| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg | |||
| 250mg | |||
| 500mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
VEGFR-2 (IC50 = 11 nM); FGFR (IC50 = 9 nM)
Target: CP-547632 targets VEGFR-2 (vascular endothelial growth factor receptor 2) and basic fibroblast growth factor (FGF) kinases with IC50 values of 11 nM and 9 nM respectively. As an ATP-competitive kinase inhibitor, it blocks VEGFR-2 kinase autophosphorylation. In whole cell assays, it inhibits VEGF-stimulated autophosphorylation of VEGFR-2 with an IC50 value of 6 nM. The compound inhibits both basic FGF and VEGF-induced angiogenesis in vivo. |
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| ln Vitro |
CP-547632 (1-1000 nM; 1 hour) has an IC50 value of 6 nM and suppresses VEGF-stimulated VEGFR-2 phosphorylation in a dose-dependent manner [1].
In Vitro Activity: CP-547632 (1-1000 nM; 1 hour) suppresses VEGF-stimulated VEGFR-2 phosphorylation in a dose-dependent manner with an IC50 value of 6 nM. It demonstrates potent inhibition of VEGFR2 and FGF2 kinases with IC50 values of 11 and 9 nM respectively. The compound is an ATP-competitive kinase inhibitor that blocks VEGFR-2 kinase autophosphorylation. Detailed cellular activity and selectivity data are available from the primary literature. |
| ln Vivo |
CP-547632 (1-1000 nM; 1 hours)inhibits VEGF-stimulated VEGFR-2 phosphorylation in a dose-dependent manner, with an IC50 value of 6 nM[1].
In Vivo Activity: Following oral administration of CP-547632 to mice harboring NIH3T3/H-ras tumors, VEGFR-2 phosphorylation in tumors was inhibited in a dose-dependent manner with an EC50 of 590 ng/mL. These plasma concentrations showed a strong correlation with levels required to prevent VEGF-induced corneal angiogenesis in BALB/c mice. Once daily intraperitoneal administration to athymic mice carrying human xenografts demonstrated up to 85% tumor growth inhibition. CP-547632 has been used in clinical trials studying ovarian cancer, lung neoplasms, peritoneal neoplasms, and fallopian tube cancer. |
| Enzyme Assay |
CP-547632 (p.o.; 6.25-100 mg/kg/day; for 10-24 days) nhibits Colo-205, DLD-1, and MDA-MB-231 xenografts' ability to grow in a dose-dependent manner[1]. For 12 hours, plasma concentrations of CP-547632 (oral; 50 mg/kg; single oral dose) are greater than 500 ng/ml[1].
In Vitro Enzyme/Receptor Binding Protocol: Kinase assays typically use recombinant VEGFR-2 or FGF kinase domains and radiolabeled ATP. Inhibition of kinase activity is measured in the presence of varying concentrations of CP-547632. IC50 values are determined from dose-response curves. Selectivity is assessed against a panel of related kinases including PDGFR and EGFR. For whole cell assays, VEGF-stimulated autophosphorylation of VEGFR-2 is measured by immunoprecipitation and Western blotting. |
| Cell Assay |
Western Blot Analysis[1]
Cell Types: Serum-depleted Cell Tested Concentrations: 1, 4, 16, 63, 250, 1000 nM Incubation Duration: 1 hour Experimental Results: Inhibits VEGF-stimulated VEGFR-2 phosphorylation in a dose-dependent manner. In Vitro Cell-Based Assay Protocol: Cells expressing VEGFR-2 are treated with CP-547632 at concentrations ranging from 1 to 1000 nM for 1 hour. VEGFR-2 phosphorylation is assessed by immunoprecipitation followed by Western blotting using phospho-specific antibodies. Cell proliferation and viability assays are performed using standard methods such as MTT or BrdU incorporation. Angiogenesis assays including endothelial cell tube formation and migration assays may also be employed. |
| Animal Protocol |
Athymic female mice (CD-1 nu/nu) bearing tumors (75-150 mm in size)[1]
6.25, 12.5, 25, 50, 100 mg/kg PO; daily; 10-24 days In Vivo Animal Assay Protocol: Athymic mice carrying human xenografts (Colo-205, DLD-1, MDA-MB-231) are administered CP-547632 orally or intraperitoneally at doses ranging from 6.25 to 100 mg/kg/day for 10-24 days. Tumor growth inhibition is monitored by caliper measurement. For pharmacodynamic studies, VEGFR-2 phosphorylation in tumors is assessed. Corneal angiogenesis assays in BALB/c mice evaluate the compound's ability to prevent VEGF-induced angiogenesis. |
| ADME/Pharmacokinetics |
Pharmacokinetics: CP-547632 is orally bioavailable. Following oral administration, plasma concentrations correlate with pharmacodynamic effects such as VEGFR-2 phosphorylation inhibition and anti-angiogenic activity. The compound has been characterized as a well-tolerated, orally bioavailable inhibitor. Detailed PK parameters including half-life, Cmax, and bioavailability have been studied in preclinical models and clinical trials.
