BFH772 NEW
| Price | $38 | $60 | $105 |
| Package | 2mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: BFH772 | CAS No.: 890128-81-1 |
| Purity: 99.36% | Supply Ability: 10g |
| Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | BFH772 |
| Description | BFH772, a structure analogue of BAW2881, 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. |
| Cell Research | Subconfluent HUVECs were incubated in triplicate in 96-well plates with basal medium containing 1.5% FCS and a constant concentration of VEGF (10 ng/mL), bFGF (0.5 ng/mL), or FCS (5%) in the presence or absence of compounds. After 24 h of incubation, BrdUrd labeling solution was added and cells incubated an additional 24 h before fixation, blocking, and addition of peroxidaselabeled anti-BrdUrd antibody. Bound antibody was then detected spectrophotometrically at 450 nm.(Only for Reference) |
| Kinase Assay | In vitro kinase assay is based on a filter binding assay, using the recombinant GST-fused kinase domains expressed in baculovirus and purified over glutathione-sepharose, γ-[33P]ATP as the phosphate donor, and poly(Glu:Tyr 4:1) peptide as the acceptor. Each GST-fused kinase is incubated under optimized buffer conditions [20 mM Tris-HCl buffer (pH 7.5), 1-3 mM MnCl2, 3-10 mM MgCl2, 3-8 μg/mL poly(Glu:Tyr 4:1), 0.25 mg/mL polyethylene glycol 20000, 8 μM ATP, 10 μM sodium vanadate, 1 mM DTT] and 0.2 μCi γ-33P ATP in a total volume of 30 μL in the presence or absence of a test substance for 10 min at ambient temperature. The reaction is stopped by adding 10 mL of 250 mM EDTA. Using a 384-well filter system, half the volume is transferred onto an Immobilon-polyvinylidene difluoride membrane. The membrane is then washed extensively and dried, and scintillation counting is performed. IC50s for compounds are calculated by linear regression analysis of the percentage inhibition[1]. |
| In vitro | Daily oral administration of 3 mg/kg BFH772 effectively inhibits melanoma growth, with primary tumors reducing by 54-90% and metastatic tumors diminishing by 71-96%. |
| In vivo | BFH772 inhibits ligand-induced autophosphorylation of RET, PDGFR, and KIT kinases with an IC50 (half maximal inhibitory concentration) value of 30-160 nM. It effectively targets VEGFR2 with an IC50 of 3 nM, demonstrating efficacy 500 times lower against FLK-1, FLT-1, and FLT-4 compared to VEGFR2. Beyond VEGFR2, BFH772 also targets B-RAF, RET, and TIE-2, albeit with over 40 times lower efficacy compared to its action on VEGFR2. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | Ethanol : 81 mg/mL (184.3 mM) H2O : < 1 mg/mL (insoluble or slightly soluble) DMSO : 81 mg/mL (184.3 mM) |
| Keywords | BFH-772 | inhibit | VEGFR | BFH 722 | Vascular endothelial growth factor receptor | Inhibitor | BFH722 | BFH 772 | BFH772 |
| Inhibitors Related | Ribociclib | Nintedanib | Regorafenib monohydrate | Sunitinib Malate | Sorafenib | Regorafenib | Sanguinarine chloride | Nintedanib esylate | Sorafenib tosylate | Lenvatinib mesylate | Pazopanib | Axitinib |
| Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Clinical Compound Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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United States- Since: 2011-01-07
- Address: 36 Washington Street, Wellesley Hills
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