| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
SNX0723 targets Hsp90 (heat shock protein 90), a molecular chaperone involved in the folding, stabilization, and function of numerous client proteins involved in cell proliferation, survival, and oncogenesis. The compound binds to Hsp90 with high affinity: Ki = 4.4 nM for human Hsp90 (HsHsp90) and Ki = 47 nM for Plasmodium falciparum Hsp90 (PfHsp90). By inhibiting Hsp90, SNX0723 destabilizes its client proteins, leading to disruption of multiple signaling pathways. The compound also inhibits alpha-synuclein oligomerization (EC50 = 48 nM), suggesting potential for neurodegenerative disease research.
|
|---|---|
| ln Vitro |
In vitro studies demonstrate that SNX0723 is a potent Hsp90 inhibitor with an IC50 of 14 nM. The compound shows high binding affinity for HsHsp90 (Ki = 4.4 nM) and PfHsp90 (Ki = 47 nM). SNX0723 inhibits alpha-synuclein oligomerization with an EC50 of 48 nM. The compound has anti-Plasmodium activity, inhibiting liver-stage P. berghei ANKA parasites with an EC50 of 3.3 μM. SNX0723 exhibits antitumor activity in vitro and can rescue alpha-synuclein-induced toxicity. The compound's brain permeability makes it valuable for CNS research.
|
| ln Vivo |
In vivo studies show that SNX0723 is orally active and brain-permeable. The compound's ability to inhibit Hsp90 and alpha-synuclein oligomerization suggests potential for neurodegenerative disease research. The anti-Plasmodium activity indicates potential for malaria research. The compound's antitumor activity supports further investigation in cancer models. Further in vivo studies are warranted to fully characterize the compound's efficacy in various disease models.
|
| Enzyme Assay |
The in vitro Hsp90 binding assay for SNX0723 involves measuring Hsp90 binding affinity using surface plasmon resonance (SPR) or fluorescence polarization. Recombinant Hsp90 is immobilized on a sensor chip or labeled with a fluorescent probe. Varying concentrations of SNX0723 (0.01 nM-10 μM) are added and binding affinity is measured. Ki values are calculated from competition binding experiments. Hsp90 ATPase activity is measured using a coupled enzyme assay or malachite green phosphate detection. Alpha-synuclein oligomerization is assessed by SDS-PAGE, size exclusion chromatography, or Thioflavin T fluorescence. Anti-Plasmodium activity is assessed by measuring parasite growth.
|
| Cell Assay |
In vitro cellular assays for SNX0723 typically use cancer cell lines, neuronal cells, or Plasmodium-infected cells. Cells are cultured in appropriate media and treated with the compound at concentrations of 0.1 nM-10 μM for 24-72 hours. Hsp90 client protein levels are measured by Western blot (e.g., HER2, Akt, Raf-1). Cell viability is assessed using MTT or CCK-8 assays. Apoptosis is evaluated using caspase-3/7 activity assays and Annexin V staining. Alpha-synuclein oligomerization is assessed in neuronal cell models. Anti-malarial activity is assessed in Plasmodium-infected cells.
|
| Animal Protocol |
In vivo animal studies for SNX0723 would typically involve mouse models of cancer, neurodegeneration, or malaria. Mice are treated with the compound via oral gavage at doses of 1-50 mg/kg daily or on a scheduled basis for 2-4 weeks. Tumor volume is measured regularly and tumor weight is determined at necropsy. For neurodegeneration studies, alpha-synuclein transgenic mice are used and behavioral tests and histology are performed. For malaria studies, Plasmodium-infected mice are treated and parasitemia is measured. Hsp90 inhibition in tissues is confirmed by measuring client protein levels.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of SNX0723 indicate good oral bioavailability and brain permeability. The compound has a molecular weight of approximately 400 and is a small molecule. It is soluble in DMSO and other organic solvents. The compound should be stored at -20°C for long-term preservation. After oral administration, the compound reaches systemic circulation and distributes to tissues including the brain. The duration of Hsp90 inhibition is consistent with the compound's half-life.
|
| Toxicity/Toxicokinetics |
Toxicological data for SNX0723 is not extensively reported. As an Hsp90 inhibitor, the compound may affect multiple cellular pathways and have potential toxicity. The compound is for research use only and not for human therapeutic applications. Standard safety precautions should be followed when handling. For detailed toxicity information, specialized toxicological studies would need to be performed.
|
| References | |
| Additional Infomation |
SNX0723 (SNX-0723) is a research-grade compound with CAS number 1073969-18-2. It is a selective, brain-permeable, orally active Hsp90 inhibitor (IC50 = 14 nM). It binds HsHsp90 (Ki = 4.4 nM) and PfHsp90 (Ki = 47 nM) with high affinity. It inhibits alpha-synuclein oligomerization (EC50 = 48 nM) and has anti-Plasmodium activity. It exhibits antitumor activity. This compound has not advanced to clinical trials and is not FDA-approved. It is strictly for research purposes only.
|
| Molecular Formula |
C22H26FN3O3
|
|---|---|
| Molecular Weight |
399.458549022675
|
| Exact Mass |
399.195
|
| CAS # |
1073969-18-2
|
| PubChem CID |
67495834
|
| Appearance |
Off-white to light yellow solid powder
|
| LogP |
3.2
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
29
|
| Complexity |
657
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
FC1C(C(N)=O)=C(C=C(C=1)N1C=C(C)C2C(CC(C)(C)CC1=2)=O)N[C@@H]1COCC1
|
| InChi Key |
GAGDTKJJVCLACJ-ZDUSSCGKSA-N
|
| InChi Code |
InChI=1S/C22H26FN3O3/c1-12-10-26(17-8-22(2,3)9-18(27)19(12)17)14-6-15(23)20(21(24)28)16(7-14)25-13-4-5-29-11-13/h6-7,10,13,25H,4-5,8-9,11H2,1-3H3,(H2,24,28)/t13-/m0/s1
|
| Chemical Name |
2-fluoro-6-[[(3S)-oxolan-3-yl]amino]-4-(3,6,6-trimethyl-4-oxo-5,7-dihydroindol-1-yl)benzamide
|
| Synonyms |
SNX- 0723; SNX 0723; SNX0723
|
| 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) |
DMSO : ~20.83 mg/mL (~52.15 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.21 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 20.8 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 | 2.5034 mL | 12.5169 mL | 25.0338 mL | |
| 5 mM | 0.5007 mL | 2.5034 mL | 5.0068 mL | |
| 10 mM | 0.2503 mL | 1.2517 mL | 2.5034 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
