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BFH772

Cat. No. M9249
BFH772 Structure
Size Price Availability Quantity
5mg USD 68  USD68 In stock
10mg USD 115  USD115 In stock
25mg USD 225  USD225 In stock
50mg USD 330  USD330 In stock
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Quality Control & Documentation
Biological Activity

BFH772 is a potent and selective VEGF inhibitor. BFH772 is highly effective at targeting VEGFR2 kinase with an IC50 value of 3 nM. BFH772 inhibits the ligand induced autophosphorylation of RET, PDGFR, and KIT kinases, with IC50 values ranging between 30 and 160 nM.

In vivo, BFH772 (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.

Chemical Information
Molecular Weight 439.39
Formula C23H16F3N3O3
CAS Number 890128-81-1
Solubility (25°C) DMSO: 5 mg/mL (Need warming)
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Bold G, et al. J Med Chem. A Novel Potent Oral Series of VEGFR2 Inhibitors Abrogate Tumor Growth by Inhibiting Angiogenesis.

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Keywords: BFH772 supplier, VEGFR/PDGFR, inhibitors, activators


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