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Purity: ≥98%
Spautin-1 is a specific autophagy inhibitor which inhibits the deubiquitinating activity of USP10 and USP13 with IC50 of ∼0.6-0.7 μM. It can also enhances IM(imatinib-induced)-induced CML (Chronic myelogenous leukemia) cell apoptosis by reducing the expression of the anti-apoptotic proteins Mcl-1 and Bcl-2 and enhances IM-induced apoptosis by inactivating PI3K/AKT and activating downstream GSK3β, which can lead to downregulation of Mcl-1 and Bcl-2. Spautin-1 represents a promising agent to improve the efficacy of IM in the treatment of CML patients.
| ln Vitro |
Spautin-1 decreases the expression of the anti-apoptotic proteins Mcl-1 and Bcl-2, which increases the apoptosis that imatinib mesylate (IM) induces in CmL cells. Spautin-1's pro-apoptotic action is associated with GSK3β activation, a significant PI3K/AKT downstream effector. In the CmL cell line K562, spautin-1 increases IM-induced cytotoxicity by lowering the IC50 from 1 μM to 0.5 μM [1]. Reduced autophagy inhibition is linked to the mechanism by which spautin-1 treats acute pancreatitis [2].
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| ln Vivo |
Spautin-1 ameliorates the pathophysiology of acute pancreatitis produced by cerulein or L-arginine. Spautin-1 pretreatment significantly reduced the increase in serum amylase and lipase levels, indicating trypsin activity. The increase in serum TNFα levels generated by cerulein was reduced in the presence of spautin-1. Spautin-1 medication can alleviate inflammatory damage such as edema, degeneration, coagulative necrosis and inflammatory cell infiltration produced by cerulein [2].
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| References |
[1]. Shao S, et al. Spautin-1, a novel autophagy inhibitor, enhances imatinib-induced apoptosis in chronic myeloid leukemia. Int J Oncol. 2014 May;44(5):1661-1668.
[2]. Xiao J, et al. Spautin-1 Ameliorates Acute Pancreatitis via Inhibiting Impaired Autophagy and Alleviating Calcium Overload. Mol Med. 2016 Aug 18;22 |
| Molecular Formula |
C15H11F2N3
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| Molecular Weight |
271.26
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| CAS # |
1262888-28-7
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| SMILES |
FC1=CC=C(CNC2=C3C=C(F)C=CC3=NC=N2)C=C1
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.22 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 (9.22 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 | 3.6865 mL | 18.4325 mL | 36.8650 mL | |
| 5 mM | 0.7373 mL | 3.6865 mL | 7.3730 mL | |
| 10 mM | 0.3687 mL | 1.8433 mL | 3.6865 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.
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Spautin-1 inhibits IM-induced autophagy in K562 cells.Int J Oncol.2014 May;44(5):1661-8.
Spautin-1 promotes IM-induced apoptosis in K562 cells.Int J Oncol.2014 May;44(5):1661-8. |
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