Size | Price | Stock | Qty |
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1mg |
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Other Sizes |
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Purity: ≥98%
ln Vitro |
(E)-Akt inhibitor-IV (compound 7) exhibited an average GI20 of 0.04 μM across four distinct cell lines, namely MDA-MB468, MDA-MB231, MCF7, and 184B5 [1]. At an average GI of 20, -IV has minimal effect on 184B5 non-myocardial growth [1].
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References |
Molecular Formula |
C31H27IN4S
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Molecular Weight |
614.54
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Exact Mass |
614.1
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CAS # |
681281-88-9
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Related CAS # |
(E)-Akt inhibitor-IV;959841-49-7
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PubChem CID |
5719375
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Appearance |
Typically exists as solid at room temperature
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LogP |
8.319
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Hydrogen Bond Donor Count |
0
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Hydrogen Bond Acceptor Count |
4
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Rotatable Bond Count |
6
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Heavy Atom Count |
37
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Complexity |
732
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Defined Atom Stereocenter Count |
0
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SMILES |
CC[N+]1=C(N(C2=C1C=C(C=C2)C3=NC4=CC=CC=C4S3)C5=CC=CC=C5)/C=C/N(C)C6=CC=CC=C6.[I-]
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InChi Key |
NAYRELMNTQSBIN-UHFFFAOYSA-M
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InChi Code |
InChI=1S/C31H27N4S.HI/c1-3-34-28-22-23(31-32-26-16-10-11-17-29(26)36-31)18-19-27(28)35(25-14-8-5-9-15-25)30(34)20-21-33(2)24-12-6-4-7-13-24/h4-22H,3H2,1-2H31H/q+1/p-1 SMILES
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Chemical Name |
5-(2-Benzothiazolyl)-3-ethyl-2-[2-(methylphenylamino)ethenyl]-1-phenyl-1H-benzimidazolium iodide
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Synonyms |
AKTIV Akt Inhibitor-IV Akt Inhibitor IV
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.6272 mL | 8.1362 mL | 16.2723 mL | |
5 mM | 0.3254 mL | 1.6272 mL | 3.2545 mL | |
10 mM | 0.1627 mL | 0.8136 mL | 1.6272 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.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT05251298 | RECRUITING | Other: Coordination through the online platform "JamesAKTIV" | Parkinson Disease | University Hospital Muenster | 2021-11-28 | Not Applicable |
NCT03164239 | COMPLETED | Behavioral: Intervention group - telephone and print exercise intervention | Physical Activity | University of Agder | 2011-04-01 | Not Applicable |
NCT04745507 | UNKNOWN STATUS | Other: Inpatient Equivalent Home Treatment | Addiction Anxiety Disorders Eating Disorders Mental Disorder |
Vivantes Netzwerk für Gesundheit GmbH | 2021-01-01 | |
NCT02678234 | WITHDRAWN | Drug: Paracetamol, phenylephrine HCl, and vitamin C | Infections, Respiratory Tract | GlaxoSmithKline | 2017-02-01 | Phase 3 |
NCT00180557 | COMPLETED | Device: Flextend II, Fineline 2, Fineline Atrial J, Selute Picotip | Bradycardia Heart Block Sick Sinus Syndrome |
Guidant Corporation | 2003-09 | Phase 4 |
GI20 value (μM) of PI3K-Akt inhibitors on three human breast cancer cell lines and one non-cancer breast cell line. GI20 is the drug dose required to reduce cell proliferation by 20%, and the value was calculated from sigmoidal dose response curves (variable slope) using the GraphPad Prism V. 4.03 program (GraphPad Software Inc.). Values are mean of triplicates of at least three independent experiments. Errors are standard errors.[1].Changkun Hu, et al. A 4-aminoquinoline derivative that markedly sensitizes tumor cell killing by Akt inhibitors with a minimum cytotoxicity to non-cancer cells. Eur J Med Chem. 2010 Feb;45(2):705-9. td> |
CQ analogs 2 and 3, but not 1, 4 and 5, effectively killed 184B5 non-cancer cells when combined with constant amount of Akt inhibitors. The doses of Akt inhibitors 7–10 were 0.04, 0.4, 3.5, and 0.5 μM, respectively. Values are mean of triplicates of at least three independent experiments. Errors are standard errors.[1].Changkun Hu, et al. A 4-aminoquinoline derivative that markedly sensitizes tumor cell killing by Akt inhibitors with a minimum cytotoxicity to non-cancer cells. Eur J Med Chem. 2010 Feb;45(2):705-9. td> |
Combination effect of variant doses of CQ analog 5 and 0.4 μM of Akt inhibitor 8 (A) or 3.5 μM of Akt inhibitor 9 (B) on MDA-MB231, MDA-MB468, MCF-7, and 184B5 cells. Values are mean of triplicates of at least three independent experiments. Errors are standard errors.[1].Changkun Hu, et al. A 4-aminoquinoline derivative that markedly sensitizes tumor cell killing by Akt inhibitors with a minimum cytotoxicity to non-cancer cells. Eur J Med Chem. 2010 Feb;45(2):705-9. td> |