MDL | - |
---|---|
Molecular Weight | 510.63 |
Molecular Formula | C26H38N8O3 |
SMILES | NC1=C2C(C3=CC(OC)=C(NC(OC(C)(C)C)=O)C=C3)=NN(CCN4CCC(N(C)C)CC4)C2=NC=N1 |
eCF506 is a highly potent and orally bioavailable inhibitor of the non-receptor tyrosine kinase Src with an IC 50 of less than 0.5 nM.
IC50: less than 0.5 nM (Src) [1]
eCF506 induces a very potent antiproliferative effect in both MCF7 and MDA-MB-231 cells. eCF506 inhibits phosphorylation of SRC and FAK at low nanomolar levels, with complete inhibition observed at 100 nM. eCF506 significantly reduces cell motility at 10 nM as early as 6 h into the study, with equivalent efficacy to dasatinib. eCF506 exclusively inhibits SFK, with subnanomolar IC 50 values against SRC and YES (IC 50 =0.5, 2.1 nM). It is important to highlight that eCF506 displays a vast difference in activity (>950-fold difference) between ABL and its primary target SRC [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
eCF506 shows a moderate oral bioavailability (25.3%). A significant reduction of phospho-SRC Y416 is observed in the xenograft sections from mice treated with eCF506 relative to the untreated animal controls [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Solid
Room temperature in continental US; may vary elsewhere.
Powder | -20°C | 3 years |
---|---|---|
4°C | 2 years | |
In solvent | -80°C | 6 months |
-20°C | 1 month |
DMSO : 62.5 mg/mL ( 122.40 mM ; Need ultrasonic)
H 2 O : < 0.1 mg/mL (insoluble)
Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
---|
1 mM | 1.9584 mL | 9.7918 mL | 19.5837 mL |
5 mM | 0.3917 mL | 1.9584 mL | 3.9167 mL |
10 mM | 0.1958 mL | 0.9792 mL | 1.9584 mL |