| Size | Price | Stock | Qty |
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| 10mg |
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| ln Vitro |
3CAI has the ability to inhibit AKT. In vitro kinase assays were used to test the impact of 3CAI on the kinase activities of AKT1, MEK1, JNK1, ERK1, and TOPK based on these screening data. The findings indicated that 3CAI (1 μM) did not have any effect on the other kinases tested; instead, it only inhibited the activity of AKT1 kinase. AKT1 is more effectively inhibited by 3CAI than by PI3K, with 60% inhibition at 1 μM and 10% at 10 μM, respectively. Both AKT1 and AKT2 activity were markedly suppressed by 3CAI in a dose-dependent manner. Apoptosis is induced and AKT downstream targets are inhibited by 3CAI. The AKT-mediated phosphorylation sites of GSK3β (Ser9) and mTOR (Ser2448) were markedly and time-dependently decreased by 3CAI. Furthermore, following 12 or 24 hours of treatment, 3CAI also increased the levels of the pro-apoptotic marker proteins p53 and p21. In 6 centimeter dishes, HCT116 and HT29 colon cancer cells were seeded with 1% FBS/McCoy's 5A (HCT116) supplemented with 3CAI (4 μM), I3C, or AKT inhibitor, and incubated for four days. The findings demonstrated that, in comparison to untreated control cells, the number of apoptotic cells in HCT116 and HT29 colon cancer cells was significantly higher following 3CAI treatment [1].
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| ln Vivo |
In order to investigate the in vivo anticancer activity of 3CAI, individual athymic nude mice were given injections of HCT116 cancer cells into their right flank. For a period of 21 days, mice were given vehicle, I3C (100 mg/kg), or 3CAI (20 or 30 mg/kg) orally five times a week. Treatment of mice with 30 mg/kg 3CAI effectively decreased the growth of HCT116 tumors by 50% (p<0.05) as compared to the vehicle treatment group. Interestingly, mice who received these dosages of 3CAI therapy did not exhibit any overt toxicity or appreciable weight loss as compared to the group that received vehicle treatment. The expression of these AKT target proteins is significantly inhibited by 3CAI at 30 mg/kg in tumor tissue [1].
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| References |
| Molecular Formula |
C10H8NOCL
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|---|---|
| Molecular Weight |
193.62962
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| Exact Mass |
193.029
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| CAS # |
28755-03-5
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| PubChem CID |
152961
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| Appearance |
Off-white to pink solid powder
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| Density |
1.337g/cm3
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| Boiling Point |
379.1ºC at 760 mmHg
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| Flash Point |
183ºC
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| Vapour Pressure |
6.02E-06mmHg at 25°C
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| Index of Refraction |
1.659
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| LogP |
2.589
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
13
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| Complexity |
207
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
LLZQFAXTCYDVTR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H8ClNO/c11-5-10(13)8-6-12-9-4-2-1-3-7(8)9/h1-4,6,12H,5H2
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| Chemical Name |
2-chloro-1-(1H-indol-3-yl)ethanone
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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 : ~250 mg/mL (~1291.12 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (10.74 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 (10.74 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 | 5.1645 mL | 25.8224 mL | 51.6449 mL | |
| 5 mM | 1.0329 mL | 5.1645 mL | 10.3290 mL | |
| 10 mM | 0.5164 mL | 2.5822 mL | 5.1645 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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