BAW2881 (NVP-BAW2881)
(Synonyms: BAW2881) 目录号 : GC11726
A VEGFR inhibitor
Cas No.:861875-60-7
Sample solution is provided at 25 µL, 10mM.
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IC50: 1.0-4.3 nM for VEGFR1-3
BAW2881 (NVP-BAW2881) is a VEGFR inhibitor.
Vascular endothelial growth factor (VEGF) is a potent endothelial cell mitogen regulating blood and lymphatic vessel development and homeostasis. There are three main subtypes of VEGFR, numbered VEGFR 1, 2 and 3.
In vitro: Previous study showed that BAW2881 could inhibit a limited number of kinases including c-RAF, B-RAF, RET, ABL, and TIE-2 at submicromole IC50s. BAW2881 could also inhibit the ligand induced autophosphorylation of RET, PDGFR, and KIT kinases. Moreover, low IC50 value (0.12 ± 0.06 nM) demonstrated that BAW2881 remarkably abrogated VEGF induced proliferation [1].
In vivo: In a psoriasis mouse model, BAW2881 was able to reduce the number of blood and lymphatic vessels and infiltrating leukocytes in the skin, and normalize the epidermal architecture. BAW2881 also showed strong anti-inflammatory effects in acute inflammation models. Moreover, the pretreatment with topical BAW2881 could significantly inhibit VEGF-A-induced vascular permeability in the skin of both pigs and mice. In addition, it was found that the topical application of BAW2881 was able to reduce the inflammatory response in pig skin caused by UV-B irradiation or by contact hypersensitivity reactions [2].
Clinical trial: Up to now, BAW2881 is still in the preclinical development stage.
References:
[1] Bold G et al. A Novel Potent Oral Series of VEGFR2 Inhibitors Abrogate Tumor Growth by Inhibiting Angiogenesis. J Med Chem. 2016 Jan 14;59(1):132-46.
[2] Halin C,Fahrngruber H,Meingassner JG,Bold G,Littlewood-Evans A,Stuetz A,Detmar M. Inhibition of chronic and acute skin inflammation by treatment with a vascular endothelial growth factor receptor tyrosine kinase inhibitor. Am J Pathol.2008 Jul;173(1):265-77.
Cell experiment: | 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]. |
Animal experiment: | 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]. |
References: [1]. Bold G, et al. A Novel Potent Oral Series of VEGFR2 Inhibitors Abrogate Tumor Growth by Inhibiting Angiogenesis. J Med Chem. 2016 Jan 14;59(1):132-46. | |
| Cas No. | 861875-60-7 | SDF | |
| 别名 | BAW2881 | ||
| 化学名 | 6-((2-aminopyrimidin-4-yl)oxy)-N-(3-(trifluoromethyl)phenyl)-1-naphthamide | ||
| Canonical SMILES | O=C(C1=C2C=CC(OC3=NC(N)=NC=C3)=CC2=CC=C1)NC4=CC=CC(C(F)(F)F)=C4 | ||
| 分子式 | C22H15F3N4O2 | 分子量 | 424.38 |
| 溶解度 | ≥ 42.4mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet