STF-62247

Modify Date: 2025-08-22 18:27:20

STF-62247 Structure
STF-62247 structure
Common Name STF-62247
CAS Number 315702-99-9 Molecular Weight 267.349
Density 1.3±0.1 g/cm3 Boiling Point 444.8±47.0 °C at 760 mmHg
Molecular Formula C15H13N3S Melting Point 174.66° C
MSDS Chinese USA Flash Point 222.8±29.3 °C
Symbol GHS07
GHS07
Signal Word Warning

 Use of STF-62247


STF-62247 is TGN inhibitor with IC50 of 0.625μM and 16μM in RCC4 and RCC4/VHL cells,respectively.It specifically induces autophagic cell death in cells that have lost VHL, an essential mutation in the development of RCC.IC50: 0.625/16μM in RCC4 and RCC4/VHL cells,respectively.[1]In vitro: STF-62247 induces cytotoxicity in VHL-deficient cells in a HIF-independent manner, STF-62247 increases acidification in VHL-deficient cells ,TGN is a target of STF-62247 and a drug-selective pathway synthetically lethal in VHL-deficient cells.[1] Golgi trafficking are required as initial signals in STF-62247-induced autophagy.[2]STF-62247 increases radiosensitivity in a VHL-dependent manner.[3]In vivo: SN12C, SN12C-VHL shRNA, or 786-O cells were implanted subcutaneously into the flanks of immunodeficient mice. The selective cytotoxicity of STF-62247 for the VHL-deficient cells was also demonstrated in 786-O cells compared to their wild-type VHL counterparts by clonogenic assay in vitro. Daily treatment with STF-62247 significantly reduced tumor growth of VHL-deficient cells. This decrease in tumor growth was concentration dependent. Importantly, drug treatment did not have any effect on the growth of SN12C tumor cells that have wild-type VHL. Together,STF-62247 reduces tumor growth in VHL-deficient cells in mice.[1]

 Names

Name N-(3-methylphenyl)-4-pyridin-4-yl-1,3-thiazol-2-amine
Synonym More Synonyms

 STF-62247 Biological Activity

Description STF-62247 is TGN inhibitor with IC50 of 0.625μM and 16μM in RCC4 and RCC4/VHL cells,respectively.It specifically induces autophagic cell death in cells that have lost VHL, an essential mutation in the development of RCC.IC50: 0.625/16μM in RCC4 and RCC4/VHL cells,respectively.[1]In vitro: STF-62247 induces cytotoxicity in VHL-deficient cells in a HIF-independent manner, STF-62247 increases acidification in VHL-deficient cells ,TGN is a target of STF-62247 and a drug-selective pathway synthetically lethal in VHL-deficient cells.[1] Golgi trafficking are required as initial signals in STF-62247-induced autophagy.[2]STF-62247 increases radiosensitivity in a VHL-dependent manner.[3]In vivo: SN12C, SN12C-VHL shRNA, or 786-O cells were implanted subcutaneously into the flanks of immunodeficient mice. The selective cytotoxicity of STF-62247 for the VHL-deficient cells was also demonstrated in 786-O cells compared to their wild-type VHL counterparts by clonogenic assay in vitro. Daily treatment with STF-62247 significantly reduced tumor growth of VHL-deficient cells. This decrease in tumor growth was concentration dependent. Importantly, drug treatment did not have any effect on the growth of SN12C tumor cells that have wild-type VHL. Together,STF-62247 reduces tumor growth in VHL-deficient cells in mice.[1]
Related Catalog
References

[1]. Turcotte, S. et al. 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)

[2]. Chan, D. A. & Giaccia, A. J. Targeting cancer cells by synthetic lethality: autophagy and VHL in cancer therapeutics. Cell cycle 7, 2987-2990, doi:10.4161/cc.7.19.6776 (2008)

[3]. Anbalagan, S. et al. Radiosensitization of renal cell carcinoma in vitro through the induction of autophagy. Radiotherapy and oncology : journal of the European Society for Therapeutic Radiology and Oncology 103, 388-393, doi:10.1016/j.radonc.2012.04.001 (2012

 Chemical & Physical Properties

Density 1.3±0.1 g/cm3
Boiling Point 444.8±47.0 °C at 760 mmHg
Melting Point 174.66° C
Molecular Formula C15H13N3S
Molecular Weight 267.349
Flash Point 222.8±29.3 °C
Exact Mass 267.083008
PSA 66.05000
LogP 3.16
Vapour Pressure 0.0±1.1 mmHg at 25°C
Index of Refraction 1.671
Storage condition -20°C

 Safety Information

Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H302-H319
Precautionary Statements P305 + P351 + P338
Personal Protective Equipment dust mask type N95 (US);Eyeshields;Gloves;type P2 (EN 143) respirator cartridges
RIDADR NONH for all modes of transport

 Synthetic Route

~87%

STF-62247 Structure

STF-62247

CAS#:315702-99-9

Literature: Hay, Michael P.; Turcotte, Sandra; Flanagan, Jack U.; Bonnet, Muriel; Chan, Denise A.; Sutphin, Patrick D.; Nguyen, Phuong; Giaccia, Amato J.; Denny, William A. Journal of Medicinal Chemistry, 2010 , vol. 53, # 2 p. 787 - 797

 Precursor & DownStream

Precursor  2

DownStream  0

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 Synonyms

STF-62247
2-Thiazolamine, N-(3-methylphenyl)-4-(4-pyridinyl)-
N-(3-Methylphenyl)-4-(4-pyridinyl)-1,3-thiazol-2-amine
N-(3-methyl-phenyl)-4-pyridin-4-yl-1,3-thiazol-2-amine
4-(pyridin-4-yl)-N-m-tolylthiazol-2-amine
N-(3-Methylphenyl)-4-(4-pyridinyl)-2-thiazolamine
S1041_Selleck
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