| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| ln Vitro |
The cell viability of HL60, MOLT-4, and CCRF-CEM cells is inhibited by MPT0B392 (B392) (0.001-0.1 μM; 24 and 48 hours) with IC50 values of 0.02 μM, 0.03 μM, and 0.02 μM, in that order [1]. MPT0B392 (0.1 μM; 48 hours) causes HL60 cancer cells to undergo apoptosis [1]. MPT0B392 (0.1 μM, 6-48 hours; 0.01-0.1 μM, 24 and 48 hours) induces cell arrest in the G2/M phase, which is followed by a concentration- and time-dependent accumulation in the subG1 phase [1]. MPT0B392 (0.1 μM; 48 hours) decreases Mcl-1L and increases Bcl-2 and Mcl-1S phosphorylation[1].
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| ln Vivo |
In an in vivo xenograft model, MPT0B392 (oral gavage; 50 mg/kg or 100 mg/kg for 12 or 14 days) has demonstrated comparatively strong antileukemic action [1].
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| Cell Assay |
Cell viability assay [1]
Cell Types: HL60 (acute promyelocytic leukemia), MOLT-4 (acute lymphoblastic leukemia), CCRF-CEM (acute lymphoblastic leukemia) Cell Tested Concentrations: 0.001, 0.003, 0.01, 0.03, 0.1 μM Incubation Duration: 24 48 hrs (hours) Experimental Results: Inhibition of cell viability. Apoptosis analysis[1] Cell Types: HL60 Cell Tested Concentrations: 0.1 μM Incubation Duration: 48 hrs (hours) Experimental Results: Induced apoptosis of cancer cells. Cell cycle analysis[1] Cell Types: HL60 Cell Tested Concentrations: 0.1 μM or 0.01, 0.03, 0.1 μM Incubation Duration: 0.1 μM, 6-48 hrs (hours); 0.01-0.1 μM, 24 and 48 hrs (hours) Experimental Results: Triggered cell arrest at G2/M phase and then accumulate in the subG1 phase in a concentration- and time-dependent manner. Western Blot Analysis [1] Cell Types: HL60 cells Tested Concentrations: 0.1 μM Incubation Duration: 48 hrs (hours) Experimental Results: Bcl-2 and Mcl-1S phosphorylation increased, and Mcl-1L phosphorylation diminished. |
| Animal Protocol |
Animal/Disease Models: Severe combined immunodeficiency (SCID) mice [1]
Doses: 50 mg/kg or 100 mg/kg Route of Administration: po (oral gavage); 12 or 14 days Experimental Results: Caused significant tumor growth delay (83.3% ) and tumor volume suppression without loss of body weight. |
| References |
| Molecular Formula |
C19H20N2O6S
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|---|---|
| Molecular Weight |
404.44
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| Exact Mass |
404.104
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| CAS # |
1346169-92-3
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| PubChem CID |
56834893
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
2.5
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
28
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| Complexity |
598
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N1C2C(=C(N)C(OC)=CC=2)C=CC=1S(C1=CC(OC)=C(OC)C(OC)=C1)(=O)=O
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| InChi Key |
RBBRZMLZQCYQJM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H20N2O6S/c1-24-14-7-6-13-12(18(14)20)5-8-17(21-13)28(22,23)11-9-15(25-2)19(27-4)16(10-11)26-3/h5-10H,20H2,1-4H3
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| Chemical Name |
6-methoxy-2-(3,4,5-trimethoxyphenyl)sulfonylquinolin-5-amine
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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 |
| 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 : ~100 mg/mL (~247.26 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.18 mM) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4726 mL | 12.3628 mL | 24.7255 mL | |
| 5 mM | 0.4945 mL | 2.4726 mL | 4.9451 mL | |
| 10 mM | 0.2473 mL | 1.2363 mL | 2.4726 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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