BFH772

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

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.

相关产品：Drug Repurposing Compound Library Plus  |  Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Kinase Inhibitor Library  |  Protein Tyrosine Kinase Compound Library  |  Anti-Cancer Compound Library  |  Clinical Compound Library  |  Drug Repurposing Compound Library  |  Differentiation Inducing Compound Library  |  Reprogramming Compound Library  |  Anti-COVID-19 Compound Library  |  Anti-Breast Cancer Compound Library  |  Anti-Lung Cancer Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  Angiogenesis-Related Compound Library  |  Anti-Liver Cancer Compound Library   |  Anti-Colorectal Cancer Compound Library   |  Anti-Pulmonary Fibrosis Compound Library  |  Heterocyclic Compound Library  |  Membrane Protein-targeted Compound Library  |  Membrane Receptor-targeted Compound Library  |  Highly Selective Inhibitors Library  |  Cytokine Inhibitors Library  |  Sorafenib  |  Lenvatinib  |  Sunitinib  |  Regorafenib  |  Nintedanib  |  Bevacizumab  |  Semaxinib  |  Cabozantinib  |  Ponatinib  |  Axitinib  |  Midostaurin  |  Chloramphenicol  |  Pazopanib  |  PD173074  |  5Z-7-Oxozeaenol  |  Linifanib  |  Tanshinone IIA  |  Vandetanib  |  Foretinib  |  SU 5402  |  Fruquintinib  |  SPHINX31  |  Ripretinib  |  E3330  |  Dovitinib  |  GW806742X  |  Sitravatinib

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  荧光染料  |  PROTAC  |  同位素标记物

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Dye Reagents  |  PROTAC  |  Isotope-Labeled Compounds