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BFH772
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BFH772图片
CAS NO:890128-81-1
规格:≥98%
包装与价格:
包装价格(元)
1mg电议
2mg电议
5mg电议
10mg电议
25mg电议
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产品介绍
理化性质和储存条件
Molecular Weight (MW)439.39
FormulaC23H16F3N3O3
CAS No.890128-81-1
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 87 mg/mL (198.0 mM)
Water: <1 mg/mL
Ethanol: 87 mg/mL (198.0 mM)
SMILES O=C(C1=C2C=CC(OC3=NC=NC(CO)=C3)=CC2=CC=C1)NC4=CC=CC(C(F)(F)F)=C4
SynonymsBFH 772; BFH-772; BFH772
实验参考方法
In Vitro

In vitro activity: BFH772 was highly effective at targeting VEGFR2 kinase with an IC50 value of 3 nM, however, lost 500-fold potency on FLK-1, FLT-1, and FLT-4. BFH772 was highly selective, In addition to VEGFR2, it also targeted B-RAF, RET, and TIE-2, albeit with at least 40-fold lower potency. BFH772 inhibits the ligand induced autophosphorylation of RET, PDGFR, and KIT kinases, with IC50 values ranging between 30 and 160 nM.


Kinase Assay: 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.


Cell Assay: Subconfluent HUVECs were incubated in triplicate in 96-well plates with basal medium containing 1.5% FCS and a constant concentration of VEGF (10 ng/mL), bFGF (0.5 ng/mL), or FCS (5%) in the presence or absence of compounds. After 24 h of incubation, BrdUrd labeling solution was added and cells incubated an additional 24 h before fixation, blocking, and addition of peroxidaselabeled anti-BrdUrd antibody. Bound antibody was then detected spectrophotometrically at 450 nm.

In VivoThe 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.
Animal modelSprague–Dawley rats
Formulation & DosageDissolved in N-methyl pyrrolidone/polyethylene glycol200(30:70, v/v); 1 mg/kg; i.v. injection
References

J Med Chem. 2016 Jan 14;59(1):132-46.