CAS 940310-85-0; nvp-bhg712

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货号

品牌

产品名称

规格

包装、参考价格

N796327

MACKLIN

NVP-BHG712

10mM in DMSO

795元/1ml;

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储存：-20°C

N864524

MACKLIN

NVP-BHG712

≥98%

495元/5mg;

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储存：-20°C

N1099

TCI

NVP-BHG 712

>95.0%(HPLC)

990元/10MG; 3450元/50MG;

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基本信息

纯度/分析方法	>95.0%(HPLC)
分子式/分子量	C₂₆H₂₀F₃N₇O = 503.49
外观与形状(20℃)	固体
储存温度	-20℃
应避免的情况	加热
PubChem物质ID	354335680
MDL编号	MFCD20272929

技术规格

Appearance	White to Light yellow to Light orange powder to crystal
Purity(HPLC)	min. 95.0 area%
Elemental analysis(Nitrogen)	18.5 to 20.5 %

1239106

J&K

NVP-BHG712

99%, 是受体酪氨酸激酶ephb4(ed50=25nm)的一种非常有效的选择性吸入剂

1189元/5MG; 2240元/10MG;

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基本信息

分子式	C₂₆H₂₀F₃N₇O
分子量	503.49
存储条件	Freezer -20℃

产品描述

NVP-BHG712是一种特异性的EphB4抑制剂，ED50为25 nM，区别于对VEGFR和EphB4的抑制，对c-Raf， c-Src和c-Abl也具有抑制活性，IC50分别为0.395 μM， 1.266 μM和1.667 μM。

靶点（IC50 & Targe）

c-Abl,1.667μM

C-Raf,0.395μM

c-Src,1.266μM

EphB4,25nM(ED50)

Tie-2,>10μM

体外研究

NVP-BHG712作用于稳定转染的A375黑色素瘤细胞，也抑制RTK自磷酸化，这种作用存在剂量依赖性，作用于EphB4和VEGFR2时, EC50分别为25 nM和 4.2 μM。 [1]

体内研究

NVP-BHG712 按3 mg/kg剂量口服给药生长因子诱导血管生成的模型，通过抑制EphB4前进信号，显著抑制VEGF刺激的组织和血管形成。而且, NVP-BHG712按10 mg/kg/kg剂量口服处理，有效逆转VEGF增强的组织形成和血管生长。NVP-BHG712 按3 mg/kg剂量口服处理小鼠，浓度约为10 μM，长期处理血浆及肺和肝脏组织，处理高达8小时，导致EphB4激酶活性长期受抑制。[1]

动物实验

Animal Models: 植入生长因子诱导VEGF调节血管生长的小鼠模型

Formulation: NVP-BHG712溶于1-甲基-2-吡咯烷酮(NMP)，然后使用PEG-300稀释，终浓度为10% v/v NMP和 90% v/v PEG300

Dosages: ≤30 mg/kg

Administration: 口服处理

(Only for Reference)

参考文献

[1] Martiny-Baron G, et al. Angiogenesis. 2010, 13(3), 259-267.

安全信息

图形或危害标志
危险说明	H302 H410
防范说明	P264 P270 P273 P301+P312 P330 P391 P501
UN号码	3077
危险分类	9
包装等级	III
TSCA	是

SML0333

Sigma-Aldrich

NVP-BHG712

≥98% (HPLC)

1480.38元/5 MG; 5967.79元/25 MG;

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产品说明

应用

NVP-BHG712 has been used as an epinephrine type-B receptor 4 (Eph-B4) inhibitor:

to study its effects on human colorectal cancer cell growth in vitro and the growth of tumor cells in mice.
to study the regulation of endothelial nitric oxide synthase.
to study its effects on vascularization and growth of endometriotic lesions.

NVP-BHG712 has been used as an ephrin type-B receptor 4 (Eph-B4) inhibitor to study its effect on Eph-B4 phosphorylation in ephrin-B2/Fc stimulated mouse lung endothelial cells.

包装

5, 25 mg in glass bottle

生化/生理作用

NVP-BHG712 is a very potent, selective inhbitor of the receptor tyrosine kinase EphB4 (ED₅₀ = 25 nM). NVP-BHG712 blocks Ephrin receptor autophosphorylation and VEGF-induced angiogenesis.
NVP-BHG712 obstructs angiogenesis mediated by vascular endothelial growth factor in vivo. It also blocks the efflux of ATP-binding cassette (ABC) transporter subfamily C member 10 (ABCC10) into the HEK293 cells by overexpressing the ABCC10 transporter.
NVP-BHG712 (4-methyl-3-(1-methyl-6-(pyridin-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-ylamino)-N-(3-(trifluoromethyl)phenyl)benzamide) inhibits the activity of ABC transporter subfamily C member 10 (ABCC10), which is responsible for mediating paclitaxel resistance. Therefore, NVP-BHG712 in combination with paclitaxel is effective against cancers that are resistant to paclitaxel due to the expression of the ABCC10.

特点和优势

This compound is a featured product for Kinase Phosphatase Biology research. Click here to discover more featured Kinase Phosphatase Biology products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
This compound is featured on the Eph page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

基本信息

经验(实验)分子式	C₂₆H₂₀F₃N₇O
分子量	503.48
MDL编号	MFCD20272929
PubChem化学物质编号	329825338
NACRES	NA.77

产品性质

质量水平	100
测定	≥98% (HPLC)
形式	powder
颜色	white to beige
溶解性	DMSO: 2 mg/mL, clear
储存温度	−20℃
SMILES string	Cc1ccc(cc1Nc2nc(nc3n(C)ncc23)-c4cccnc4)C(=O)Nc5cccc(c5)C(F)(F)F
InChI	1S/C26H20F3N7O/c1-15-8-9-16(25(37)32-19-7-3-6-18(12-19)26(27,28)29)11-21(15)33-23-20-14-31-36(2)24(20)35-22(34-23)17-5-4-10-30-13-17/h3-14H,1-2H3,(H,32,37)(H,33,34,35)
InChI key	ZCCPLJOKGAACRT-UHFFFAOYSA-N

安全信息

象形图
警示用语：	Danger
危险声明	H301
预防措施声明	P301 + P310
危险分类	Acute Tox. 3 Oral
储存分类代码	6.1D - Non-combustible, acute toxic Cat.3 / toxic hazardous materials or hazardous materials causing chronic effects
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable