| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| ln Vitro |
SRSF1-IN-1 (STP2) (72 h) effectively inhibited the proliferation of HepG2, MCF7, HCT116, U251, HGC27, AGS, BGC823, SGC7901, A549 and B16F10 cell lines, with IC50 values of 0.63, 1.79, 0.52, 2.43, 0.62, 1.03, 1.3, 1.88, >10 and 1.03 μM, respectively. Compared with normal human LO2 hepatocytes, it also showed selective toxicity to tumor cells[1]. SRSF1-IN-1 (0.5-2 μM; 48 h) dose-dependently induced apoptosis in HGC27 and AGS gastric cancer cells, increased the proportion of apoptotic cells, downregulated the anti-apoptotic protein Bcl-xl, and upregulated cleaved PARP and cleaved caspase 3[1]. SRSF1-IN-1 (0.5-2 μM; 24 hours) can arrest HGC27 and AGS gastric cancer cells in the S phase, accompanied by upregulation of P21 protein expression and downregulation of CyclinE2 protein expression [1]. SRSF1-IN-1 (0.5-2 μM; 24 hours) can dose-dependently downregulate the expression of SRSF1 mRNA and protein in HGC27 and AGS gastric cancer cells; at a concentration of 2 μM, SRSF1-IN-1 can inhibit the RNA splicing pathway in HGC27 cells and upregulate autophagy-related genes [1]. SRSF1-IN-1 (0.5-2 μM; 48 hours) can induce autophagy in HGC27 and AGS gastric cancer cells; when combined with 2 μM chloroquine (CQ) for 24 hours, it can also enhance the formation of LC3B spots [1].
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| ln Vivo |
STP2 (25-100 mg/kg; intraperitoneal injection; once daily; for 15 days) showed dose-dependent in vivo antitumor activity in a mouse HGC27 gastric cancer xenograft model, inhibiting tumor growth by 63.68% and 82.66% at doses of 25 mg/kg and 100 mg/kg, respectively, without causing significant weight loss [1]. STP2 (1 g/kg; intraperitoneal injection; single dose) was well tolerated in male ICR mice, with a 100% survival rate, gradual weight gain, and no significant liver histopathological abnormalities were observed within 7 days [1].
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| Cell Assay |
Apoptosis analysis [1] Cell Types: HGC27, AGS Test concentrations: 0.5 μM, 1 μM, 2 μM
Incubation Duration: 48 hours Experimental Results: Apoptosis was induced in a dose-dependent manner: In HGC27 cells, the apoptosis rate increased from 8.15% to 47.8%; in AGS cells, the apoptosis rate increased from 7.59% to 63.3%. In both cell lines, the expression of the anti-apoptotic protein Bcl-xl was decreased, while the expression of cleaved-PARP and cleaved-caspase 3 was increased. Cell cycle analysis [1] Cell Types: HGC27, AGS Tested Concentrations: 0.5 μM, 1 μM, 2 μM Incubation Duration: 24 hours Experimental Results: Increased proportion of S phase cells: The proportion of S phase cells in HGC27 cells increased from 50.19% to 75.34%; the proportion of S phase cells in AGS cells increased from 32.86% to 52.16%. P21 protein expression increased and CyclinE2 protein expression decreased in both cell lines, and there was no obvious dose dependence. Real-time quantitative PCR[1] Cell Types: HGC27, AGS Tested Concentrations: 0.5 μM, 1 μM, 2 μM Incubation Duration: 24 hours Experimental Results: After treating HGC27 cells with 2 μM, the RNA splicing pathway was significantly downregulated, SRSF1 mRNA expression decreased, and autophagy-related genes (BECN1, MAP1LC3B, MAP1LC3B2) expression increased. SRSF1 mRNA levels were dose-dependently reduced in both HGC27 and AGS cells. SRSF1 protein levels were also dose-dependently reduced in both cell lines.
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| Animal Protocol |
Animal/Disease Models:BALB/c nude mice (male, 6 weeks old, HGC27 cell xenograft model of gastric cancer) [1]
Doses: 25 mg/kg; 100 mg/kg Route of Administration: Intraperitoneal injection; once daily for 15 days Experimental Results: Tumor growth was inhibited in a dose-dependent manner. The tumor growth inhibition rate (TGI) was 63.68% in the 25 mg/kg dose group and 82.66% in the 100 mg/kg dose group. No significant weight loss was observed during the 15-day treatment period. The P62 protein level was decreased and the LC3B protein level (autophagy marker) was increased in the HGC27 tumor tissue of the treated mice. Animal/Disease Models:ICR (male) [1] Doses: 1 g/kg Route of Administration: Intraperitoneal injection; single dose Experimental Results: The survival rate of mice reached 100% during the 7-day observation period. The weight of mice gradually increased within 7 days. No obvious abnormal changes in the morphology of hepatocytes were observed in the liver tissue, and no phenomena such as increased cell volume, empty/bright cytoplasm or blurred cell boundaries were observed. |
| References |
| Molecular Formula |
C20H24O5S
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|---|---|
| Molecular Weight |
376.47
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| Appearance |
Typically exists as solids at room temperature
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| SMILES |
S=C1OCC2=C1CC[C@@]3(C)[C@@]2([H])C[C@H](O4)[C@]54[C@@]3(O6)[C@@H]6[C@H]7[C@@](O7)(C(C)C)[C@H]5O
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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 |
| 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 | 2.6563 mL | 13.2813 mL | 26.5625 mL | |
| 5 mM | 0.5313 mL | 2.6563 mL | 5.3125 mL | |
| 10 mM | 0.2656 mL | 1.3281 mL | 2.6563 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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