BFH772 |
Catalog No.GC15340 |
BFH772는 3nM의 IC50 값으로 VEGFR2 키나아제를 표적화하는데 매우 효과적인 강력한 경구 VEGFR2 억제제이다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 890128-81-1
Sample solution is provided at 25 µL, 10mM.
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
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