compound 3i (666-15)
Molecular Weight(MW): 620.52
Compound 3i (666-15) is a potent and selective inhibitor of CREB-mediated gene transcription (IC50 = 0.081 ± 0.04 μM) and also potently inhibits cancer cell growth without harming normal cells.
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|Description||Compound 3i (666-15) is a potent and selective inhibitor of CREB-mediated gene transcription (IC50 = 0.081 ± 0.04 μM) and also potently inhibits cancer cell growth without harming normal cells.|
666-15 could potently inhibit cancer cell growth. In MDA-MB-231 and MDA-MB-468 cells, the GI50 for 666-15 is 73 and 46 nM, respectively. In A549 and MCF-7 cells, it exhibit robust activity as well with GI50 of 0.47 and 0.31 μM. 666-15 inhibits CREB’s transcription activity in living cells independent of direct CREB or CBP binding interaction.
In an in vivo MDA-MB-468 xenograft model, 666-15 completely suppresses the tumor growth without overt toxicity. Preliminary toxicity studies show that intraperitoneal (ip) injection of 10 mg/kg of 666-15 is well tolerated in mice.
|In vitro||DMSO||100 mg/mL (161.15 mM)|
|Ethanol||3 mg/mL (4.83 mM)|
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