| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
|
Purity: ≥98%
SH-4-54 (SH 454; SH4-54; SH454; SH-454) is a novel and potent STAT inhibitor with potential antineoplastic activity. It inhibits STAT3/5 with KD values of 300 nM and 464 nM, respectively. SH-4-54 shows potent anti-proliferative activity in vitro against glioblastoma brain cancer stem cells (BTSCs) and effectively suppresses STAT3 phosphorylation and its downstream transcriptional targets at low nanomolar concentrations.
| ln Vitro |
At low nM concentrations, SH-4-54 efficiently inhibits STAT3 phosphorylation and its downstream transcriptional targets while also killing glioblastoma brain cancer stem cells (BTSCs). At therapeutic dosages, SH-4-54 effectively reduces pSTAT3 with nanomolar IC50s, blocking STAT3's downstream targets. It also exhibits no toxicity in human fetal astrocytes and demonstrates exceptional cytotoxicity in human BTSCs[1].
|
||
|---|---|---|---|
| ln Vivo |
In vivo, SH-4-54 inhibits pSTAT3 and demonstrates blood-brain barrier permeability, which together potently regulate the growth of glioma tumors. SH-4-54 reduces pSTAT3 expression in treated mice's tumor cells, highlighting the effectiveness of STAT3 inhibitors in treating BTSCs and confirming their therapeutic efficacy for use in GBM clinical applications. Treatable tumors seem to undergo more apoptosis and less proliferation when exposed to SH-4-54[1].
|
||
| Animal Protocol |
|
||
| References |
| Molecular Formula |
C29H27F5N2O5S
|
|
|---|---|---|
| Molecular Weight |
610.59
|
|
| Exact Mass |
610.156
|
|
| CAS # |
1456632-40-8
|
|
| Related CAS # |
|
|
| PubChem CID |
72188643
|
|
| Appearance |
White to off-white solid powder
|
|
| Density |
1.431±0.06 g/cm3
|
|
| Boiling Point |
717.2±70.0 °C at 760 mmHg
|
|
| Flash Point |
387.5±35.7 °C
|
|
| Vapour Pressure |
0.0±2.4 mmHg at 25°C
|
|
| Index of Refraction |
1.590
|
|
| LogP |
7.64
|
|
| Hydrogen Bond Donor Count |
1
|
|
| Hydrogen Bond Acceptor Count |
11
|
|
| Rotatable Bond Count |
9
|
|
| Heavy Atom Count |
42
|
|
| Complexity |
1010
|
|
| Defined Atom Stereocenter Count |
0
|
|
| InChi Key |
VFPYGNNOSJWBHF-UHFFFAOYSA-N
|
|
| InChi Code |
InChI=1S/C29H27F5N2O5S/c1-35(42(40,41)28-26(33)24(31)23(30)25(32)27(28)34)16-22(37)36(21-13-11-20(12-14-21)29(38)39)15-17-7-9-19(10-8-17)18-5-3-2-4-6-18/h7-14,18H,2-6,15-16H2,1H3,(H,38,39)
|
|
| Chemical Name |
4-(N-(4-cyclohexylbenzyl)-2-((2,3,4,5,6-pentafluoro-N-methylphenyl)sulfonamido)acetamido)benzoic acid
|
|
| 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 (4.09 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 (4.09 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6378 mL | 8.1888 mL | 16.3776 mL | |
| 5 mM | 0.3276 mL | 1.6378 mL | 3.2755 mL | |
| 10 mM | 0.1638 mL | 0.8189 mL | 1.6378 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.
|
|---|
|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
