An inhibitor of VEGFR2 (IC50 = 0.0027 μM for the human receptor); selective for human VEGFR2 over mouse VEGFR2 and human VEGFR1 and VEGFR3 (IC50s = 1.5

BFH772 – 1 mg

Brand:
Cayman
CAS:
890128-81-1
Storage:
-20
UN-No:
De Minimis - 3077 / 9

BFH772 is an inhibitor of VEGF receptor 2 (VEGFR2; IC50 = 0.0027 μM for the human receptor).{42999} 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.  

 

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Description

An inhibitor of VEGFR2 (IC50 = 0.0027 μM for the human receptor); 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; inhibits VEGF-induced proliferation of HUVECs (IC50 = <0.01 nM); inhibits VEGF-induced increases in tissue weight and Tie2 levels in an angiogenesis chamber implant model in mice at 1 and 3 mg/kg per day; inhibits primary tumor and metastasis growth in a B16 melanoma mouse model at 3 mg/kg per day

Formal name: 6-[[6-(hydroxymethyl)-4-pyrimidinyl]oxy]-N-[3-(trifluoromethyl)phenyl]-1-naphthalenecarboxamide

Synonyms: 

Molecular weight: 439.4

CAS: 890128-81-1

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|VEGFR Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Angiogenesis||Research Area|Cancer|Cell Migration & Metastasis||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling

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