| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 100mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
VEGFR2 (IC50 = 62 nM)
BIBF-1202 targets VEGFR2 (vascular endothelial growth factor receptor 2), a key receptor tyrosine kinase involved in angiogenesis. It inhibits VEGFR2 kinase with an IC₅₀ of 62 nM. As the primary metabolite of nintedanib, BIBF-1202 retains the antiangiogenic activity of the parent compound. VEGFR2 is a critical mediator of tumor angiogenesis, and its inhibition leads to reduced tumor vascularization and growth. The compound's activity against VEGFR2 makes it a valuable tool for studying angiogenesis and developing antiangiogenic cancer therapies. |
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| ln Vitro |
BIBF 1120's primary metabolic route involves methyl ester cleavage to produce BIBF 1202. Following this, BIBF 1202's free carboxyl group undergoes glucuronidation to yield 1-O-acylglucuronide [2].
In vitro, BIBF-1202 is a potent inhibitor of VEGFR2 kinase with an IC₅₀ of 62 nM. It is produced in the main metabolic pathway of nintedanib (BIBF 1120) by the cleavage of methyl esters. The free carboxyl group of BIBF-1202 is then glucuronidated to 1-O-acyl glucuronide. In cell-based assays, BIBF-1202 inhibits VEGFR2-mediated signaling, leading to reduced endothelial cell proliferation, migration, and tube formation. The compound's antiangiogenic activity makes it useful for studying tumor vascularization and developing antiangiogenic therapies. |
| ln Vivo |
In vivo, BIBF-1202 is the primary metabolite of nintedanib (BIBF 1120) and contributes to the overall pharmacological activity of the parent drug. As a VEGFR2 inhibitor with an IC₅₀ of 62 nM, BIBF-1202 has antiangiogenic effects that can reduce tumor growth and metastasis. The compound is primarily used in preclinical cancer research to study antiangiogenic therapy and tumor vascularization. Comprehensive in vivo studies of BIBF-1202 alone are limited, as it is typically studied as part of nintedanib's metabolic profile.
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| Enzyme Assay |
In vitro enzyme assays for BIBF-1202 involve measuring the inhibition of VEGFR2 kinase activity. The assay typically uses recombinant VEGFR2 kinase incubated with varying concentrations of BIBF-1202 in the presence of ATP and a peptide substrate. The phosphorylation of the substrate is measured using scintillation counting or fluorescence-based methods. The IC₅₀ for VEGFR2 inhibition is 62 nM. The compound's selectivity for VEGFR2 over other kinases can be assessed using kinase panel screening. These assays confirm the compound's potent activity against VEGFR2.
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| Cell Assay |
In vitro cell-based assays for BIBF-1202 evaluate its effects on endothelial cell function. Human umbilical vein endothelial cells (HUVECs) or other endothelial cell lines are cultured and treated with serial dilutions of BIBF-1202. The compound's effects on cell proliferation are assessed using MTT or BrdU incorporation assays. Endothelial cell migration is evaluated using scratch wound or Boyden chamber assays. Tube formation is assessed using Matrigel-based angiogenesis assays. These assays confirm the compound's antiangiogenic activity in cellular contexts.
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| Animal Protocol |
In vivo animal experiments for BIBF-1202 are not extensively reported, as the compound is primarily studied as the metabolite of nintedanib. For potential in vivo studies, BIBF-1202 can be administered orally or via intraperitoneal injection in mouse xenograft models of cancer. The compound is soluble in DMSO at 40 mg/mL. Tumor growth inhibition and vascularization would be assessed by caliper measurements and immunohistochemistry for CD31 or other endothelial markers. Comprehensive in vivo studies are needed to establish the efficacy of BIBF-1202 alone.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) data for BIBF-1202 are derived from studies of nintedanib metabolism. BIBF-1202 is the primary carboxylate metabolite of nintedanib, formed by the cleavage of methyl esters. The free carboxyl group of BIBF-1202 is then glucuronidated to 1-O-acyl glucuronide. The compound has a molecular weight of 525.6 g/mol and is soluble in DMSO at 40 mg/mL. Comprehensive PK studies of BIBF-1202 alone are limited, as it is typically studied as part of nintedanib's metabolic profile.
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| Toxicity/Toxicokinetics |
The toxicity profile of BIBF-1202 has not been extensively characterized, as the compound is primarily studied as a metabolite. For laboratory handling, BIBF-1202 should be treated as a hazardous chemical. Appropriate personal protective equipment should be used when handling the compound. The compound is for research use only and is not intended for human or veterinary use. Comprehensive toxicological studies are needed to fully characterize the safety profile of BIBF-1202.
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| References | |
| Additional Infomation |
BIBF-1202 is the primary carboxylate metabolite of nintedanib (BIBF 1120) and inhibits VEGFR2 kinase with an IC₅₀ of 62 nM. It has a molecular formula of C₃₀H₃₁N₅O₄ and a molecular weight of 525.6 g/mol. BIBF-1202 is formed through the cleavage of the methyl ester moiety of nintedanib. The compound is primarily used in preclinical cancer research to study antiangiogenic therapy and receptor tyrosine kinase-driven signaling. BIBF-1202 is for research use only and is not intended for human use.
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| Molecular Formula |
C30H31N5O4
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|---|---|
| Molecular Weight |
525.61
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| Exact Mass |
525.238
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| Elemental Analysis |
C, 68.55; H, 5.95; N, 13.32; O, 12.18
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| CAS # |
894783-71-2
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| Related CAS # |
BIBF 1202-13C,d3
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| PubChem CID |
135461425
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3.614
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
39
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| Complexity |
877
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(/C1C=CC=CC=1)(=C1\C(=O)NC2C=C(C=CC\1=2)C(=O)O)\NC1C=CC(N(C)C(=O)CN2CCN(C)CC2)=CC=1
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| InChi Key |
SDJMWYVJAVLZEG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C30H31N5O4/c1-33-14-16-35(17-15-33)19-26(36)34(2)23-11-9-22(10-12-23)31-28(20-6-4-3-5-7-20)27-24-13-8-21(30(38)39)18-25(24)32-29(27)37/h3-13,18,32,37H,14-17,19H2,1-2H3,(H,38,39)
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| Chemical Name |
2-hydroxy-3-[N-[4-[methyl-[2-(4-methylpiperazin-1-yl)acetyl]amino]phenyl]-C-phenylcarbonimidoyl]-1H-indole-6-carboxylic acid
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| Synonyms |
BIBF-1202; BIBF1202; BIBF 1202
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ≥ 45 mg/mL (~85.6 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9026 mL | 9.5128 mL | 19.0255 mL | |
| 5 mM | 0.3805 mL | 1.9026 mL | 3.8051 mL | |
| 10 mM | 0.1903 mL | 0.9513 mL | 1.9026 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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