BAW2881 (NVP-BAW2881) (Synonyms: NVP-BAW 2881) |
Catalog No.GC11726 |
BAW2881 (NVP-BAW2881) (BAW2881) is a potent and selective VEGFR2 inhibitor with an IC50 of 4 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 861875-60-7
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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. |
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.
Cas No. | 861875-60-7 | SDF | |
Synonyms | NVP-BAW 2881 | ||
Chemical Name | 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 | ||
Formula | C22H15F3N4O2 | M.Wt | 424.38 |
Solubility | ≥ 42.4mg/mL in DMSO | Storage | Store at -20°C |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Average Rating: 5
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