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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
SH5-07 (SH5 07; SH-507; SH5-07), a structural analog of BP-1-102, is a novel, potent and hydroxamic acid-based STAT3 inhibitor with potential antitumor activity. It shows potent anti-proliferative activity in vitro and high in vivo antitumor efficacy against human glioma and breast cancer models. SH5-07 dose-dependently inhibits Stat3 activity with an IC50 of 3.9±0.6 μM in in vitro assay. It preferentially inhibits Stat3: Stat3 DNA-binding activity, ahead of inhibiting Stat1:Stat3 activity, with minimal effects on Stat1:Stat1 activity. SH5-07 binds Stat3, disrupts Stat3 association with growth factor receptor, and thereby inhibits Stat3 phosphorylation.
| ln Vitro |
An analog of BP-1-102 is hydroxamic acid, or SH5-07. In an in vitro assay, Stat3 activity is dose-dependently inhibited by SH5-07, with an IC50 of 3.9±0.6 μM. With negligible effects on Stat1:Stat1 activity, it preferentially inhibits the DNA-binding activity of Stat3:Stat3, prior to inhibiting Stat1:Stat3. By binding to Stat3, SH5-07 prevents Stat3 from attaching to the growth factor receptor, which prevents Stat3 from being phosphorylated. It causes malignant cells with constitutively active Stat3 to exhibit antitumor cell effects. The expression of recognized Stat3-regulated genes is inhibited by SH5 -07. The expression of Bcl-2, Bcl-xL, c-Myc, Survivin, Cyclin D1, and Mcl-1 decreases in response to a 24-hour treatment with 5 μM SH5-07[1].
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| ln Vivo |
The growth of established subcutaneous mouse xenografts of human glioma (U251MG) and breast tumor (MDA-MB-231), which have aberrantly-active Stat3, is inhibited by tail vein injection or oral gavage delivery of SH5-07 or SH4-54. This is related with lower expression of c-Myc, Mcl-1, and Cyclin D1. The tumors measure 90-150 mm3. There are no appreciable alterations in body weights, blood cell counts, gross organ architecture, or overt toxicity[1].
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| References |
[1]. Yue P,et al. Hydroxamic Acid and Benzoic Acid-Based STAT3 Inhibitors Suppress Human Glioma and Breast Cancer Phenotypes In Vitro and In Vivo. Cancer Res. 2016 Feb 1;76(3):652-63
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| Molecular Formula |
C29H28F5N3O5S
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| Molecular Weight |
625.61
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| CAS # |
1456632-41-9
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| Related CAS # |
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| SMILES |
O=C(NO)C1=CC=C(N(CC2=CC=C(C3CCCCC3)C=C2)C(CN(C)S(=O)(C4=C(F)C(F)=C(F)C(F)=C4F)=O)=O)C=C1
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.00 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 25.0 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: ≥ 2.5 mg/mL (4.00 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 25.0 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 | 1.5984 mL | 7.9922 mL | 15.9844 mL | |
| 5 mM | 0.3197 mL | 1.5984 mL | 3.1969 mL | |
| 10 mM | 0.1598 mL | 0.7992 mL | 1.5984 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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