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$0.00 - Kobayashi T, .et al. A-674563 increases chondrocyte marker expression in cultured chondrocytes by inhibiting Sox9 degradation, Biochem Biophys Res Commun, 2018, Jan 1;495(1):1468-1475 PMID: 29196261
- Lin Xu, .et al. Concurrent targeting Akt and sphingosine kinase 1 by A-674563 in acute myeloid leukemia cells, Biochem Biophys Res Commun, 2016, Apr 15;472(4):662-8 PMID: 26920060
- Zou Y, .et al. Pre-clinical assessment of A-674563 as an anti-melanoma agent, Biochem Biophys Res Commun, 2016, Aug 12;477(1):1-8 PMID: 26970307
Biological Activity
A-674563 is a B/Akt inhibitor with an IC50 of 14 nM and also shows inhibitory activity against PKA and CDK2 with IC50 of 16 and 46 nM, respectively.
Targets
| Target | Value |
|---|---|
| Akt1 | ki: 11nM |
| PKA | ki: 16nM |
| CDK2 | ki: 46nM |
| GSK-3β | ki: 110nM |
| ERK2 | ki: 260nM |
| PKCδ | ki: 360nM |
| RSK2 | ki: 580nM |
| MAPK-AP2 | ki: 1.1μM |
| PKCγ | ki: 1.2μM |
| FLT1 | ki: >2.2μM |
| Chk1 | ki: 2.6μM |
| KDR | ki: >3.7μM |
| CK2 | ki: 5.4μM |
| c-Kit | ki: >5.8μM |
| Src | ki: 13μM |
| PDK-1 | ki: >20μM |
| In vitro (25°C) | DMSO | 71 mg/mL (198.08 mM) | |
| Water | 71 mg/mL (198.08 mM) | ||
| Ethanol | 18 mg/mL (50.21 mM) | ||
| In vivo | Saline | 28 mg/mL | |
|
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
|||
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 27.9 mL | 139.51 mL | 279.02 mL |
| 0.5 mM | 5.58 mL | 27.9 mL | 55.8 mL |
| 1 mM | 2.79 mL | 13.95 mL | 27.9 mL |
| 5 mM | 0.56 mL | 2.79 mL | 5.58 mL |
*The above data is based on the productmolecular weight 358.4 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Catalog Num | A11034 |
|---|---|
| Actions | Inhibitor |
| CAS No. | 552325-73-2 |
| Formula | C22H22N4O |
| M. Wt | 358.4 |
| Purity | >98% |
| Synonyms | A674563 |
| SMILES | CC1=C2C=C(C=CC2=NN1)C3=CC(=CN=C3)OC[[email protected]](CC4=CC=CC=C4)N |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
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