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: Cat #: V1272 CAS #: 1456632-41-9 Purity ≥ 98%
Description: 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.
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| Molecular Weight (MW) | 625.61 |
|---|---|
| Molecular Formula | C29H28F5N3O5S |
| CAS No. | 1456632-41-9 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 100 mg/mL (159.8 mM) |
| Water: <1 mg/mL | |
| Ethanol: 100 mg/mL (159.8 mM) | |
| Synonyms | SH5 07; SH507; SH5-07 |
| Protocol | In Vitro | In vitro activity: SH5-07 is a hydroxamic acid analog of BP-1-102. 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. It induces antitumor cell effects against malignant cells harboring constitutively-active Stat3. SH5-07 inhibits the expression of known Stat3-regulated genes. Bcl-2, Bcl-xL, c-Myc, Survivin, Cyclin D1 and Mcl-1 expression is reduced in response to 24 h, 5 μM SH5-07 treatment. Kinase Assay: SH5-07 is a hydroxamic acid based Stat3 inhibitor with an IC50 of 3.9±0.6 μM in in vitro assay. Cell Assay: Cells are treated with 0-8 μM agent for 24-48 h. For cell cycle profile analysis, cells are harvested and fixed with 70% ice-cold ethanol and stained with propidium iodide (PI). For apoptosis analysis, cells are collected and stained with FITC-Annexin V using Apoptosis Detection Kit. Both the DNA content of cells and the Annexin V-positive cells are analyzed by FACScan flow cytometer. Cell cycle phase distribution is analyzed using the Cell-Fit program. Data acquisition is gated to exclude cell doublets |
|---|---|---|
| In Vivo | Tail vein injection or oral gavage delivery of SH5-07 or SH4-54 inhibits growth of 90-150 mm3 established subcutaneous mouse xenografts of human glioma (U251MG) and breast (MDA-MB-231) tumors that harbor aberrantly-active Stat3, associated with decreased c-Myc, Mcl-1 and Cyclin D1 expression. No significant changes in body weights, blood cell counts, or the gross anatomy of organs, or obvious signs of toxicity are observed. | |
| Animal model | Mouse xenografts with human glioma (U251MG) and breast (MDA-MB-231) tumors |
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 1.5984 mL | 7.9922 mL | 15.9844 mL | 31.9688 mL |
| 5mM | 0.3197 mL | 1.5984 mL | 3.1969 mL | 6.3938 mL |
| 10mM | 0.1598 mL | 0.7992 mL | 1.5984 mL | 3.1969 mL |
| 20mM | 0.0799 mL | 0.3996 mL | 0.7992 mL | 1.5984 mL |
This equation is commonly abbreviated as: C1 V1 = C2 V2
- (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.