AKT-IN-3
Based on 1 Customer Validation
AKT-IN-3 (compound E22) is a potent, orally active low hERG blocking Akt inhibitor, with 1.4 nM, 1.2 nM and 1.7 nM for Akt1, Akt2 and Akt3, respectively. AKT-IN-3 (compound E22) also exhibits good inhibitory activity against other AGC family kinases, such as PKA, PKC, ROCK1, RSK1, P70S6K, and SGK. AKT-IN-3 (compound E22) induces apoptosis and inhibits metastasis of cancer cells.
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- Purity: 98.12%
- CAS No.: 2374740-21-1
- 화학식: C23H23Cl2F2N5O3
- 분자량:526.36
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
|
Akt1 1.4 nM (IC50) |
Akt2 1.2 nM (IC50) |
Akt3 1.7 nM (IC50) |
PKA 0.3 nM (IC50) |
P70S6K 8.9 (IC50) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
1.1 μM
Compound: E22
|
Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay
Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay
|
[PMID: 31298542] |
| LNCaP | IC50 |
0.05 μM
Compound: E22
|
Antiproliferative activity against human LNCAP cells
Antiproliferative activity against human LNCAP cells
|
[PMID: 31298542] |
| LNCaP | IC50 |
44 nM
Compound: E22
|
Inhibition of Akt in human LNCaP cells assessed as reduction in PRAS40 phosphorylation at T246 residue after 1 hr by ELISA
Inhibition of Akt in human LNCaP cells assessed as reduction in PRAS40 phosphorylation at T246 residue after 1 hr by ELISA
|
[PMID: 31298542] |
| OVCAR-8 | IC50 |
0.8 μM
Compound: E22
|
Antiproliferative activity against human OVCAR8 cells
Antiproliferative activity against human OVCAR8 cells
|
[PMID: 31298542] |
Chemical Information
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CAS No. 2374740-21-1
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Appearance Solid
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분자량 526.36
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화학식 C23H23Cl2F2N5O3
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Color White to off-white
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SMILES
CNC(C[C@H]1NC[C@@H](NC(C2=CC(C3=C(Cl)C=NN3C)=C(Cl)O2)=O)[C@H](C4=CC(F)=C(F)C=C4)C1)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : ≥ 100 mg/mL (189.98 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8998 mL | 9.4992 mL | 18.9984 mL | 47.4960 mL |
| 5 mM | 0.3800 mL | 1.8998 mL | 3.7997 mL | 9.4992 mL | |
| 10 mM | 0.1900 mL | 0.9499 mL | 1.8998 mL | 4.7496 mL | |
| 15 mM | 0.1267 mL | 0.6333 mL | 1.2666 mL | 3.1664 mL | |
| 20 mM | 0.0950 mL | 0.4750 mL | 0.9499 mL | 2.3748 mL | |
| 25 mM | 0.0760 mL | 0.3800 mL | 0.7599 mL | 1.8998 mL | |
| 30 mM | 0.0633 mL | 0.3166 mL | 0.6333 mL | 1.5832 mL | |
| 40 mM | 0.0475 mL | 0.2375 mL | 0.4750 mL | 1.1874 mL | |
| 50 mM | 0.0380 mL | 0.1900 mL | 0.3800 mL | 0.9499 mL | |
| 60 mM | 0.0317 mL | 0.1583 mL | 0.3166 mL | 0.7916 mL | |
| 80 mM | 0.0237 mL | 0.1187 mL | 0.2375 mL | 0.5937 mL | |
| 100 mM | 0.0190 mL | 0.0950 mL | 0.1900 mL | 0.4750 mL |