BFH772
IC50: 3 nM
BFH772 is a VEGFR2 inhibitor.
The VEGF family including VEGF-A, VEGF-B, VEGF-C, VEGF-D, and PlGF signals through VEGFR1, VEGFR2, and VEGFR3 cell surface tyrosine kinase receptors that are located on the host vascular endothelium, lymphatic, and hematopoietic systems.
In vitro: BFH772 was highly effective at targeting VEGFR2 kinase, however, lost 500-fold potency on FLK-1, FLT-1, and FLT-4. BFH772 also targeted B-RAF, RET, and TIE-2, albeit with at least 40-fold lower potency. BFH772 inhibited the ligand induced autophosphorylation of RET, PDGFR, and KIT kinases. BFH772 was selective against the kinases of EGFR, ERBB2, INS-R, and IGF-1R and against the cytoplasmic BCR-ABL kinase [1].
In vivo: The dose response curves of BFH772 at 0.3, 1, and 3 mg/kg showed that even at the lowest concentrations, this naphthalene-1-carboxamide inhibited VEGF induced tissue weight and TIE-2 levels but only reached statistical significance at 1 mg/kg and above. Moreover, BFH772 at 3 mg/kg orally dosed once per day could potently inhibit melanoma growth (54-90% for primary tumor and 71-96% for metastasis tumor) when compared with control ratios [1].
Clinical trial: A proof of concept study to evaluate the safety, tolerability, and efficacy of 12 week administration of BFH772 ointment in rosacea patients has completed, but no result data are released [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.
[2] http://adisinsight. springer.com/trials/700244037
| Storage | Store at -20°C |
| M.Wt | 439.39 |
| Cas No. | 890128-81-1 |
| Formula | C23H16F3N3O3 |
| Solubility | ≥53.4 mg/mL in DMSO; ≥15.33 mg/mL in EtOH; insoluble in H2O |
| Chemical Name | 6-((6-(hydroxymethyl)pyrimidin-4-yl)oxy)-N-(3-(trifluoromethyl)phenyl)-1-naphthamide |
| SDF | Download SDF |
| Canonical SMILES | O=C(C1=C2C=CC(OC3=NC=NC(CO)=C3)=CC2=CC=C1)NC4=CC=CC(C(F)(F)F)=C4 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Quality Control & MSDS
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Chemical structure
