MGCD-265 analog | MGCD-265 | c-Met/VEGFR2 Inhibitor | AmBeed-信号通路专用抑制剂

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MGCD-265 analog {[allProObj[0].p_purity_real_show]}

货号：A209718 同义名： MGCD-265

MGCD-265, an ATP-competitive inhibitor, can inhibit c-Met and VEGFR1, 2, 3 with IC50s of 1 nM and 3 nM, 3 nM, 4 nM, respectively. It also exhibits inhibition of Ron and Tie2.

MGCD-265 analog 化学结构
CAS号：875337-44-3

MGCD-265 analog 3D分子结构
CAS号：875337-44-3

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MGCD-265 analog 纯度/质量文件产品仅供科研

货号：A209718 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 >

VEGFR 亚型比较
Tie-2 亚型比较

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	PDGFR,RET	98%
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	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	c-Kit,BTK	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		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/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	98%
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	Tie-2 ↓ ↑	其他靶点	纯度
Tie2 kinase inhibitor 1	++ Tie-2, IC50: 0.25 μM		99%+
MGCD-265 analog	+++ Tie-2, IC50: 7 nM		99%+
Pexmetinib	✔	p38 MAPK	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。

MGCD-265 analog 生物活性

靶点	VEGFR1 VEGFR1, IC50:3 nM VEGFR3 VEGFR3, IC50:4 nM VEGFR2 VEGFR2, IC50:3 nM Tie-2 Tie-2, IC50:7 nM
描述	MGCD-265 is a potent, multi-target and ATP-competitive inhibitor of c-Met and VEGFR1/2/3 with IC50 of 1 nM, 3 nM/3 nM/4 nM, respectively and also inhibits Ron and Tie2.

MGCD-265 analog 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
293T cells		Function assay		Inhibition of TPR-fused Met phosphorylation expressed in human 293T cells by ELISA, IC50=0.05 μM	19211249
Sf9 cells		Function assay		Inhibition of GST tagged VEGFR2 expressed in Sf9 cells, IC50=0.01 μM	18434145

MGCD-265 analog 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
NCT02954991	Carcinoma, Non-Small-Cell Lung	Phase 2	Recruiting	April 2019	-
NCT00679133	Advanced Malignancies	Phase 1	Completed	-	United States, Michigan ... 展开 >> Karmanos Cancer Institute Detroit, Michigan, United States, 48201 United States, Texas University of Texas M.D. Anderson Cancer Center Houston, Texas, United States, 77030 收起 <<
NCT00975767	Advanced Malignancies, Non-sma... 展开 >>ll Cell Lung Cancer 收起 <<	Phase 1	Terminated(The study was termi... 展开 >>nated due to a need for a reformulation of the study drug. Phase 1 completed, no patients enrolled in Phase 2.) 收起 <<	-	United States, Michigan ... 展开 >> Barbara Ann Karmanos Cancer Center Detroit, Michigan, United States, 48201 United States, North Carolina Duke University Medical Center Durham, North Carolina, United States, 27710 United States, Pennsylvania University of Pennsylvania Abramson Cancer Center Philadelphia, Pennsylvania, United States, 19104 United States, Texas The University of Texas MD Anderson Cancer Center Houston, Texas, United States, 77030 South Texas Accelerated Research Therapeutics, LLC San Antonio, Texas, United States, 78229 收起 <<

MGCD-265 analog 参考文献

[1]Claridge S, Raeppel F, et al. Discovery of a novel and potent series of thieno[3,2-b] pyridine-based inhibitors of c-Met and VEGFR2 tyrosine kinases. Bioorg Med Chem Lett. 2008 May 1;18(9):2793-8.

MGCD-265 analog 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.93mL

0.39mL

0.19mL

9.66mL

1.93mL

0.97mL

19.32mL

3.86mL

1.93mL

MGCD-265 analog 技术信息

CAS号	875337-44-3
分子式	C₂₆H₂₀FN₅O₂S₂
分子量	517.598

别名	MGCD-265
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Store in freezer, under -20°C

