NVP-BAW2881-BAW2881-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemENVP-BAW2881Cat. No.: HY-100394CAS No.: 861875-60-7Synonyms: BAW2881分式: CHFNO分量: 424.38作靶点: VEGFR作通路: Protein Tyrosine Kinase/RTK储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 33 mg/mL (77.

2、76 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.3564 mL 11.7819 mL 23.5638 mL5 mM 0.4713 mL 2.3564 mL 4.7128 mL10 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，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 NVP-BAW2881 (BAW2881)是有效，选择性的 VEGFR2

3、 抑制剂，IC50 为值9 nM。IC50 & Target VEGFR1 VEGFR2 VEGFR3820 nM (IC50) 9 nM (IC50) 420 nM (IC50)1/2 Master of Small Molecules 您边的抑制剂师www.MedChemE体外研究 The VEGF-driven cellular receptor autophosphorylation in CHO cells of BAW2881 is inhibited with an IC50 of4 nM. BAW2881 inhibits a limited number of kinases

4、 including c-RAF, B-RAF, RET, ABL, and TIE-2 at sub-M IC50s 1. NVP-BAW2881 is highly selective for VEGFR, although it also demonstrates activity againstTie2 (IC50=650 nM) and RET (IC50=410 nM). The IC50 values of NVP-BAW2881 toward a wide panel ofother kinases are 10 M. NVP-BAW2881 inhibits VEGF-A-i

5、nduced phosphorylation of VEGFR-2 inHUVECs and in VEGFR-2-transfected Chinese hamster ovary cells, with IC50 values of 2.9 and 4.2 nM,respectively 2.体内研究 In a transgenic mouse model of psoriasis, NVP-BAW2881 reduces the number of blood and lymphaticvessels and infiltrating leukocytes in the skin, an

6、d normalized the epidermal architecture. NVP-BAW2881also displays strong anti-inflammatory effects in models of acute inflammation; pretreatment with topicalNVP-BAW2881 significantly inhibits VEGF-A-induced vascular permeability in the skin of pigs and mice 2.PROTOCOLCell Assay 2 HUVECs or LECs (120

7、0) are seeded into fibronectin-coated 96-well plates. After 24 hours, the cells aretransferred 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 combinationof 20 ng/

8、mL VEGF-A and 1 nM to 1 M NVP-BAW2881. Proliferation is also assayed in LECs incubated with500 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 electronm

9、icroscope 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice: A contact hypersensitivity response is induced in the ear skin of 8-week-old female K14/VEGF-A TGAdministration 2 mice. Five days after sensitization (day 0), the right ear is chal

10、lenged by topical application of 10 Loxazolone (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 vehiclesalone. The ear thickness is measured every other day usin

11、g calipers. On day 21, mice are sacrificed and theweight 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.REFERENCES1. Bold G, et al. A Novel Potent Oral Series of VEGFR2 Inh

12、ibitors Abrogate Tumor Growth by Inhibiting Angiogenesis. J Med Chem. 2016Jan 14;59(1):132-46.2. Halin C, et al. Inhibition of chronic and acute skin inflammation by treatment with a vascular endothelial growth factor receptor tyrosinekinase inhibitor. Am J Pathol. 2008 Jul;173(1):265-77.McePdfHeightCaution: P