BFH772

BFH772 is a potent oral VEGFR2 inhibitor, which is highly effective at targeting VEGFR2 kinase with an IC50 value of 3 nM.

Product information

CAS Number: 890128-81-1

Molecular Weight: 439.39

Formula: C23H16F3N3O3

Chemical Name: 6-{[6-(hydroxymethyl)pyrimidin-4-yl]oxy}-N-[3-(trifluoromethyl)phenyl]naphthalene-1-carboxamide

Smiles: OCC1=CC(=NC=N1)OC1=CC2=CC=CC(C(=O)NC3C=C(C=CC=3)C(F)(F)F)=C2C=C1

InChiKey: JNLSTLQFDDAULK-UHFFFAOYSA-N

InChi: InChI=1S/C23H16F3N3O3/c24-23(25,26)15-4-2-5-16(10-15)29-22(31)20-6-1-3-14-9-18(7-8-19(14)20)32-21-11-17(12-30)27-13-28-21/h1-11,13,30H,12H2,(H,29,31)

Technical Data

Appearance: Solid Power

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

Solubility: DMSO : 100 mg/mL (227.59 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

BFH772 is highly selective; apart from inhibiting VEGFR2 at 3 nM IC50, it also targets B-RAF, RET, and TIE-2, albeit with at least 40-fold lower potency. BFH772 is inactive (IC50>10 μM; >2 μM for cKIT) against all other tyrosine specific- and serine/threonine-specific protein kinases tested. BFH772 inhibits VEGFR2 with IC50 of 4.6±0.6 nM in CHO cells. BFH772 inhibits VEGFR2 with IC50 of 3 nM in HUVEC cells. BFH772 inhibits the ligand induced autophosphorylation of RET, PDGFR, and KIT kinases, with IC50 values ranging between 30 and 160 nM. BFH772 is selective (IC50 values >0.5 μM) against the kinases of EGFR, ERBB2, INS-R, and IGF-1R and against the cytoplasmic BCR-ABL kinase. IC50 of BFH772 (<0.01 nM, n=2) demonstrates that they abrogated VEGF induced proliferation at remarkably low nM concentrations.

In Vivo:

BFH772 at 3 mg/kg orally dosed once per day potently inhibits melanoma growth (by 54-90% for primary tumor and 71-96% for metastasis growth) as depicted by treatment to control ratios. Dose–response curves of BFH772 at 0.3, 1, and 3 mg/kg demonstrate that even at the lowest concentrations, this naphthalene-1-carboxamide inhibits VEGF induced tissue weight and TIE-2 levels but only reaches statistical significance at 1 mg/kg and above.

Products are for research use only. Not for human use.