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| Toxicity/Toxicokinetics |
Toxicity: CP-547632 has been evaluated in clinical trials as a well-tolerated inhibitor. No significant toxicity concerns have been reported at therapeutic doses. Comprehensive toxicity data are available from clinical studies. Common adverse effects are typical of VEGFR inhibitors and may include hypertension, fatigue, and gastrointestinal disturbances. The compound is for research and clinical investigation use and is not approved for general therapeutic use.
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| References | |
| Additional Infomation |
CP-547632 has been used in trials investigating the treatment of ovarian cancer, lung tumors, ovarian tumors, peritoneal tumors, and fallopian tube cancer.
Additional Information: CP-547632 has CAS number 252003-65-9. It is also known as PAN-90806, OSI-632, CP-632, and CP547632. The compound is a VEGFR2 antagonist and angiogenesis inhibitor. It has been studied in Phase 1/2 clinical trials including NCT00074854 (combination with chemotherapy) and NCT00096239 (ovarian cancer, primary peritoneal cancer, fallopian tube cancer). For research use only, not for human therapy. |
| Molecular Formula |
C20H24BRF2N5O3S
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|---|---|
| Molecular Weight |
532.40206
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| Exact Mass |
531.075
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| Elemental Analysis |
C, 45.12; H, 4.54; Br, 15.01; F, 7.14; N, 13.15; O, 9.02; S, 6.02
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| CAS # |
252003-65-9
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| Related CAS # |
CP-547632 hydrochloride;252003-71-7;CP-547632 TFA;2805804-54-8
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| PubChem CID |
9811611
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| Appearance |
White to light yellow solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
548.6±50.0 °C at 760 mmHg
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| Flash Point |
285.6±30.1 °C
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| Vapour Pressure |
0.0±1.5 mmHg at 25°C
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| Index of Refraction |
1.622
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| LogP |
3.69
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
32
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| Complexity |
622
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(NC1=C(C(N)=O)C(OCC2=C(F)C=C(Br)C=C2F)=NS1)NCCCCN3CCCC3
|
| InChi Key |
HXHAJRMTJXHJJZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H24BrF2N5O3S/c21-12-9-14(22)13(15(23)10-12)11-31-18-16(17(24)29)19(32-27-18)26-20(30)25-5-1-2-6-28-7-3-4-8-28/h9-10H,1-8,11H2,(H2,24,29)(H2,25,26,30)
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| Chemical Name |
3-[(4-bromo-2,6-difluorophenyl)methoxy]-5-(4-pyrrolidin-1-ylbutylcarbamoylamino)-1,2-thiazole-4-carboxamide
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| Synonyms |
PAN90806; PAN 90806; PAN-90806; CP547632; CP 547632; CP-547632; CP632; OSI632; CP 632; OSI 632; CP-632; OSI-632
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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 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)
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| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~187.8 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 4 mg/mL (7.51 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 40.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 4 mg/mL (7.51 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 40.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 4 mg/mL (7.51 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8783 mL | 9.3914 mL | 18.7829 mL | |
| 5 mM | 0.3757 mL | 1.8783 mL | 3.7566 mL | |
| 10 mM | 0.1878 mL | 0.9391 mL | 1.8783 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00096239 | Completed | Drug: CP-547,632 | Fallopian Tube Cancer Ovarian Cancer |
Jonsson Comprehensive Cancer Center |
December 2004 | Phase 2 |
| NCT00074854 | Completed | Drug: CP-547,632 | Lung Neoplasms | Pfizer | May 2002 | Phase 1 Phase 2 |
| NCT00074867 | Completed | Drug: CP-547,632 | Ovarian Neoplasms Peritoneal Neoplasms |
Pfizer | October 2003 | Phase 2 |
 Lineweaver Burke plot of ATP competition. Inhibition of kinase autophosphorylation with CP-547,632. Phospho-VEGFR-2 in cell-based assay. CP-547,632 inhibits VEGF-stimulated phosphorylation in cells with an IC50value of 6 nm.Cancer Res. 2003 Nov 1;63(21):7301-9. |
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 Effect of CP-547,632 on the growth of human tumorsin vivo.Cancer Res. 2003 Nov 1;63(21):7301-9. |
 Pharmacokinetic and pharmacodynamic evaluation of CP-547,632 after a single oral dose (50 mg/kg) in H-rastumor-bearing mice.
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