STF-62247

Catalog No.S1041 Batch:S104103

Technical Data

Formula	C₁₅H₁₃N₃S
Molecular Weight	267.35	CAS No.	315702-99-9
Solubility (25°C)*	In vitro	DMSO	53 mg/mL (198.24 mM)
		Ethanol	3 mg/mL (11.22 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description	STF-62247 is a molecule targeting VHL-deficient renal cell carcinoma that induces autophagy. STF-62247 shows selective toxicity and growth inhibition of renal cells lacking VHL; 25-fold greater sensitivity observed for cells with VHL deficiency compared to wild-type (VHL+).
In vitro	In vitro, STF-62247 shows cytotoxicity and tumor growth inhibitory activity against wild-type VHL and VHL-deficient renal cell carcinoma (RCC) in a HIF-independent manner with IC50 of 16 μM and 0.625 μM, respectively. Moreover, STF-62247 also leads to cell death by increasing acidification and inducing autophagy in VHL-deficient cells. ^[1] STF-62247 specifically induces macroautophagy and enhances the fusion of autophagosome and lysosomes to form autolysosomes by interfering with Golgi-endoplasmic reticulum transport in cells that have lost VHL . ^[2] A recent study shows that induction of autophagy by STF-62247 increases sensitivity of RCC under hypoxic conditions to radiation in a VHL-dependent manner. ^[3]
In vivo	In vivo mouse model, STF-62247 at a dose of 8 mg/kg by intraperitoneal injection significantly reduces tumor growth of VHL-deficient SN12C tumor cells. ^[1]

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines SN12C and RCC4 Concentrations 0 to 40 μM Incubation Time 24 hours Method For cell viability, 100,000 cells are plated in a 12-well plate. The following day, 1.25 μM STF-62247 is added in the presence or absence of 1 mM 3-MA for 24 hours at 37 °C. Cells are trypsinized and counted by trypan blue exclusion. For XTT assays, 5000 RCC4 with and without VHL cells or 2,500 SN12C with and without VHL shRNA cells are plated in 96-well plates. The following day, vehicle (DMSO), STF-62247 is added to media by serial dilution. Four days later, the media is aspirated and XTT solution containing 0.3 mg/ml of XTT in Phenol Red-free media, 20% FCS and 2.65 mg/ml N-methyl dibenzopyrazine methyl sulfate (PMS) is added to the cells and incubated at 37 °C for 1-2 hours. Metabolism of XTT is quantified by measuring the absorbance at 450 nm on a plate reader.
Animal Study:^{^[1]}	Animal Models SN12C, SN12C-VHL shRNA or 786-O cells are injected subcutaneously into the flanks of immune-deficient mice. Dosages ≤8 mg/kg Administration Administered via i.p.

Cell Assay:^{^[1]}

Cell lines
SN12C and RCC4
Concentrations
0 to 40 μM
Incubation Time
24 hours
Method
For cell viability, 100,000 cells are plated in a 12-well plate. The following day, 1.25 μM STF-62247 is added in the presence or absence of 1 mM 3-MA for 24 hours at 37 °C. Cells are trypsinized and counted by trypan blue exclusion. For XTT assays, 5000 RCC4 with and without VHL cells or 2,500 SN12C with and without VHL shRNA cells are plated in 96-well plates. The following day, vehicle (DMSO), STF-62247 is added to media by serial dilution. Four days later, the media is aspirated and XTT solution containing 0.3 mg/ml of XTT in Phenol Red-free media, 20% FCS and 2.65 mg/ml N-methyl dibenzopyrazine methyl sulfate (PMS) is added to the cells and incubated at 37 °C for 1-2 hours. Metabolism of XTT is quantified by measuring the absorbance at 450 nm on a plate reader.

Animal Study:^{^[1]}

Animal Models
SN12C, SN12C-VHL shRNA or 786-O cells are injected subcutaneously into the flanks of immune-deficient mice.
Dosages
≤8 mg/kg
Administration
Administered via i.p.

References

Customer Product Validation

: , , Neuropsychiatr Dis Treat, 2015, 11:2091-9.

Selleck's STF-62247 has been cited by 1 publication

Autophagy dysfunction upregulates beta-amyloid peptides via enhancing the activity of γ-secretase complex [Cai Z, et al. Neuropsychiatr Dis Treat, 2015, 11:2091-9]	PubMed: 26316755

Autophagy dysfunction upregulates beta-amyloid peptides via enhancing the activity of γ-secretase complex [Cai Z, et al. Neuropsychiatr Dis Treat, 2015, 11:2091-9]

PubMed: 26316755

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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