| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
|
Purity: ≥98%
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.
| 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 | |
| Additional Infomation |
N-(3-methylphenyl)-4-pyridin-4-yl-2-thiazolamine is a substituted aniline.
|
| Molecular Formula |
C15H13N3S
|
|
|---|---|---|
| Molecular Weight |
267.35
|
|
| Exact Mass |
267.083
|
|
| CAS # |
315702-99-9
|
|
| Related CAS # |
|
|
| 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 |
|
|
| 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)
|
| Solubility (In Vitro) |
|
|||
|---|---|---|---|---|
| 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. View More
Solubility in Formulation 3: 1% DMSO +30% polyethylene glycol+1% Tween 80 : 7 mg/mL |
| 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.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(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.
 STF-62247 induces cytotoxicity and reduces tumor growth in VHL-deficient cells in HIF-independent manner.Cancer Cell. 2008 Jul 8; 14(1): 90. |
|---|
 Presence of autophagic vacuoles with STF-62247 in RCCs.Cancer Cell. 2008 Jul 8; 14(1): 90. |
 Atg5 is involved in autophagic cell death of STF-62247.Cancer Cell. 2008 Jul 8; 14(1): 90. |
 Golgi trafficking and PI3K involved in STF-62247 signaling pathway and acidification of vesicle after STF-62247 treatment.Cancer Cell. 2008 Jul 8; 14(1): 90. |
|---|
 Evaluation of autophagy in RCC treated with analogs of the STF-62247.Cancer Cell. 2008 Jul 8; 14(1): 90. |
 Golgi trafficking proteins are sensitive and a target for the STF-62247.Cancer Cell. 2008 Jul 8; 14(1): 90. |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA