| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
The nuclear form of beta‑catenin, specifically its interaction with TCF4 (T‑cell factor 4).
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| ln Vitro |
aStAx-35R TFA is a stapled peptide that acts as a competitive inhibitor of the beta‑catenin/TCF4 interaction. It selectively induces growth inhibition in Wnt‑dependent cancer cells by disrupting the transcriptional activity of the beta‑catenin/TCF4 complex. This inhibition leads to reduced expression of Wnt target genes such as Cyclin D1 and c‑Myc, resulting in cell cycle arrest and apoptosis.
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| ln Vivo |
In vivo, aStAx-35R TFA has demonstrated anti‑tumor activity in mouse xenograft models of colorectal cancer. When administered via intraperitoneal injection, the peptide inhibits tumor growth by suppressing Wnt/beta‑catenin signaling, leading to reduced proliferation and increased apoptosis in tumor tissues.
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| Enzyme Assay |
A general cell‑free protocol for assessing beta‑catenin/TCF4 binding: A fluorescence polarization (FP) or TR‑FRET assay is used. Purified beta‑catenin protein (50 nM) is incubated with a fluorescently labeled TCF4 peptide (5 nM) in assay buffer (20 mM Tris‑HCl, pH 7.5, 150 mM NaCl, 0.01% Tween‑20, 1 mM DTT) with varying concentrations of aStAx-35R TFA (0.01‑100 uM). The FP signal is measured after 30 minutes to calculate the IC50.
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| Cell Assay |
A general cellular protocol for assessing Wnt/beta‑catenin inhibition: Wnt‑dependent cancer cells (e.g., HCT116, SW480) are seeded in 96‑well plates. Cells are treated with serial dilutions of aStAx-35R TFA (0.1‑50 uM) for 48‑72 hours. Cell viability is measured using CellTiter‑Glo assay. For Western blot, cells are treated for 24 hours, lysed, and probed with anti‑beta‑catenin, anti‑Cyclin D1, anti‑c‑Myc, and anti‑GAPDH antibodies.
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| Animal Protocol |
General animal protocol for aStAx-35R TFA: Female NOD/SCID mice are subcutaneously implanted with 5×10⁶ HCT116 colon cancer cells. When tumors reach ~150 mm3, mice are randomized (n=8/group). aStAx-35R TFA is formulated in sterile saline and administered via intraperitoneal (IP) injection at doses of 5, 10, and 20 mg/kg once daily for 21 days. Tumor volume is measured twice weekly. At study end, tumors are harvested for IHC (Ki‑67, cleaved caspase‑3, beta‑catenin), Western blot, and TUNEL staining.
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| ADME/Pharmacokinetics |
General PK protocol for stapled peptides: aStAx-35R TFA is administered to mice via IP (10 mg/kg) and IV (2 mg/kg). Blood samples are collected at 0.083, 0.25, 0.5, 1, 2, 4, 8, and 24 hours. Plasma concentrations are quantified by LC‑MS/MS. PK parameters (Cmax, Tmax, AUC, t1/2, clearance, Vd, and IP bioavailability) are calculated. Peptides typically have a short half‑life due to proteolysis.
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| Toxicity/Toxicokinetics |
General toxicity protocol for aStAx-35R TFA: A 14‑day repeat‑dose IP toxicity study is performed in ICR mice. aStAx-35R TFA is administered at doses of 5, 15, and 40 mg/kg/day. Parameters include clinical signs, body weight, food consumption, hematology (CBC, differential), serum chemistry (ALT, AST, BUN, creatinine), and histopathology of major organs (liver, kidney, spleen, bone marrow, gastrointestinal tract).
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| References | |
| Additional Infomation |
aStAx-35R TFA is a stapled peptide with the sequence Ac‑RRWPR‑SS‑ILD‑SS‑HVRRWR‑NH2. The peptide is stabilized by hydrocarbon staples that maintain its alpha‑helical conformation, enhancing cell permeability and proteolytic stability. The TFA salt form improves solubility. It was described in Grossmann TN, et al. Proc Natl Acad Sci U S A. 2012;109(44):17942‑7.
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| Molecular Formula |
C111H178N40O20.XC2HF3O2
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| Molecular Weight |
2392.86 (free base)
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| Appearance |
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, 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
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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.) |
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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