666-15

Cas No.:	1433286-70-4
SMILES:	O=C(NC1=CC=C(Cl)C=C1O)C2=CC3=CC=CC=C3C=C2OCCNC(C4=C(OCCCN)C=C(C=CC=C5)C5=C4)=O.Cl
Formula:	C33H31Cl2N3O5
M.Wt:	620.52
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	666-15 is a potent and selective CREB inhibitor with an IC50 of 81 nM.
In Vivo:	Preliminary toxicity studies show that intraperitoneal (ip) injection of 10 mg/kg of 666-15 is well tolerated in mice. The tumor growth in the mice treated with 666-15 is efficaciously inhibited with complete tumor stasis. During the same period, the tumor volume in the vehicle-treated group is more than tripled. The body weights of 666-15-treated animals and vehicle-treated ones are indistinguishable from each other during the entire treatment period[1].
In Vitro:	666-15 potently inhibits 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 exhibits robust activity as well with GI50 of 0.47 and 0.31 μM. 666-15 is also found to be a rather weak inhibitor of CREB-CBP interaction with IC50 of 18.27 μM. 666-15 inhibits CREB’s transcription activity in living cells independent of direct CREB or CBP binding interaction. 666-15 is very potent in inhibiting CREB’s transcription activity. 666-15 also inhibits endogenous CREB target gene expression, the transcript level of nuclear receptor related 1 protein (Nurr1/NR4A2)[1].