STF-62247 is a novel potent TGN (trans-Golgi network) inhibitor with IC50 of 0.625μM and 16μM in RCC4 and RCC4/VHL cells, respectively. It shows selective toxicity and growth inhibition of renal cells lacking VHL (von Hippel-Lindau, a tumor suppressor gene), and has 25-fold greater sensitivity observed for cells with VHL deficiency compared to wild-type (VHL+). In vitro study demonstrated that STF-62247 exhibited selectively cytotoxicity and tumor growth inhibitory activity towards 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. In addion, STF-62247 also resulted in cell apoptosis by inducing acidification and increasing autophagy in VHL-deficient cells.

Physicochemical Properties

Molecular Formula	C15H13N3S
Molecular Weight	267.35
Exact Mass	267.083
CAS #	315702-99-9
Related CAS #	315702-99-9
PubChem CID	704473
Appearance	Light yellow to yellow solid powder
Density	1.3±0.1 g/cm3
Boiling Point	444.8±47.0 °C at 760 mmHg
Melting Point	174.66° C
Flash Point	222.8±29.3 °C
Vapour Pressure	0.0±1.1 mmHg at 25°C
Index of Refraction	1.671
LogP	3.16
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	4
Rotatable Bond Count	3
Heavy Atom Count	19
Complexity	281
Defined Atom Stereocenter Count	0
InChi Key	KATNUHQNJGNLPW-UHFFFAOYSA-N
InChi Code	InChI=1S/C15H13N3S/c1-11-3-2-4-13(9-11)17-15-18-14(10-19-15)12-5-7-16-8-6-12/h2-10H,1H3,(H,17,18)
Chemical Name	N-(3-methylphenyl)-4-pyridin-4-yl-1,3-thiazol-2-amine
Synonyms	STF-62247;STF 62247;STF62247
HS Tariff Code	2934.99.9001
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)

Biological Activity

ln Vitro	STF-62247 (0-30 μM) is particularly lethal to VHL-deficient cells relative to their wild-type VHL counterparts in RCC4, RCC4/VHL, SN12C, and SN12C-VHL shRNA cells[1]. Cells treated with STF-62247 accumulated intracytoplasmic vacuoles, which are indicative of autophagous cells. Furthermore, compared to wild-type VHL cells, these vacuoles are bigger in RCC4 and SN12C-VHL shRNA cells that lack VHL[1].
ln Vivo	STF-62247 (2.7-8 mg/kg; intraperitoneal injection; daily; for 9 days) therapy effectively decreases tumor growth of VHL-deficient cells[1].
Animal Protocol	Animal/Disease Models: SCID (severe combined immunodeficient) mouse implanted with SN12C-VHL shRNA cells[1] Doses: 2.7 mg/kg, or 8 mg/kg Route of Administration: intraperitoneal (ip)injection; daily; for 9 days Experimental Results: Dramatically decreased tumor growth of VHL-deficient cells.
References	[1]. A molecule targeting VHL-deficient renal cell carcinoma that induces autophagy. Cancer cell 14, 90-102, doi:10.1016/j.ccr.2008.06.004 (2008).
Additional Infomation	N-(3-methylphenyl)-4-pyridin-4-yl-2-thiazolamine is a substituted aniline.

Solubility Data

Solubility (In Vitro)

DMSO:53 mg/mL (198.2 mM) Water:<1 mg/mL Ethanol:3 mg/mL (11.2 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (9.35 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 (9.35 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 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. Solubility in Formulation 3: 1% DMSO +30% polyethylene glycol+1% Tween 80 : 7 mg/mL  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	3.7404 mL	18.7021 mL	37.4042 mL
	5 mM	0.7481 mL	3.7404 mL	7.4808 mL
	10 mM	0.3740 mL	1.8702 mL	3.7404 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.