1. Protein Tyrosine Kinase/RTK
  2. VEGFR
  3. NVP-BAW2881

NVP-BAW2881 (Synonyms: BAW2881)

目录号: HY-100394 纯度: 98.17%
产品使用指南

NVP-BAW2881 (BAW2881) 是有效,选择性的 VEGFR2 抑制剂,IC50 为值9 nM。

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NVP-BAW2881 Chemical Structure

NVP-BAW2881 Chemical Structure

CAS No. : 861875-60-7

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥747
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2 mg ¥500
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5 mg ¥800
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10 mg ¥1400
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25 mg ¥2700
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50 mg ¥4400
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100 mg ¥6400
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200 mg   询价  
500 mg   询价  

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Top Publications Citing Use of Products
  • 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-BAW2881 (BAW2881) is a potent and selective VEGFR2 inhibitor with an IC50 of 4 nM.

IC50 & Target

VEGFR1

820 nM (IC50)

VEGFR2

9 nM (IC50)

VEGFR3

420 nM (IC50)

体外研究
(In Vitro)

The VEGF-driven cellular receptor autophosphorylation in CHO cells of BAW2881 is inhibited with an IC50 of 4 nM. BAW2881 inhibits a limited number of kinases including c-RAF, B-RAF, RET, ABL, and TIE-2 at sub-μM IC50s[1]. NVP-BAW2881 is highly selective for VEGFR, although it also demonstrates activity against Tie2 (IC50=650 nM) and RET (IC50=410 nM). The IC50 values of NVP-BAW2881 toward a wide panel of other kinases are >10 μM. NVP-BAW2881 inhibits VEGF-A-induced phosphorylation of VEGFR-2 in HUVECs and in VEGFR-2-transfected Chinese hamster ovary cells, with IC50 values of 2.9 and 4.2 nM, respectively[2].

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

体内研究
(In Vivo)

In a transgenic mouse model of psoriasis, NVP-BAW2881 reduces the number of blood and lymphatic vessels and infiltrating leukocytes in the skin, and normalized the epidermal architecture. NVP-BAW2881 also displays strong anti-inflammatory effects in models of acute inflammation; pretreatment with topical NVP-BAW2881 significantly inhibits VEGF-A-induced vascular permeability in the skin of pigs and mice[2].

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

分子量

424.38

Formula

C22H15F3N4O2

CAS 号
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 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 33 mg/mL (77.76 mM)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3564 mL 11.7819 mL 23.5638 mL
5 mM 0.4713 mL 2.3564 mL 4.7128 mL
10 mM 0.2356 mL 1.1782 mL 2.3564 mL
*

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, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

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

  • 1.

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

    Solubility: ≥ 2.5 mg/mL (5.89 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.89 mM,饱和度未知) 的澄清溶液。

    以 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;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.89 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.89 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 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。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献
Cell Assay
[2]

HUVECs or LECs (1200) are seeded into fibronectin-coated 96-well plates. After 24 hours, the cells are transferred into LEC medium containing 2% fetal bovine serum and incubated for an additional 24 hours. Cells (eight wells/condition) are incubated with medium alone (control), 20 ng/mL VEGF-A, or a combination of 20 ng/mL VEGF-A and 1 nM to 1 μM NVP-BAW2881. Proliferation is also assayed in LECs incubated with 500 ng/mL VEGF-C. The DMSO is adjusted to 0.1% in all wells. After 72 hours, cells are incubated with 5-methylumbelliferylheptanoate for subsequent fluorescent quantification of viable cells, using a electron microscope[2].

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

Animal Administration
[2]

Mice: A contact hypersensitivity response is induced in the ear skin of 8-week-old female K14/VEGF-A TG mice. Five days after sensitization (day 0), the right ear is challenged by topical application of 10 μL oxazolone (1%) on each side. Starting on day 7, once-daily oral doses of 25 mg/kg NVP-BAW2881 or twice-daily topical doses of 0.5% NVP-BAW2881 are administered for 14 days. Control groups are given vehicles alone. The ear thickness is measured every other day using calipers. On day 21, mice are sacrificed and the weight of each ear and of its draining retro-auricular lymph node (LN) is determined[2].

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

参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2

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产品名称:
NVP-BAW2881
目录号:
HY-100394
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