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

NVP-BAW2881 (Synonyms: BAW2881)

Cat. No.: HY-100394 Purity: 98.42%
Handling Instructions

NVP-BAW2881 (BAW2881) is a potent and selective VEGFR2 inhibitor with an IC50 of 4 nM.

For research use only. We do not sell to patients.

NVP-BAW2881 Chemical Structure

NVP-BAW2881 Chemical Structure

CAS No. : 861875-60-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 112 In-stock
Estimated Time of Arrival: December 31
2 mg USD 84 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 216 In-stock
Estimated Time of Arrival: December 31
25 mg USD 420 In-stock
Estimated Time of Arrival: December 31
50 mg USD 720 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1140 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Based on 1 publication(s) in Google Scholar

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Description

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)

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].

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].

Molecular Weight

424.38

Formula

C₂₂H₁₅F₃N₄O₂

CAS No.

861875-60-7

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 33 mg/mL (77.76 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
References
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.

References
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NVP-BAW2881
Cat. No.:
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