| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| ln Vitro |
HGC27, AGS, and MKN45 cell growth is considerably inhibited by M435-1279 (0, 2, 4, 8, 16, and 31 μM; 48 hours) [1]. M435-1279 (0, 4, 8, 12, 16, and 20 μM) reduces the viability of cells in GES-1, HGC27, MKN45, and AGS cells, respectively, with IC50 values of 16.8, 11.88, 6.93, and 7.76 μM [1]. M435-1279 (31 nM to 500 μM) binds to UBE2T with a KD value of 50.5 μM. In 48 hours, M435-1279 (11.88 μM) prevents excessive activation of Wnt/β-catenin staining and RACK1 ubiquitination [1].
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|---|---|
| ln Vivo |
M435-1279 (5 mg/kg/day; intratumoral injection for 18 days) suppresses tumor growth [1]. M435-1279 causes increased RACK1 protein expression and direct Ki-67 and β-catenin protein expression in intratumoral tumors
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| Cell Assay |
Cell viability assay [1]
Cell Types: HGC27, AGS and MKN45 Cell Tested Concentrations: 0, 4, 8, 12, 16, 20 μM Incubation Duration: Experimental Results: Inhibited cell viability, IC50 was 16.8, 11.88, 6.93, 7.76 μM respectively. in GES-1, HGC27, MKN45, and AGS cells. |
| Animal Protocol |
Animal/Disease Models: BALB/C nude mouse CDX model (MKN45 tumor size: 75–100 mm3) [1 ]
Doses: 5 mg/kg/day Route of Administration: Intratumoral injection for 18 days Experimental Results: Slowed tumor growth. Induced higher RACK1 protein expression and diminished Ki-67 and β-catenin protein expression in intratumoral tumors. |
| References |
| Molecular Formula |
C18H17N3O5S2
|
|---|---|
| Molecular Weight |
419.4747
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| Exact Mass |
419.06
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| CAS # |
1359431-16-5
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| PubChem CID |
54733438
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| Appearance |
White to off-white solid powder
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| LogP |
2.1
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
28
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| Complexity |
799
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S1C2=C(C(=C(C(N([H])C3C([H])=C([H])C(=C([H])C=3[H])S(N([H])[H])(=O)=O)=O)C(N2[H])=O)O[H])C2=C1C([H])([H])C([H])([H])C([H])([H])C2([H])[H]
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| InChi Key |
MVQJFYRZMPKNIV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H17N3O5S2/c19-28(25,26)10-7-5-9(6-8-10)20-16(23)14-15(22)13-11-3-1-2-4-12(11)27-18(13)21-17(14)24/h5-8H,1-4H2,(H,20,23)(H2,19,25,26)(H2,21,22,24)
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| Chemical Name |
4-hydroxy-2-oxo-N-(4-sulfamoylphenyl)-5,6,7,8-tetrahydro-1H-[1]benzothiolo[2,3-b]pyridine-3-carboxamide
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ~50 mg/mL (~119.20 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.96 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 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 | 2.3840 mL | 11.9198 mL | 23.8396 mL | |
| 5 mM | 0.4768 mL | 2.3840 mL | 4.7679 mL | |
| 10 mM | 0.2384 mL | 1.1920 mL | 2.3840 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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