| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
VEGFR2 (KDR; pIC50 = 7.81) and Tie-2 (TEK); also inhibits tropomyosin-related kinases TRKA, TRKB and TRKC (71-88% inhibition at 100 nM).
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| ln Vitro |
In NCI-60 panel screening, the GW768505A free base has the effect of preventing the proliferation of cancer cells [2]. Protomycin-related kinases TRKA, TRKB, and TRKC are all potently inhibited by GW768505A free base, which also inhibits KDR and TIE2 (71–88 percent inhibition at 100 nM) [2].
GW768505A demonstrates potent inhibition of KDR and TIE2 (71-88% inhibition at 100 nM). It inhibits proliferation of cancer cells in NCI-60 panel screening and exhibits anti-angiogenic activity in endothelial cell assays. In HFF cells, cytotoxic IC50 = 0.79 microM. |
| ln Vivo |
Specific in vivo efficacy data for this compound are not detailed in standard references; as a dual VEGFR2/Tie-2 inhibitor with anti-angiogenic activity, it would be expected to inhibit tumor growth and angiogenesis in xenograft models, though quantitative in vivo data are unavailable in public literature.
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| Enzyme Assay |
Cell-free kinase assays: Recombinant VEGFR2 (KDR) or Tie-2 kinases are incubated with ATP and substrate in the presence of varying GW768505A concentrations. Kinase activity is measured by phosphorylation of peptide substrates using fluorescence polarization or radioactive methods (e.g., 33P-ATP incorporation). pIC50 = 7.81 is derived from concentration-response curves.
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| Cell Assay |
Cancer cell growth inhibition in NCI-60 panel screening: 60 human cancer cell lines (9 tumor types) are treated with GW768505A at varying concentrations (typically 10-⁸-10-⁴ M) for 48h; cell viability assessed by sulforhodamine B (SRB) assay. Cytotoxicity in HFF cells: IC50 = 0.79 microM determined via standard viability assays.
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| Animal Protocol |
In vivo animal protocols for this specific compound are not described in the available literature; as a VEGFR2/Tie-2 inhibitor, typical in vivo studies would involve subcutaneous xenograft models in immunocompromised mice with oral or intraperitoneal administration, measuring tumor volume, angiogenesis markers (CD31), and body weight.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for GW768505A are not detailed in standard references; molecular weight 537.47, LogP 5.4, DMSO solubility ~8.33 mg/mL (~15.50 mM), predicted high plasma protein binding and limited oral bioavailability typical of highly lipophilic kinase inhibitors. Terminal half-life and clearance not reported.
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| Toxicity/Toxicokinetics |
No detailed toxicity data in public literature; safety data sheet indicates under fire conditions may decompose and emit toxic fumes. Avoid release into the environment (aquatic toxicity may be a concern for heterocyclic compounds). In vitro cytotoxicity: IC50 = 0.79 microM in HFF cells. Standard laboratory precautions recommended.
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| References | |
| Additional Infomation |
GW768505A was first disclosed in Bioorganic & Medicinal Chemistry Letters (2007) as an orally active 4-amino-5-diarylurea-furo[2,3-d]pyrimidine derivative with anti-angiogenic activity. Characterized in the Published Kinase Inhibitor Set (2016) showing inhibition of TRKA/B/C. Not entered clinical trials; for research use only. Potential applications in oncology (anti-angiogenesis) and vascular biology. Also referred to as GW-768505A or GW768505A free base.
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| Molecular Formula |
C₂₇H₁₉F₄N₅O₃
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|---|---|
| Molecular Weight |
537.47
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| Exact Mass |
573.119
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| CAS # |
501693-25-0
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| PubChem CID |
5326956
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
5.4
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
39
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| Complexity |
822
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=CC=C(C=C1)C2=C(C3=C(N=CN=C3O2)N)C4=CC=C(C=C4)NC(=O)NC5=C(C=CC(=C5)C(F)(F)F)F
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| InChi Key |
FGZIONRFHVNRJB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H19F4N5O3/c1-38-18-9-4-15(5-10-18)23-21(22-24(32)33-13-34-25(22)39-23)14-2-7-17(8-3-14)35-26(37)36-20-12-16(27(29,30)31)6-11-19(20)28/h2-13H,1H3,(H2,32,33,34)(H2,35,36,37)
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| Chemical Name |
1-[4-[4-amino-6-(4-methoxyphenyl)furo[2,3-d]pyrimidin-5-yl]phenyl]-3-[2-fluoro-5-(trifluoromethyl)phenyl]urea
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| Synonyms |
GW 768505A free base; GW-768505A free base
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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 : ~8.33 mg/mL (~15.50 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 | 1.8606 mL | 9.3028 mL | 18.6057 mL | |
| 5 mM | 0.3721 mL | 1.8606 mL | 3.7211 mL | |
| 10 mM | 0.1861 mL | 0.9303 mL | 1.8606 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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