2. Apoptosis GPCR/G Protein
  3. Apoptosis PTHR
  4. Tigapotide

Tigapotide (PCK-3145) is a synthetic 15-mer peptide derived from prostate-secretory protein, and acts as an antineoplastic agent. Tigapotide inhibits tumor growth, experimental bone metastasis, and malignancy-associated hypocalcemia. Tigapotide induces apoptosis in prostate cancer cells and tumors, and suppresses the growth of prostate cancer cells. Tigapotide inhibits the production of parathyroid hormone-related protein (PTHrP) in tumors and plasma. Tigapotide reduces plasma calcium levels in hypercalcemic tumor-bearing rats. Tigapotide is applicable for the research of prostate cancer and malignancy-associated hypercalcemia.

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Tigapotide

Tigapotide Chemical Structure

CAS No. : 848084-83-3

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Tigapotide Related Antibodies

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Description

Tigapotide (PCK-3145) is a synthetic 15-mer peptide derived from prostate-secretory protein, and acts as an antineoplastic agent. Tigapotide inhibits tumor growth, experimental bone metastasis, and malignancy-associated hypocalcemia. Tigapotide induces apoptosis in prostate cancer cells and tumors, and suppresses the growth of prostate cancer cells. Tigapotide inhibits the production of parathyroid hormone-related protein (PTHrP) in tumors and plasma. Tigapotide reduces plasma calcium levels in hypercalcemic tumor-bearing rats. Tigapotide is applicable for the research of prostate cancer and malignancy-associated hypercalcemia[1][2].

In Vitro

Tigapotide causes dose-dependent inhibition of MatLyLu-PTHrP prostate cancer cell growth in in vitro[2].
Tigapotide 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.

Tigapotide Related Antibodies
In Vivo

Tigapotide (1-100 μg/kg/day; subcutaneous injection; daily administration; up to 15 days) dose-dependently inhibits the growth of primary prostate tumors in subcutaneous MatLyLu-PTHrP xenografts in male Copenhagen rats, reduces PTHrP levels in tumor tissues and plasma, decreases plasma calcium levels, induces tumor cell apoptosis, significantly delays the progression of hindlimb paralysis caused by prostate cancer bone metastasis in male rats, and reduces tumor burden in their lumbar vertebrae[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Copenhagen rats (male, inoculated s.c. into the right flank with MatLyLu-PTHrP cells)[2]
Dosage: 1.0 μg/kg/day; 10 μg/kg/day; 100 μg/kg/day
Administration: s.c.; daily; up to 15 days
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.
Clinical Trial
Molecular Weight

2025.15

Formula

C82H121N21O33S3
CAS No.
Sequence

Glu-Trp-Gln-Thr-Asp-Asn-{Cys(Acm)}-Glu-Thr-{Cys(Acm)}-Thr-{Cys(Acm)}-Tyr-Glu-Thr
Sequence Shortening

EWQTDN-{Cys(Acm)}-ET-{Cys(Acm)}-T-{Cys(Acm)}-YET
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Tigapotide Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Tigapotide848084-83-3PCK-3145PCK3145PCK 3145ApoptosisPTHRParathyroid hormone receptorhypercalcemia of malignancyparathyroid hormone-related proteinmale Copenhagen ratshypercalcemic tumor-bearing ratsprostate cancerprostate cancer cellshormone-refractory prostate cancerprostate secretory proteinskeletal metastasesMatLyLu-PTHrP prostate cancer cellsInhibitorinhibitorinhibit

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