BEZ235 Tosylate
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CAS No. | 1028385-32-1 | Cat. No. | BCP16240 |
Name | BEZ235 Tosylate | ||
Synonyms | BEZ-235 Tosylate;BEZ 235 Tosylate; | ||
SMILES | |||
Chemical Name | |||
Formula | C37H31N5O4S | M. Wt | 641.74 |
Purity | 98% | Storage | Store at 4-8°C |
Description | in vitro: BEZ235 significantly reduces the phosphorylation levels of the mTOR activated kinase p70S6K. BEZ235 results in a reduction of S235/S236P-RPS6 levels with IC50 of 6.5 nM. The activity of BEZ23 against mTOR is determined using a biochemical mTOR K-LISA assay with IC50 of 20.7 nM. BEZ235 shows slightly lower activity against its β paralogue with IC50 of 75 nM. The PI3K/Akt/mTOR pathway is often constitutively activated in human tumor cells. BEZ235 blocks PI3K and mTOR kinase activity by binding to the ATP-binding cleft of these enzymes. Both PTEN-null cell lines PC3M and U87MG show a dose-dependent reduction in cell proliferation when treated with increasing concentrations of BEZ235 with an average GI50 of 10-12 nM. BEZ235 is an mTORC1/2 catalytic inhibitor. in vivo: BEZ235 induces regression of the tumors (69%) without statistically significant effect on body weight gain. Altogether, these preliminary in vivo efficacy results show that BEZ235 causes disease stasis when administ |
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