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BFH772

CAS No. : 890128-81-1

MCE 国际站：BFH772

产品活性：BFH772 是一种有效的，具有口服活性的 VEGFR2 抑制剂，IC₅₀ 为 3 nM。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：VEGFR

In Vitro: 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.

In Vivo: BFH772 at 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. Dose–response curves of BFH772 at 0.3, 1, and 3 mg/kg demonstrate that even at the lowest concentrations, this naphthalene-1-carboxamide inhibits VEGF induced tissue weight and TIE-2 levels but only reaches statistical significance at 1 mg/kg and above.

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