BAW2881
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 407228

CAS#: 861875-60-7

Description: BAW2881 is a potent and selective VEGFR inhibitor (vascular endothelial growth factor receptor tyrosine kinase inhibitor) with activity to inhibit chronic and acute skin inflammation. NVP-BAW2881 inhibited proliferation, migration, and tube formation by human umbilical vein endothelial cells and lymphatic endothelial cells in vitro. NVP-BAW2881 reduced the number of blood and lymphatic vessels and infiltrating leukocytes in the skin, and normalized the epidermal architecture. NVP-BAW2881 also displayed strong anti-inflammatory effects in models of acute inflammation; pretreatment with topical NVP-BAW2881 significantly inhibited VEGF-A-induced vascular permeability in the skin of pigs and mice.


Chemical Structure

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BAW2881
CAS# 861875-60-7

Theoretical Analysis

MedKoo Cat#: 407228
Name: BAW2881
CAS#: 861875-60-7
Chemical Formula: C22H15F3N4O2
Exact Mass: 424.1147
Molecular Weight: 424.3832
Elemental Analysis: C, 62.26; H, 3.56; F, 13.43; N, 13.20; O, 7.54

Price and Availability

Size Price Availability Quantity
50.0mg USD 450.0 2 Weeks
100.0mg USD 650.0 2 Weeks
200.0mg USD 1050.0 2 Weeks
500.0mg USD 1850.0 2 Weeks
1.0g USD 2950.0 2 Weeks
2.0g USD 5650.0 2 Weeks
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Synonym: BAW2881; BAW-2881; BAW 2881; NVP-BAW2881; NVP-BAW-2881; NVP-BAW 2881.

IUPAC/Chemical Name: 6-((2-aminopyrimidin-4-yl)oxy)-N-(3-(trifluoromethyl)phenyl)-1-naphthamide

InChi Key: MLLQJNIKDWEEFT-UHFFFAOYSA-N

InChi Code: InChI=1S/C22H15F3N4O2/c23-22(24,25)14-4-2-5-15(12-14)28-20(30)18-6-1-3-13-11-16(7-8-17(13)18)31-19-9-10-27-21(26)29-19/h1-12H,(H,28,30)(H2,26,27,29)

SMILES Code: O=C(C1=C2C=CC(OC3=NC(N)=NC=C3)=CC2=CC=C1)NC4=CC=CC(C(F)(F)F)=C4

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Product Data:

Biological target: BAW2881 is a VEGFR2 inhibitor with an IC50 of 4 nM.
In vitro activity: To determine whether NVP-BAW2881 had a blocking effect on VEGF-A-induced proliferation of endothelial cells, HUVECs were incubated in VEGF-A-containing medium in the presence or absence of NVP-BAW2881. Although VEGF-A promoted HUVEC cell proliferation (1.3-fold more cells, compared with control; P < 0.0001), the lowest concentration of NVP-BAW2881 tested (1 nmol/L) potently inhibited this response (Figure 1A). Similarly, when testing the effects of this compound on LEC proliferation, 1 nmol/L NVP-BAW2881 significantly reduced VEGF-A-induced proliferation, compared with controls (P < 0.001; Figure 1B). Since VEGF-C is thought to be main mediator of lymphangiogenesis in vivo, whether NVP-BAW2881 could also block VEGF-C-induced proliferation of LECs was evaluated. Although 1 μmol/L NVP-BAW2881 significantly reduced VEGF-C-induced LEC proliferation (P = 0.042, Figure 1C), lower concentrations of the compound did not have a significant effect. Furthermore, 10 nmol/L and 1 μmol/L concentrations of NVP-BAW2881 completely inhibited the migration of HUVECs and of LECs toward VEGF-A in in vitro transmigration assays (Figure 1, D and E). Reference: Am J Pathol. 2008 Jul;173(1):265-77. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2438303/
In vivo activity: The in vivo effects of NVP-BAW2881 were evaluated in a transgenic mouse model of psoriasis. Psoriasis-like lesions were induced in the right ears of K14/VEGF-A mice by inducing a CHS response, and NVP-BAW2881 was administered, topically or orally, beginning 7 days later. A significant reduction in ear swelling was observed within 5 days in groups given oral doses (−21%, P = 0.003) and within 7 days in groups given topical applications (−25%, P = 0.006) of NVP-BAW2881 (Figure 3, A and B, respectively). At the defined study endpoint (14 days after treatment began; study day 21), ear swelling had decreased by 56% (P < 0.0001) in the oral treatment group, as compared with the control group. Similarly, topical treatment with NVP-BAW2881 reduced ear swelling by 43% (P = 0.0001) as compared with controls. Reference: Am J Pathol. 2008 Jul;173(1):265-77. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2438303/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
Ethanol 20.0 47.13
DMF 30.0 70.69
DMSO 50.0 117.82
DMSO:PBS (pH 7.2) (1:2) 0.33 0.78

Preparing Stock Solutions

The following data is based on the product molecular weight 424.3832 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. 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. doi: 10.2353/ajpath.2008.071074. Epub 2008 Jun 5. PMID: 18535184; PMCID: PMC2438303.
In vitro protocol: 1. 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. doi: 10.2353/ajpath.2008.071074. Epub 2008 Jun 5. PMID: 18535184; PMCID: PMC2438303.
In vivo protocol: 1. 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. doi: 10.2353/ajpath.2008.071074. Epub 2008 Jun 5. PMID: 18535184; PMCID: PMC2438303.

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1: 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. doi: 10.2353/ajpath.2008.071074. Epub 2008 Jun 5.
PubMed PMID: 18535184; PubMed Central PMCID: PMC2438303.

BAW2881

50.0mg / USD 450.0