| 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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| 500mg |
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| 1g |
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Purity: ≥98%
MSAB is a novel and potent inhibitor of Wnt/β-catenin signaling with anticancer activity. It acts by binding to β-catenin, promoting its degradation, and specifically downregulating Wnt/β-catenin target genes. The Wnt/β-catenin signaling pathway plays a major role in tissue homeostasis, and its dysregulation can lead to various human diseases. Aberrant activation of β-catenin is oncogenic and is a critical driver in the development and progression of human cancers.
| ln Vitro |
MSAB (2-10 μM) specifically lowers Wnt-dependent cells' survival while having minimal effect on Wnt-independent cells and healthy human cells [1]. T cell factor (TCF) luciferase reporter activity in HCT116 cells is inhibited by MSAB (0.01-10 μM; 20 hours) [1]. In HEK293T cells, Wnt3a-induced elevations in TOP-Luc activation and active β-catenin levels are inhibited by MSAB (20 hours) [1]. In HCT116 cells, MSAB (0.5-10 μM; 20 hours) lowers the levels of endogenous Wnt target gene mRNA and protein [1]. Protease-dependent MSAB (5 μM) stimulates β-catenin degradation in HCT116 cells for 16 hours [1].
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| ln Vivo |
In a mouse xenograft model, MSAB (10–20 mg/kg; daily intraperitoneal injection for 2 weeks) reduces the formation of tumors in Wnt-dependent cancer cells [1]. In MMTV-Wnt1 transgenic mice, MSAB (10–20 mg/kg; intraperitoneally given twice daily for two weeks) suppresses tumor growth [1].
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| Animal Protocol |
Animal/Disease Models: Athymic nude mice (5-6 weeks) injected with HCT116, HT115, H23 or H460 cells [1]
Doses: 10, 20 mg/kg Route of Administration: Daily intraperitoneal (ip) injection for 2 weeks Experimental Results: Various mice The size and weight are diminished in Wnt-dependent manner in HCT116, HT115, and H23 tumor types. |
| References |
[1]. Hwang SY, et, al. Direct Targeting of β-Catenin by a Small Molecule Stimulates Proteasomal Degradation and Suppresses Oncogenic Wnt/β-Catenin Signaling. Cell Rep. 2016 Jun 28;16(1):28-36.
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| Molecular Formula |
C15H15NO4S
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|---|---|
| Molecular Weight |
305.3489
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| CAS # |
173436-66-3
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| SMILES |
CC1C=CC(S(NC2=CC=CC(C(OC)=O)=C2)(=O)=O)=CC=1
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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 : ~250 mg/mL (~818.73 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.81 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 20.8 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: ≥ 2.08 mg/mL (6.81 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 | 3.2749 mL | 16.3747 mL | 32.7493 mL | |
| 5 mM | 0.6550 mL | 3.2749 mL | 6.5499 mL | |
| 10 mM | 0.3275 mL | 1.6375 mL | 3.2749 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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