Physicochemical Properties
| Molecular Formula | C22H25BRF5N5O5S |
| Molecular Weight | 646.43 |
| CAS # | 2805804-54-8 |
| Related CAS # | CP-547632;252003-65-9;CP-547632 hydrochloride;252003-71-7 |
| Appearance | Off-white to light yellow solid powder |
| HS Tariff Code | 2934.99.9001 |
| Storage |
Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition | Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs) |
Biological Activity
| Targets | VEGFR2 11 nM (IC50) FGFR 9 nM (IC50) |
| ln Vitro | With an IC50 value of 6 nM, CP-547632 TFA (1-1000 nM; 1 hour) inhibits VEGF-stimulated VEGFR-2 phosphorylation in a dose-dependent manner[1]. |
| ln Vivo | Colo-205, DLD-1, and MDA-MB-231 xenografts experience a dose-dependent growth inhibition in response to CP-547632 TFA (po; 6.25-100 mg/kg/day; for 10-24 days)[1]. Oral CP-547632 TFA administered at a dose of 50 mg/kg produces plasma concentrations greater than 500 ng/ml for a duration of 12 hours[1]. |
| Cell Assay |
Western Blot Analysis[1] Cell Types: Serum- deprived cells Tested Concentrations: 1, 4, 16, 63, 250, 1000 nM Incubation Duration: 1 hrs (hours) Experimental Results: Inhibited VEGF-stimulated VEGFR-2 phosphorylation in a dose-dependent fashion. |
| Animal Protocol |
Animal/Disease Models: Athymic female mice (CD-1 nu/nu) bearing tumors (75 -150 mm in size)[1] Doses: 6.25, 12.5, 25, 50, 100 mg/kg Route of Administration: PO; daily; 10-24 days Experimental Results: Caused a dose-dependent inhibition of growth in Colo-205, DLD- 1, and MDA-MB-231 xenografts. Animal/Disease Models: Female athymic mice bearing H-Ras tumor[1] Doses: 50 mg/kg Route of Administration: Oral Experimental Results: A single oral dose of 50 mg/kg yielded plasma concentrations above 500 ng /ml for 12 hrs (hours). |
| References |
[1]. Pharmacological characterization of CP-547,632, a novel vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor for cancer therapy. Cancer Res. 2003 Nov 1;63(21):7301-9. |
Solubility Data
| Solubility (In Vitro) | DMSO: 150 mg/mL (232.04 mM) |
| 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 (e.g. IP/IV/IM/SC) Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline) *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). 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)] *Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline) Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline) Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline) Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil) Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL 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). Oral Formulation 3: Dissolved in PEG400 Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose Oral Formulation 6: Mixing with food powders Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5470 mL | 7.7348 mL | 15.4696 mL | |
| 5 mM | 0.3094 mL | 1.5470 mL | 3.0939 mL | |
| 10 mM | 0.1547 mL | 0.7735 mL | 1.5470 mL |