| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
TRPV6 14 nM (IC50)
TRPV6 (Transient Receptor Potential Vanilloid 6), a non-voltage-gated calcium channel. SOR-C13 TFA binds to the TRPV6 channel with high affinity (IC50 = 14 nM), blocking calcium ion entry into cells. In cancer cells, this inhibits calcium-dependent pro-survival signaling pathways, leading to cell cycle arrest and apoptosis. Inhibition of TRPV6 is associated with reduced malignancy and improved prognosis. |
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| ln Vitro |
In vitro, SOR-C13 TFA potently blocks TRPV6-mediated calcium influx in TRPV6-overexpressing cancer cells at sub-micromolar concentrations. This block leads to the disruption of calcium homeostasis, activation of the unfolded protein response (UPR), and a reduction in cell proliferation. It demonstrates selective cytotoxicity against cancer cell lines that upregulate TRPV6, while having minimal effect on normal cells that do not express the channel.
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| ln Vivo |
In female NOD/SCID mice, SOR-C13 (intraperitoneal injection; 400, 600, 800 mg/kg; daily; days 1 to 12) TFA can significantly suppress the formation of SKOV-3 cell tumors [2].
In vivo, SOR-C13 TFA has demonstrated significant anticancer activity. In orthotopic xenograft mouse models of breast cancer, systemic administration of SOR-C13 TFA results in the inhibition of primary tumor growth and, importantly, a substantial reduction in metastasis formation. These therapeutic effects are accompanied by biomarker changes indicative of UPR activation and apoptosis within the tumor tissue, validating TRPV6 as an anticancer target. |
| Enzyme Assay |
A TRPV6-mediated calcium influx assay is performed. HEK293 cells stably overexpressing the human TRPV6 channel are loaded with a calcium-sensitive fluorescent dye (e.g., Fluo-4 AM). Cells are pre-incubated with increasing concentrations of SOR-C13 TFA (0-1000 nM) for 5-10 min. Calcium influx is then triggered by adding a TRPV6-specific activator or by reducing the extracellular magnesium concentration. The change in fluorescence is measured using a plate reader, and the IC50 is calculated.
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| Cell Assay |
TRPV6-positive breast cancer cells (e.g., MDA-MB-231) are seeded in a 96-well plate. The next day, cells are treated with varying concentrations of SOR-C13 TFA (0-1000 nM) for 48-72 hours. Cell viability is assessed using a standard MTT or CellTiter-Glo assay. To confirm the mechanism, cells can be treated with the peptide for 24 h and then stained with Annexin V/PI for apoptosis analysis by flow cytometry.
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| Animal Protocol |
Animal/Disease Models: Female NOD/SCID (severe combined immunodeficient) mouse with SKOV-3 cell[2]
Doses: 400, 600, 800 mg/kg Route of Administration: IP; daily; on days 1 to 12 Experimental Results: Effectively inhibited the growth of tumor. Female athymic nude mice (6-8 weeks old) are orthotopically injected with luciferase-labeled breast cancer cells into the mammary fat pad. Once tumors are established, mice are randomized into groups (n=8-10). SOR-C13 TFA is administered via intraperitoneal injection at doses of 5-15 mg/kg, daily or every other day, for 3-4 weeks. Tumor growth is monitored by calipers and bioluminescence imaging. Lung metastases are counted at the end of the study. |
| ADME/Pharmacokinetics |
As a 13-amino acid peptide (MW ~1679.84), SOR-C13 TFA has a short plasma half-life due to proteolytic degradation, typically on the order of minutes to a few hours. It is administered via injection (i.p. or i.v.) and has poor oral bioavailability. The TFA salt form is used to improve solubility and stability. In mice, once-daily injection is sufficient to achieve a therapeutic effect.
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| Toxicity/Toxicokinetics |
SOR-C13 TFA is a research compound not approved for human clinical use. In animal studies, it is well-tolerated at therapeutic doses (5-15 mg/kg, i.p.) with no significant body weight loss or organ toxicity reported. Since TRPV6 is not widely expressed in normal adult tissues, SOR-C13 TFA is expected to have a low risk of on-target toxicity, making it a selective anticancer agent. SOR-C13 TFA is for research purposes only.
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| References |
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| Additional Infomation |
SOR-C13 TFA is a first-in-class peptide antagonist of TRPV6. It is one of the most advanced TRPV6-targeting agents in preclinical development. This compound is a valuable probe for studying the role of calcium signaling in cancer progression and metastasis. The free acid version has the CAS number 1187852-48-7. The compound should be stored as a powder at -20degC, protected from light and moisture.
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| Molecular Formula |
C74H117F3N20O21
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| Molecular Weight |
1679.84
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| Related CAS # |
SOR-C13;1187852-48-7
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| Appearance |
White to off-white solid powder
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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 and light. |
| 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) |
H2O :~100 mg/mL (~59.53 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 | 0.5953 mL | 2.9765 mL | 5.9529 mL | |
| 5 mM | 0.1191 mL | 0.5953 mL | 1.1906 mL | |
| 10 mM | 0.0595 mL | 0.2976 mL | 0.5953 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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