| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Targets |
SHP-1 p-STAT3
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| ln Vitro |
Treatment with SC-43 (0-10 μM; 24 hours) enhanced sub-G1 cells and G2-M arrest in HuCCT-1, KKU-100, and CGCCA cells, suggesting that SC-43 promotes specific apoptosis in these cell lines Function[1]. The HuCCT-1, KKU-100, and CGCCA cells treated with SC-43 (0-10 μM) for 24 hours demonstrated a considerable rise in cleaved caspase-3 and PARP levels [1]. By stimulating SH2 domain-containing phosphatase 1 (SHP-1) activity, SC-43 causes p-STAT3 to be downregulated, which in turn causes cyclin B1 and Cdc2 to be downstream. By directly attaching to N-SH2 and removing its own inhibition, SC-43 increases SHP-1 activity [1].
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| ln Vivo |
Treatment with SC-43 (10-30 mg/kg; gavage; daily; for 23 days; male NCr athymic nude mice) inhibited the formation of xenograft tumors, decreased p-STAT3, and elevated SHP-1 activity[1].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: HuCCT-1, KKU-100, and CGCCA cells Tested Tested Concentrations: 0 μM, 0.25 μM, 0.5 μM, 0.75 μM, 1 μM, 2.5 μM, 5 μM, 10 μM Incubation Duration: 24 hrs (hours) , 48 hrs (hours), 72 hrs (hours) Experimental Results: Revealed the anti-proliferative effects in CCA cell lines in a dose-dependent manner after treating 24, 48 and 72 hrs (hours) respectively. Cell Cycle Analysis[1] Cell Types: HuCCT-1, KKU-100 , and CGCCA cells Tested Tested Concentrations: 0 μM, 1 μM, 2.5 μM, 5 μM, 10 μM Incubation Duration: 24 hrs (hours) Experimental Results: demonstrated increased sub-G1 cells and G2-M arrest. Western Blot Analysis[1] Cell Types: HuCCT- 1, KKU-100, and CGCCA cells Tested Tested Concentrations: 0 μM, 1 μM, 2.5 μM, 5 μM, 10 μM Incubation Duration: 24 hrs (hours) Experimental Results: Demonstrated significant increase in cleaved caspase-3 and PARP level. |
| Animal Protocol |
Animal/Disease Models: Male NCr athymic nude mice (5-7 weeks of age) injected with HuCCT-1 cells[1]
Doses: 10 mg/kg or 30 mg/kg Route of Administration: Oral gavage; daily; for 23 days Experimental Results: demonstrated xenograft tumor growth inhibition, p-STAT3 reduction and SHP-1 activity elevation. |
| References |
[1]. Ming-Hung Hu, et al. Targeting SHP-1-STAT3 signaling: A promising therapeutic approach for the treatment of cholangiocarcinoma. Oncotarget. 2017 May 10;8(39):65077-65089.
[2]. Tung-Hung Su, et al. Src-homology protein tyrosine phosphatase-1 agonist, SC-43, reduces liver fibrosis. Sci Rep. 2017 May 11;7(1):1728. |
| Molecular Formula |
C21H13CLF3N3O2
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|---|---|
| Molecular Weight |
431.80
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| CAS # |
1400989-25-4
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| SMILES |
C(F)(F)(C1C=C(C=CC=1Cl)NC(=O)NC1=CC(=CC=C1)OC1=CC=C(C=C1)C#N)F
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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) |
DMSO: 250 mg/mL (578.97 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (4.82 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.82 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3159 mL | 11.5794 mL | 23.1589 mL | |
| 5 mM | 0.4632 mL | 2.3159 mL | 4.6318 mL | |
| 10 mM | 0.2316 mL | 1.1579 mL | 2.3159 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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