| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| ln Vitro |
By strengthening the β-catenin complex disruptor that activates GSK3β, KYA1797K directly attaches to the regulator of the G protein signaling domain of axin, starting the control of β-catenin and Ras. The growth of APC and KRAS CRC is successfully inhibited by KYA1797K. It also promotes the formation of the β-catenin destruction complex and activates GSK3β, which phosphorylates β-catenin and K-Ras at S33/S37/T41 and T144/T148. β-catenin and Ras are degraded by KYA1797K in SW480, LoVo, DLD1, and HCT15 cells in a dose-dependent manner. In DLD1 cells expressing WT β-catenin or WT K-Ras, KYA1797K destabilizes both Ras and β-catenin [1].
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| ln Vivo |
Both in the Apcmin/+/KrasG12DLA2 mouse model and in tagged APC and K-Ras mutant CRC cell xenograft mice, KYA1797K effectively decreases tumor size. Tumor weight and volume were 70% decreased by KYA1797K (25 mg/kg). Treatment causes a considerable decrease in Wnt/β-catenin and Ras signaling targets, as well as β-catenin and Ras protein levels [1].
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| References |
[1]. Cha PH, et al. Small-molecule binding of the axin RGS domain promotes β-catenin and Ras degradation. Nat Chem Biol. 2016 Aug;12(8):593-600
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| Molecular Formula |
C17H11KN2O6S2
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|---|---|
| Molecular Weight |
442.5013
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| Exact Mass |
441.9696
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| CAS # |
1956356-56-1
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| Related CAS # |
851304-36-4 (free acid);1956356-56-1;
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| SMILES |
InChI=1S/C17H12N2O6S2.K/c20-15(21)7-8-18-16(22)14(27-17(18)26)9-12-5-6-13(25-12)10-1-3-11(4-2-10)19(23)24/h1-6,9H,7-8H2,(H,20,21)/q+1/p-1/b14-9-
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| InChi Key |
(5Z)-5-[[5-(4-Nitrophenyl)-2-furanyl]methylene]-4-oxo-2-thioxo-3-thiazolidinepropanoic acid potassium salt
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| InChi Code |
PHUNRLYHXGMOLG-WQRRWHLMSA-M
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| Chemical Name |
KYA1797K
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| 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)
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| Solubility (In Vitro) |
DMSO : ~6 mg/mL (~13.56 mM)
H2O : ~1 mg/mL (~2.26 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 1 mg/mL (2.26 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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: 1 mg/mL (2.26 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2599 mL | 11.2994 mL | 22.5989 mL | |
| 5 mM | 0.4520 mL | 2.2599 mL | 4.5198 mL | |
| 10 mM | 0.2260 mL | 1.1299 mL | 2.2599 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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