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SC99 is a novel and potent inhibitor of JAK2-STAT3 activation with anticancer activity. It exhibits no effects on other transcription factors such as NF-κB, and kinases such as AKT, ERK, and c-Src.
| ln Vitro |
For a duration of 72 hours, SC99 (10 or 30 μM) causes MM cell death [1]. While SC99 (10 μM; 24 h) decreased p-STAT3 levels, it had no effect on the expression of STAT3 overall. At concentrations up to 20 μM, SC99 [1] does not affect the phosphorylation levels of AKT, ERK, mTOR, or c-Src, but it does suppress JAK2 phosphorylation in a concentration-dependent manner. In a concentration-dependent manner, SC99 (1.25, 2.5, and 5 μM; 10 min pretreatment) suppresses the phosphorylation of STAT3 caused by thrombin (0.02 U/mL) and collagen (2 μg/mL) [2]. In OPM2 cells, IL-6 (50 ng/ml; 20 minutes)-induced STAT3 nuclear translocation is inhibited by SC99 two hours prior to treatment [3].
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| ln Vivo |
SC99 (30 mg/kg; oral; daily; for 14 or 28 consecutive days) slows myeloma tumor growth in xenograft animal models [1]. SC99 (5, 10, 15 mM, 15 μL; ICV) potently suppresses the phosphorylation of JAK2 and STAT3 in the middle cerebral artery occlusion-reperfusion (MCAO/R) model (adult male SD rats; 250-300 g) impact. SC99 can alleviate neuronal apoptosis and degeneration, neurobehavioral abnormalities, inflammatory reactions, and brain edema [3].
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| Cell Assay |
Apoptosis analysis[1]
Cell Types: Six multiple myeloma (MM) cell lines (LP1, JJN3, RPMI-8226, U266, OPM2, and OCI-MY5) Tested Concentrations: 10 or 30 μM Incubation Duration: 72 hrs (hours) Experimental Results: Induces MM cell death. Apoptosis analysis[1] Cell Types: MM cell line[1] Tested Concentrations: 10 μM Incubation Duration: 24 hrs (hours) Experimental Results: diminished p-STAT3 levels but had no effect on total STAT3 expression in all cell lines examined. |
| Animal Protocol |
Animal/Disease Models: Nude mice with human MM cells OPM2 or JJN3 [1]
Doses: 30 mg/kg Route of Administration: Oral; Daily; 14 or 28 days Experimental Results: Delayed myeloma tumor growth in xenograft mouse model, Inhibited tumor growth by more than 40% within 14 days in the OPM2 model. |
| References |
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| Molecular Formula |
C15H8CL2FN3O
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|---|---|
| Molecular Weight |
336.15
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| Exact Mass |
335.002
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| CAS # |
882290-02-0
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| PubChem CID |
5896323
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.38±0.1 g/cm3(Predicted)
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| Boiling Point |
459.4±55.0 °C(Predicted)
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| LogP |
6.3
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
22
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| Complexity |
482
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC(=CC=C1C(=O)/C(=N/NC2=CC(=C(C=C2)F)Cl)/C#N)Cl
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| InChi Key |
ZKULFSMYRSFHKE-KGENOOAVSA-N
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| InChi Code |
InChI=1S/C15H8Cl2FN3O/c16-10-3-1-9(2-4-10)15(22)14(8-19)21-20-11-5-6-13(18)12(17)7-11/h1-7,20H/b21-14+
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| Chemical Name |
(1E)-N-(3-chloro-4-fluoroanilino)-2-(4-chlorophenyl)-2-oxoethanimidoyl cyanide
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| Synonyms |
SC 99 SC-99 SC99
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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 : ~83.33 mg/mL (~247.90 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (6.19 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 (6.19 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9749 mL | 14.8743 mL | 29.7486 mL | |
| 5 mM | 0.5950 mL | 2.9749 mL | 5.9497 mL | |
| 10 mM | 0.2975 mL | 1.4874 mL | 2.9749 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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