NVP-BEZ235, Free Base (4-[2,3-Dihydro-3-methyl-2-oxo-8-(3-quinolinyl)-1H-imidazo[4,5-c]quinolin-1-yl]-alpha,alpha-dimethyl-benzeneacetonitrile, BEZ235)

Blue Ice

469, 54

Supplied as a white to off-white powder.

NVP-BEZ235 is an imidazo[4, 5-c]quinoline derivative that inhibits PI3K and mTOR kinase activity by binding to the ATP-binding cleft of these enzymes. NVP-BEZ235 is able to effectively and specifically block the dysfunctional activation of the PI3K pathway and induce G(1) arrest. It also inhibits the growth of human cancer in animal models.

Solubility:
Soluble in anhydrous dimethylformamide at 10mg/ml after warming to 75ºC and cooling; soluble in DMSO at 1.33mg/ml with warming; soluble in 1-methyl-2-pyrrolidinone at about 2mg/ml if heated in a 75ºC bath and cooled; very poorly soluble in ethanol; very poorly soluble in water; maximum solubility in plain water is estimated to be about 10-20uM; buffers, serum or other additives may increase or decrease the aqueous solubility.

Melting Point:
282.5-285ºC

Elemental Analysis:
Calculated
C: 76.74%
H: 4.94%
N: 14.92%

Storage and Stability:
May be stored at RT for short-term only. Long-term storage is recommended at -20°C. For maximum recovery of product, centrifuge the original vial prior to removing the cap.