| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
STAT3
STAT3 (Signal Transducer and Activator of Transcription 3), specifically the SH2 domain. APTSTAT3-9R binds to STAT3 with high specificity and affinity (Kd ≈ 231 nM), blocking STAT3 phosphorylation and subsequent dimerization, nuclear translocation, and transcriptional activity. |
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| ln Vitro |
In human lung cancer cells (A549), APTSTAT3-9R(7.5, 15, and 30 μmol/L; 6 hours) dramatically lowers STAT3–DNA-binding activity in a dose-dependent manner[1]. For two weeks, APTSTAT3-9R (30 μM) strongly inhibits the growth and viability of cancer cells, as well as the development of new colonies. IC50 values for APTSTAT3-9R in A549, B16F1, and HepG2 cells range from 10 to 20 μM [1]. The selectivity of the aptide is indicated by the efficient inhibition of STAT3 phosphorylation by APTSTAT3-9R (7.5, 15, and 30 μmol /L; 6 hours), while leaving AKT phosphorylation unaffected.
In various cancer cell lines (B16F1 melanoma, etc.), APTSTAT3-9R (1-10 uM) blocks STAT3 phosphorylation (p-STAT3) and reduces expression of STAT3 target genes including cyclin D1, Bcl-xL, and survivin. It suppresses cancer cell viability and proliferation. |
| ln Vivo |
In 6-week-old female BALB/c nude mice with A549 cells, APTSTAT3-9R (8 mg/kg in 50 μL; intratumorally given every other day for a total of four injections) reduces tumor growth[1].
Intratumoral injection of APTSTAT3-9R exerts potent antitumor activity in both xenograft and allograft tumor models. It shows efficacy in vemurafenib-resistant melanoma when combined with anti-PD-1 immunotherapy. In pulmonary fibrosis models, APTSTAT3-9R formulated in lipid nanoparticles alleviates disease symptoms. |
| Enzyme Assay |
Surface plasmon resonance (SPR) using immobilized recombinant STAT3 protein is used to measure binding affinity (Kd). For phosphorylation inhibition studies, purified STAT3 protein is incubated with the compound in the presence of active upstream kinases (e.g., JAK2). Phosphorylation is detected by Western blot using anti-p-STAT3 antibodies.
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| Cell Assay |
Cancer cell lines (e.g., B16F1 melanoma, A549 lung cancer) are cultured and treated with APTSTAT3-9R (1-20 uM) for 24-72 hours. Cell viability is assessed by MTT or CellTiter-Glo. STAT3 phosphorylation and target gene expression (cyclin D1, survivin, Bcl-xL) are analyzed by Western blot and qPCR.
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| Animal Protocol |
In mouse xenograft models (e.g., B16F1 melanoma), APTSTAT3-9R is administered via intratumoral injection (dose typically 5-20 mg/kg) daily or every other day. Tumor volume is measured every 2-3 days. Tumor tissue is harvested for analysis of p-STAT3 and downstream targets. For pulmonary fibrosis, intravenous administration of lipid nanoparticle formulations is used.
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| ADME/Pharmacokinetics |
No detailed PK data. As a 33-amino acid peptide with a nona-arginine sequence (MW ~4948 g/mol), APTSTAT3-9R is expected to have rapid plasma degradation and short half-life without formulation. The 9R motif enables cellular penetration but does not confer oral bioavailability. Formulation in nanoparticles improves in vivo stability.
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| Toxicity/Toxicokinetics |
In preclinical studies, no severe systemic toxicity or organ damage has been reported at therapeutic doses. Formulation in biomimetic lipid nanoparticles shows negligible systemic cytotoxicity. APTSTAT3-9R is non-cytotoxic to normal cells at concentrations that inhibit cancer cell growth.
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| References | |
| Additional Infomation |
APTSTAT3-9R is a research-grade peptide, not FDA-approved. It was identified through phage display of an "aptide" library. The aptide sequence binds STAT3 with high specificity. It has demonstrated preclinical proof-of-concept in cancer and fibrosis models. Strictly for research use.
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| Molecular Formula |
C223H330N80O51
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| Molecular Weight |
4947.51
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 0.2021 mL | 1.0106 mL | 2.0212 mL | |
| 5 mM | 0.0404 mL | 0.2021 mL | 0.4042 mL | |
| 10 mM | 0.0202 mL | 0.1011 mL | 0.2021 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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