[CAS NO. 890128-81-1] BFH772
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PRODUCTS SPECIFICATIONS [890128-81-1]
Store
Catalog
SLK-S8188
Brand
Selleck
CAS
890128-81-1
DESCRIPTION [890128-81-1]
Overview
| MDL | MFCD30534392 |
|---|---|
| Molecular Weight | 439.39 |
| Molecular Formula | C23H16F3N3O3 |
| SMILES | O=C(NC1=CC=CC(C(F)(F)F)=C1)C2=C3C=CC(OC4=NC=NC(CO)=C4)=CC3=CC=C2 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Description
BFH772 is a novel potent oral inhibitor, targeting VEGFR2 kinase with IC50 of 3 nM.
Targets
| VEGFR2 [1] (Cell-free assay) |
| 3 nM |
In vitro
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.
In vivo
BFH772 all at 3 mg/kg orally dosed once per day potently inhibited melanoma growth (by 54−90% for primary tumor and 71−96% for metastasis growth).
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