| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| ln Vitro |
LNCaP and PC3 cells treated with MT 63-78 (0-50 μM; 4 days) exhibit a dose-dependent decrease in cell number along with activation of AMPK signaling [1]. The G2/M population is significantly enriched when LNCaP and CRPC cells are treated with MT 63-78 (25 μM; 24 hours) [1]. Pro-apoptotic BH3 protein Puma accumulates in conjunction with a decrease in anti-apoptotic Mcl-1 in LNCaP, PC3, C4-4, C4-2B, CL1, and 22RV1 cells treated with MT 63-78 (0-50 μM; 24 hr) [1]. Following treatment with MT 63-78 (0-50 μM; 30 min) in LNCaP and PC3 cells, phosphorylation of two important AMPK targets (raptor on Ser792 and acetyl-CoA carboxylase (ACC) on Ser79) was observed in a dose-dependent manner. Furthermore, it raises Thr172's phosphorylation on the AMPK α subunit [1].
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| ln Vivo |
In C57 BL/6 male mice, treatment with MT 63-78 (30 mg/kg; i.p.; daily; for 14 days) reduced tumor growth by 33% [1].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: LNCaP and PC3 Cell Tested Concentrations: 0 μM, 1 μM, 5 μM, 10 μM, 25 μM, 50 μM Incubation Duration: 4 days Experimental Results: A dose-dependent decrease in cell number was observed simultaneously Activation of AMPK signaling. Cell cycle analysis[1] Cell Types: LNCaP and CRPC Cell Tested Concentrations: 25 μM Incubation Duration: 24 hrs (hours) Experimental Results: Induced significant enrichment of G2/M population in androgen-sensitive and CRPC cell models. Apoptosis analysis[1] Cell Types: LNCaP, PC3, C4-4, C4-2B, CL1 and 22RV1 Cell Tested Concentrations: 0 μM, 10 μM, 25 μM, 50 μM Incubation Duration: 24 hrs (hours) Experimental Results: Induction of anti-apoptosis The decrease in Mcl-1 was consistent with the accumulation of the pro-apoptotic BH3 protein Puma in all PCa cells. Western Blot Analysis[1] Cell Types: LNCaP and PC3 Cell Tested Concentrations: 0 μM, 0.25 μM, 0.5 μM, 1 μM, 5 μM, 25 μM, 50 μM Incubation Duration: 30 min Experimental Results: Observed a dose-dependent phosphorylation of the two major AMPK targets Acetyl-CoA Carboxylase (ACC) on Ser79 and of Raptor on Ser792. A corresponding increase in Thr172 phosphorylation on the AMPK α subunit was also observed. |
| Animal Protocol |
Animal/Disease Models: C57 BL/6 male mice bearing LNCaP tumors [1]
Doses: 30 mg/kg Route of Administration: intraperitoneal (ip) injection; daily; lasted for 14 days. Experimental Results: resulted in 33% inhibition of tumor growth. |
| References |
| Molecular Formula |
C21H14N2O2
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|---|---|
| Molecular Weight |
326.348064899445
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| Exact Mass |
326.105
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| CAS # |
1179347-65-9
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| PubChem CID |
59145386
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| Appearance |
Light yellow to brown solid powder
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| LogP |
4.3
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
25
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| Complexity |
497
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| Defined Atom Stereocenter Count |
0
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| SMILES |
OC1C=CC=C(C=1C1C=CC(=CC=1)C1C=CC2=C(C(C#N)=CN2)C=1)O
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| InChi Key |
IGSYZPLXAFVMKY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H14N2O2/c22-11-16-12-23-18-9-8-15(10-17(16)18)13-4-6-14(7-5-13)21-19(24)2-1-3-20(21)25/h1-10,12,23-25H
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| Chemical Name |
5-[4-(2,6-dihydroxyphenyl)phenyl]-1H-indole-3-carbonitrile
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| Synonyms |
MT63-78; MT63 78; MT6378
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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 : ~125 mg/mL (~383.02 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.37 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 (6.37 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 | 3.0642 mL | 15.3210 mL | 30.6419 mL | |
| 5 mM | 0.6128 mL | 3.0642 mL | 6.1284 mL | |
| 10 mM | 0.3064 mL | 1.5321 mL | 3.0642 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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