溶解度

DMSO: 105 mg/mL(202.86 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

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

NCT02954991	Carcinoma, Non-Small-Cell Lung	Phase 2	Recruiting	April 2019	-
NCT00679133	Advanced Malignancies	Phase 1	Completed	-	United States, Michigan ... 展开 >> Karmanos Cancer Institute Detroit, Michigan, United States, 48201 United States, Texas University of Texas M.D. Anderson Cancer Center Houston, Texas, United States, 77030 收起 <<
NCT00975767	Advanced Malignancies, Non-sma... 展开 >>ll Cell Lung Cancer 收起 <<	Phase 1	Terminated(The study was termi... 展开 >>nated due to a need for a reformulation of the study drug. Phase 1 completed, no patients enrolled in Phase 2.) 收起 <<	-	United States, Michigan ... 展开 >> Barbara Ann Karmanos Cancer Center Detroit, Michigan, United States, 48201 United States, North Carolina Duke University Medical Center Durham, North Carolina, United States, 27710 United States, Pennsylvania University of Pennsylvania Abramson Cancer Center Philadelphia, Pennsylvania, United States, 19104 United States, Texas The University of Texas MD Anderson Cancer Center Houston, Texas, United States, 77030 South Texas Accelerated Research Therapeutics, LLC San Antonio, Texas, United States, 78229 收起 <<
NCT02117245	-		Completed	-	Canada, Quebec ... 展开 >> Algorithme Laval, Quebec, Canada 收起 <<
NCT02544633	Non-Small Cell Lung Cancer	Phase 2	Active, not recruiting	December 2018	-
NCT00697632	Advanced Cancer	Phase 1	Active, not recruiting	December 2018	United States, California ... 展开 >> City of Hope Duarte, California, United States, 91010 UC Irvine Medical Center Orange, California, United States, 92868 UC San Diego San Diego, California, United States, 92093 United States, Illinois University of Chicago Chicago, Illinois, United States, 60637 United States, Massachusetts Dana-Farber Cancer Institute Boston, Massachusetts, United States, 02115 United States, Missouri Washington University, Alvin J. Siteman Cancer Center Saint Louis, Missouri, United States, 63110 United States, New York Columbia University, Herbert Irving Comprehensive Cancer Center New York, New York, United States, 10032 United States, North Carolina Duke University Medical Center Durham, North Carolina, United States, 27710 United States, Pennsylvania Fox Chase Cancer Center Philadelphia, Pennsylvania, United States, 19111 United States, Texas University of Texas, MD Anderson Cancer Center Houston, Texas, United States, 77030 United States, Utah Huntsman Cancer Institute Salt Lake City, Utah, United States, 84112 United States, Washington Seattle Cancer Care Alliance Seattle, Washington, United States, 98109 Canada, Alberta Cross Cancer Institute Edmonton, Alberta, Canada, T6G 1Z2 Canada, British Columbia British Columbia Cancer Agency, Vancouver Center Vancouver, British Columbia, Canada, V5Z 4E6 Canada, Quebec Jewish General Hospital Montreal, Quebec, Canada, H3T IE2 Korea, Republic of National Cancer Center Gyeonggi-do, Korea, Republic of, 410-769 Seoul National University Hosptial Seoul, Korea, Republic of, 110-744 Samsung Medical Center Seoul, Korea, Republic of, 135-710 Yonsei University Health System, Severance Hospital Seoul, Korea, Republic of 收起 <<
NCT01930006	Advanced Malignancies	Phase 1	Completed	-	United States, Kansas ... 展开 >> Vince & Associates Clinical Research, Inc. Overland Park, Kansas, United States, 66212 收起 <<

MGCD-265 analog {[allProObj[0].p_purity_real_show]}

MGCD-265 analog 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

MGCD-265 analog 质控信息

MGCD-265 analog 生物活性

MGCD-265 analog 细胞研究

MGCD-265 analog 临床研究

MGCD-265 analog 参考文献

MGCD-265 analog 实验方案

MGCD-265 analog 技术信息

最近浏览的产品

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VEGFR1	VEGFR1, IC50:3 nM
VEGFR3	VEGFR3, IC50:4 nM
VEGFR2	VEGFR2, IC50:3 nM
Tie-2	Tie-2, IC50:7 nM

MGCD-265 analog {[allProObj[0].p_purity_real_show]}

MGCD-265 analog 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

MGCD-265 analog 质控信息

MGCD-265 analog 生物活性

MGCD-265 analog 细胞研究

MGCD-265 analog 临床研究

MGCD-265 analog 参考文献

MGCD-265 analog 实验方案

MGCD-265 analog 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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MGCD-265 analog 纯度/质量文件产品仅供科研