mL

1.33mL

26.63mL

5.33mL

2.66mL

ENMD-2076 技术信息

CAS号	934353-76-1
分子式	C₂₁H₂₅N₇
分子量	375.47
SMILES Code	CC1=CC(NC2=NC(/C=C/C3=CC=CC=C3)=NC(N4CCN(CC4)C)=C2)=NN1
MDL No.	MFCD16619371

别名
运输	蓝冰

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C

溶解方案

细胞实验：

DMSO: 30 mg/mL(79.9 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：请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用；以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

方案二

方案三

靶点

靶点	数值

Aurora A	Aurora A, IC50:14 nM
Aurora B	Aurora B, IC50:350 nM
VEGFR3	VEGFR3/FLT4, IC50:15.9 nM
VEGFR2	VEGFR2/KDR, IC50:58.2 nM
FGFR2	FGFR2, IC50:70.8 nM
FGFR1	FGFR1, IC50:92.7 nM

ENMD-2076 {[allProObj[0].p_purity_real_show]}

ENMD-2076 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

ENMD-2076 质控信息

ENMD-2076 生物活性

ENMD-2076 细胞实验

ENMD-2076 动物实验

ENMD-2076 参考文献

ENMD-2076 实验方案

ENMD-2076 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

热门区域

A

B

C

F

G

H

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N

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靶点	Aurora A Aurora A, IC50:14 nM Aurora B Aurora B, IC50:350 nM VEGFR3 VEGFR3/FLT4, IC50:15.9 nM VEGFR2 VEGFR2/KDR, IC50:58.2 nM
描述	ENMD-2076 has selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold selective for Aurora A than over Aurora B and less potent to VEGFR2/KDR and VEGFR3, FGFR1 and FGFR2 and PDGFRα.

ENMD-2076 {[allProObj[0].p_purity_real_show]}

ENMD-2076 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

ENMD-2076 质控信息

ENMD-2076 生物活性

ENMD-2076 细胞实验

ENMD-2076 动物实验

ENMD-2076 参考文献

ENMD-2076 实验方案

ENMD-2076 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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热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

ENMD-2076 纯度/质量文件产品仅供科研