BFH772
- Product Name
- BFH772
- CAS No.
- 890128-81-1
- Chemical Name
- BFH772
- Synonyms
- BFH772;CS-2412;Bfh-722;BFH-772; BFH 772;6-((6-(Hydroxymethyl)pyrimidin-4-yl)oxy)-N-(3-(trifluoromethyl)phenyl)-1-naphthamide;inhibit,BFH 772,VEGFR,BFH-772,BFH772,Vascular endothelial growth factor receptor,Inhibitor;1-Naphthalenecarboxamide, 6-[[6-(hydroxymethyl)-4-pyrimidinyl]oxy]-N-[3-(trifluoromethyl)phenyl]-
- CBNumber
- CB03147777
- Molecular Formula
- C23H16F3N3O3
- Formula Weight
- 439.39
- MOL File
- 890128-81-1.mol
BFH772 Property
- Boiling point:
- 541.2±50.0 °C(Predicted)
- Density
- 1.432±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- Soluble in DMSO
- form
- A crystalline solid
- pka
- 12.65±0.70(Predicted)
- color
- White to off-white
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- 21386
- Product name
- BFH-772
- Packaging
- 1mg
- Price
- $38
- Updated
- 2024/03/01
- Product number
- 21386
- Product name
- BFH-772
- Packaging
- 5mg
- Price
- $166
- Updated
- 2024/03/01
- Product number
- 21386
- Product name
- BFH-772
- Packaging
- 10mg
- Price
- $292
- Updated
- 2024/03/01
- Product number
- 21386
- Product name
- BFH-772
- Packaging
- 25mg
- Price
- $593
- Updated
- 2024/03/01
- Product number
- B6199
- Product name
- BFH772
- Packaging
- 50mg
- Price
- $709
- Updated
- 2021/12/16
BFH772 Chemical Properties,Usage,Production
Description
BFH772 is an inhibitor of VEGF receptor 2 (VEGFR2; IC50 = 0.0027 μM for the human receptor). It is selective for human VEGFR2 over mouse VEGFR2 and human VEGFR1 and VEGFR3 (IC50s = 1.5, 1.7, and 1.1 μM, respectively), as well as 40-fold selective over B-RAF, RET, and Tie2. BFH772 inhibits VEGF-induced proliferation of human umbilical vein endothelial cells (HUVECs; IC50 = <0.01 nM). It inhibits VEGF-induced increases in tissue weight and Tie2 levels in an angiogenesis chamber implant model in mice when administered at doses of 1 and 3 mg/kg per day. BFH772 (3 mg/kg per day) inhibits primary tumor and metastasis growth in a B16 melanoma mouse model.
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].
IC 50
3 nm
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
BFH772 Preparation Products And Raw materials
Raw materials
Preparation Products
BFH772 Suppliers
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View Lastest Price from BFH772 manufacturers
- Product
- BFH772 890128-81-1
- Price
- US $1.00/g
- Min. Order
- 1g
- Purity
- 99.99%
- Supply Ability
- 200kg
- Release date
- 2019-12-20