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AdipoGen Life Sciences
A-674563 (free base)
55
CHF
CHF 55.00
In stock
AG-CR1-3680-M0011 mgCHF 55.00
AG-CR1-3680-M0055 mgCHF 190.00
AG-CR1-3680-M01010 mgCHF 270.00
| Product Details | |
|---|---|
| Synonyms | αS-[[[5-(3-Methyl-1H-indazol-5-yl)-3-pyridinyl]oxy]methyl]-benzeneethanamine |
| Product Type | Chemical |
| Properties | |
| Formula |
C22H22N4O |
| MW | 358.4 |
| CAS | 552325-73-2 |
| Purity Chemicals | ≥98% (HPLC) |
| Appearance | Waxy solid. |
| Solubility | Soluble in DMF (20mg/ml), DMSO (10mg/ml) or ethanol (10mg/ml). |
| InChi Key | BPNUQXPIQBZCMR-IBGZPJMESA-N |
| Smiles | CC1=NNC2=CC=C(C3=CC(OC[C@H](CC4=CC=CC=C4)N)=CN=C3)C=C21 |
| Shipping and Handling | |
| Shipping | AMBIENT |
| Short Term Storage | +4°C |
| Long Term Storage | -20°C |
| Handling Advice | Keep cool and dry. |
| Use/Stability | Stable for at least 2 years after receipt when stored at -20°C. |
| Documents | |
| MSDS |
 Download PDF |
| Product Specification Sheet | |
| Datasheet |
Download PDF |
Description
- A-674563 is a potent, ATP-competitive, reversible and orally available Akt1 inhibitor with an IC50 of 11nM. Binds to the ATP site of the AKT kinase domain, inhibiting AKT-catalyzed phosphorylation activity.
- Also inhibits PKA and CDK2 with IC50 values of 16nM and 46nM, respectively.
- 10- to >1,800-fold selective for Akt1 versus additional kinases in the CMGC, CAMK and TK families.
- Anticancer compound. Reduces phosphorylation of Akt downstream targets in cells and slows proliferation of tumor cells in vitro with an EC50 value of 0.4µM.
- Shown to decrease tumor growth in mouse tumor xenograft models.
- Decreased sphingosine kinase 1 (SphK1) activity in AML cells to deplete pro-survival sphingosine-1-phosphate (S1P) and boost pro-apoptotic ceramide production.
Product References
- Potent and selective inhibitors of Akt kinases slow the progress of tumors in vivo: Y. Luo, et al.; Mol. Cancer Ther. 4, 977 (2005)
- Characterization of an Akt kinase inhibitor with potent pharmacodynamic and antitumor activity: N. Rhodes, et al.; Cancer Res. 68, 2366 (2008)
- Soft tissue sarcoma cells are highly sensitive to AKT blockade: a role for p53-independent up-regulation of GADD45 alpha: Q.S. Zhu, et al.; Cancer Res. 68, 2895 (2008)
- Enhanced sensitivity to sorafenib by inhibition of Akt1 expression in human renal cell carcinoma ACHN cells both in vitro and in vivo: H. Tei, et al.; Hum. Cell. 28, 114 (2015)
- Unique roles of Akt1 and Akt2 in IGF-IR mediated lung tumorigenesis: S.E. Franks, et al.; Oncotarget 7, 3297 (2016)
- Dual inhibition of AKT/FLT3-ITD by A674563 overcomes FLT3 ligand-induced drug resistance in FLT3-ITD positive AML: A. Wang, et al.; Oncotarget 7, 29131 (2016)
- Concurrent targeting Akt and sphingosine kinase 1 by A-674563 in acute myeloid leukemia cells: L. Xu, et al.; BBRC 472, 662 (2016)
- Pre-clinical assessment of A-674563 as an anti-melanoma agent: Y. Zou, et al.; BBRC 477, 1 (2016)