STF-62247

Catalog No.S1041

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+).

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In DMSO USD 90 In stock
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STF-62247 Chemical Structure

STF-62247 Chemical Structure
Molecular Weight: 267.35

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Quality Control & MSDS

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Product Description

Biological Activity

Description 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 byby intraperitoneal injection significantly reduces tumor growth of VHL-deficient SN12C tumor cells. [1]
Features

Protocol(Only for 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.
Formulation STF-62247 is dissolved in DMSO and then diluted in water
Dosages ≤8 mg/kg
Administration Administered via i.p.
Solubility 1% DMSO/30% polyethylene glycol/1% Tween 80, , 7 mg/mL
* 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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesBaboonDogMonkeyRabbitGuinea pigRatHamsterMouse
Weight (kg)121031.80.40.150.080.02
Body Surface Area (m2)0.60.50.240.150.050.0250.020.007
Km factor202012128653
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Turcotte S, et al. Cancer Cell. 2008, 14(1), 90-102.

[2] Chan DA, et al. Cell Cycle. 2008, 7(19), 2987-2990.

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Chemical Information

Download STF-62247 SDF
Molecular Weight (MW) 267.35
Formula

C15H13N3S

CAS No. 315702-99-9
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Synonyms
Solubility (25°C) * In vitro DMSO 53 mg/mL (198 mM)
Water <1 mg/mL (<1 mM)
Ethanol 3 mg/mL (11 mM)
In vivo 1% DMSO/30% polyethylene glycol/1% Tween 80, 7 mg/mL
* <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.
Chemical Name 4-(pyridin-4-yl)-N-m-tolylthiazol-2-amine

Research Area

Tech Support & FAQs

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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