1. Protein Tyrosine Kinase/RTK
  2. VEGFR PDGFR
  3. NVP-ACC789

NVP-ACC789  (Synonyms: ACC-789; ZK202650)

目录号: HY-19624 纯度: 99.94%
COA 产品使用指南

NVP-ACC789 是 人 VEGFR-1VEGFR-2 (鼠 VEGFR-2),VEGFR-3PDGFR-β 的抑制剂,IC50 值分别为 0.38,0.02 (0.23),0.18 和 1.4 μM。

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NVP-ACC789 Chemical Structure

NVP-ACC789 Chemical Structure

CAS No. : 300842-64-2

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥550
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1 mg ¥200
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5 mg ¥500
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10 mg ¥800
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25 mg ¥1100
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50 mg ¥1900
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  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

NVP-ACC789 is an inhibitor of human VEGFR-1, VEGFR-2 (mouse VEGFR-2), VEGFR-3 and PDGFR-β with IC50s of 0.38, 0.02 (0.23), 0.18, 1.4 μM, respectively.

IC50 & Target[1]

VEGFR-2

0.02 μM (IC50)

VEGFR-1

0.38 μM (IC50)

mVEGFR-2

0.23 μM (IC50)

VEGFR-3

0.18 μM (IC50)

PDGFR-β

1.4 μM (IC50)

体外研究
(In Vitro)

The enzymatic kinase assays demonstrate that NVP-ACC789 is an inhibitor of human VEGFR-1, VEGFR-2 (mouse VEGFR-2), VEGFR-3 and PDGFR-β with IC50s of 0.38, 0.02 (0.23), 0.18, 1.4 μM, respectively. In VEGF-treated cultures, addition of the VEGFR-2 inhibitor NVP-ACC789 reduces BME cell number to baseline levels from 1 μM. Likewise, bFGF-induced BME cell proliferation is reduced markedly by NVP-ACC789 from 1 to 10 μM, without however reaching basal levels. NVP-ACC789 is found to be a potent inhibitor of VEGF-induced HUVE cell proliferation with an IC50 of 1.6 nM. NVP-ACC789 also completely inhibits VEGF-induced BME and BAE cell invasion and VEGF-C-induced BAE cell invasion. The inhibition is dose-dependent in both cell types with a maximal effect from 1 μM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

NVP-ACC789 which is given in daily oral doses for 6 days blocks VEGF-induced angiogenesis in a dose-dependent manner. NVP-ACC789 also inhibits the response to bFGF to some extent, but the dose-response curve is not linear for NVP-ACC789[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

405.29

Formula

C21H17BrN4

CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 25 mg/mL (61.68 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4674 mL 12.3368 mL 24.6737 mL
5 mM 0.4935 mL 2.4674 mL 4.9347 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

In Vivo:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 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,建议您现用现配,当天使用
以下溶剂前显示的百分比是指该溶剂在您配制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

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.17 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.17 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料
参考文献
Kinase Assay
[1]

Human VEGFR-2-transfected CHO cells are seeded into 6-well plates and grown to about 80% confluency. NVP-ACC789 is added in serial dilutions and the cells incubated for 2 h at 37°C in medium without fetal calf serum (FCS). VEGF (20 ng/mL) is then added. After a 5-min incubation at 37°C, the cells are washed twice with ice-cold phosphate-buffered saline and lysed. Nuclei are removed by centrifugation for 10 min at 4°C. Protein concentrations of the lysates are determined[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

HUVE cell proliferation is determined. Cells are seeded into 1.5% gelatin-coated 96-well plates (5×103 cells per well) and incubated in endothelial cell growth medium containing 5% fetal calf serum (FCS) for 24 h. The medium is replaced with essential basic medium (1.5% FCS), and the cells are incubated for another 24 h. Essential basic medium is then replaced with fresh medium containing either 50 ng/mL VEGF or 0.5 ng/mL bFGF. NVP-ACC789 is added just before addition of growth factors. The cells are incubated for a further 24 h before adding the BrdU labeling solution. Twenty four hours later, the labeling solution is removed, the cells are fixed, and the incorporated BrdU is visualized with a peroxidase-labeled anti-BrdU antibody and TMB substrate[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Porous Teflon chambers (volume, 0.5 mL) filled with 0.8% w/v agar-containing heparin (20 U/mL) with or without VEGF (2 μg/mL) or bFGF (0.3 μg/mL) are implanted subcutaneously on the dorsal flank of female mice. The mice are treated with NVP-ACC789 (p.o. once daily) or vehicle (5% dimethyl sulfoxide, 1% Tween 80 in water) starting 1 day before implantation of the chamber and continuing for 5 days thereafter. At the end of the treatment period, the mice are killed, and the chambers are removed. The vascularized tissue growing around the chamber is removed carefully and weighed, and the blood content is assessed by measuring hemoglobin levels. The percentage inhibition of the angiogenic response (increase in tissue weight or total blood) is calculated. EC50 values are estimated from the dose response curves (% inhibition versus dose). Each experiment is performed with six animals per dose group and each dose is tested in at least two independent experiments[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

NVP-ACC789 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4674 mL 12.3368 mL 24.6737 mL 61.6842 mL
5 mM 0.4935 mL 2.4674 mL 4.9347 mL 12.3368 mL
10 mM 0.2467 mL 1.2337 mL 2.4674 mL 6.1684 mL
15 mM 0.1645 mL 0.8225 mL 1.6449 mL 4.1123 mL
20 mM 0.1234 mL 0.6168 mL 1.2337 mL 3.0842 mL
25 mM 0.0987 mL 0.4935 mL 0.9869 mL 2.4674 mL
30 mM 0.0822 mL 0.4112 mL 0.8225 mL 2.0561 mL
40 mM 0.0617 mL 0.3084 mL 0.6168 mL 1.5421 mL
50 mM 0.0493 mL 0.2467 mL 0.4935 mL 1.2337 mL
60 mM 0.0411 mL 0.2056 mL 0.4112 mL 1.0281 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
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