MDL | MFCD29924714 |
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Molecular Weight | 669.79 |
Molecular Formula | C35H32FN5O4S2 |
SMILES | O=C(C1=C(CCCOC2=CC=C(C#CCN(C)C)C=C2F)SC(N3CC4=C(C=CC=C4C(NC5=NC6=CC=CC=C6S5)=O)CC3)=N1)O |
A-1155463 is a highly potent and selective BCL-XL inhibitor with an EC 50 of 70 nM in Molt-4 cell.
Bcl-xL 0.01 nM (Ki) |
Bcl-2 80 nM (Ki) |
A-1155463 shows picomolar binding affinity to BCL-X L (K i <0.01 nM), and >1000-fold weaker binding to BCL-2 (K i = 80 nM) and related proteins BCL-W (K i = 19 nM) and MCL-1 (K i > 440 nM) [2] . A-1155463 demonstrates strong growth inhibition of over half of the colorectal cell lines as defined by EC 50 values ≤0.5 μM in the presence of 10 % FBS [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
A-1155463 caused a mechanism-based and reversible thrombocytopenia in mice and inhibited H146 small cell lung cancer xenograft tumor growth in vivo following multiple doses [2] .
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 |
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4°C | 2 years | |
In solvent | -80°C | 6 months |
-20°C | 1 month |
DMSO : 12.5 mg/mL ( 18.66 mM ; ultrasonic and warming and heat to 60°C)
Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
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1 mM | 1.4930 mL | 7.4650 mL | 14.9301 mL |
5 mM | 0.2986 mL | 1.4930 mL | 2.9860 mL |
10 mM | 0.1493 mL | 0.7465 mL | 1.4930 mL |