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AMG-47a displays subnanomolar inhibition against Lck, and low (<10 nM) inhibition against other hard to inhibit kinases such as KDR and SRC and MAPK α (p38α). In addition, at slightly higher doses but well under 10 μM, AMG-47a effectively inhibits the JNK family of kinases including TYK2 at ~ 1.2 μM. AMG-47a selectively reduced the levels of EGFP-KRASG12V protein but did not affect EGFP protein in cells.
| Cell Experiment | |
|---|---|
| Cell lines | HeLa cells |
| Preparation method | Cells were treated with varying concentrations of AMG-47a, Ponatinib, and Torin-1. Media and compound were refreshed after 3 days on cells being treated for 5 days. |
| Concentrations | 1 uM |
| Incubation time | 48-h |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 535.56 |
| Formula | C29H28F3N5O2 |
| CAS Number | 882663-88-9 |
| Solubility (25°C) | 34 mg/mL in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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| Saracatinib
Saracatinib (AZD0530) is an orally active small molecule Src inhibitor. |
| Bosutinib
Bosutinib (SKI-606) is a novel Bcr-Abl inhibitor with IC50 values of 0.1 to 0.3 umol/L. |
| Dasatinib
Dasatinib (BMS-354825) is a small molecule inhibitor of both the SRC and BCR/ABL tyrosine kinases, with IC50's for the isolated kinases of 0.55 and 3.0 nM, respectively. |
| DCC-2036
DCC-2036 is an ABL inhibitor with IC50 of 0.8 and 2 nM for u-ABL1native and p-ABL1native, respectively. |
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