Tigapotide TFA
Tigapotide TFA (PCK-3145 TFA) is a synthetic 15-mer peptide derived from prostate-secretory protein, and acts as an antineoplastic agent. Tigapotide TFA inhibits tumor growth, experimental bone metastasis, and malignancy-associated hypocalcemia. Tigapotide TFA induces Apoptosis in prostate cancer cells and tumors, and suppresses the growth of prostate cancer cells. Tigapotide TFA inhibits the production of parathyroid hormone-related protein (PTHrP) in tumors and plasma. Tigapotide TFA reduces plasma calcium levels in hypercalcemic tumor-bearing rats. Tigapotide TFA is applicable for the research of prostate cancer and malignancy-associated hypercalcemia.
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- CAS. Nr.: 848084-84-4
- Formel: C84H120F3N21O36S3
- Molecular Weight:2153.17
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Tigapotide TFA causes dose-dependent inhibition of MatLyLu-PTHrP prostate cancer cell growth in in vitro[2].
Tigapotide TFA induces apoptosis in MatLyLu-PTHrP prostate cancer cells in vitro[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Copenhagen rats (male, inoculated s.c. into the right flank with MatLyLu-PTHrP cells)[2]
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Dosage:1.0 μg/kg/day; 10 μg/kg/day; 100 μg/kg/day
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Administration:s.c.; daily; up to 15 days
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Result:Caused a dose-dependent inhibition of MatLyLu-PTHrP tumor growth, with statistically significant tumor volume reductions at 10.0 μg/kg/day and 100.0 μg/kg/day compared to vehicle controls at Day 14 and Day 16.
Reduced tumoral PTHrP production in a dose-dependent manner, with the highest dose producing the most pronounced effect.
Reduced plasma PTHrP levels in a dose-dependent manner, with statistically significant reductions at 10.0 μg/kg/day and 100.0 μg/kg/day compared to vehicle controls, with levels falling to ~60 pmol equivalents/l and ~45 pmol equivalents/l, respectively.
Reduced plasma calcium levels in a dose-dependent manner, with statistically significant reductions at 10.0 μg/kg/day and 100.0 μg/kg/day compared to vehicle controls, with levels falling to ~4.0 mmol/l and ~3.6 mmol/l, respectively.
Induced tumor cell apoptosis as measured by DNA fragmentation and TUNEL assay.
Significantly delayed the development of hind-limb paralysis compared to vehicle controls, with a higher percentage of non-paralyzed animals remaining at Days 14, 15, and 16.
Exhibited a significant decrease in tumor burden in the lumbar vertebrae compared to vehicle controls.
Was more effective at delaying the development of skeletal metastases than equimolar concentrations of PSP-94.
Chemical Information
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CAS. Nr. 848084-84-4
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Molecular Weight 2153.17
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Formel C84H120F3N21O36S3
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SMILES
C(C(O)=O)(F)(F)F.C([C@@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@@H](CC1=CC=C(O)C=C1)C(N[C@H](C(N[C@@H]([C@@H](C)O)C(O)=O)=O)CCC(O)=O)=O)=O)CSCNC(C)=O)=O)[C@@H](C)O)=O)CSCNC(C)=O)=O)[C@@H](C)O)=O)CCC(O)=O)=O)CSCNC(C)=O)=O)CC(N)=O)=O)CC(O)=O)=O)[C@@H](C)O)=O)CCC(N)=O)=O)NC([C@H](CCC(O)=O)N)=O)C=2C=3C(NC2)=CC=CC3
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Synonyms
PCK 3145 TFA
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Pippa, N., et al. Advanced nanocarriers for an antitumor peptide. J Nanopart Res 15, 2062 (2013).
[2]. Shukeir N, et al. Prostate secretory protein of 94 amino acids (PSP-94) and its peptide (PCK3145) as potential therapeutic modalities for prostate cancer. Anticancer Drugs. 2005;16(10):1045-1051. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Tigapotide TFA Related Classifications
HY-16497 Related Classifications
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- Tigapotide
- 848084-84-4
- PCK 3145
- PCK3145
- PCK-3145
- Apoptosis
- PTHR
- hypercalcemia of malignancy
- parathyroid hormone-related protein
- male Copenhagen rats
- hypercalcemic tumor-bearing rats
- prostate cancer
- prostate cancer cells
- hormone-refractory prostate cancer
- prostate secretory protein
- skeletal metastases
- MatLyLu-PTHrP prostate cancer cells
- Inhibitor
- inhibitor
- inhibit