BX795

Cas No.:	702675-74-9
Chemical Name:	N-[3-[[5-Iodo-4-[3-(thiophene-2-carbonylamino)propylamino]pyrimidin-2-yl]amino]phenyl]pyrrolidine-1-carboxamide
Synonyms:	N-[3-[[5-Iodo-4-[[3-[(2-thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide;BX-795;1-Pyrrolidinecarboxamide, N-[3-[[5-iodo-4-[[3-[(2-thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-;BX 795;BX-795 (BX 795 );N-[3-[[5-iodo-4-[3-(thiophene-2-carbonylamino)propylamino]pyrimidin-2-yl]amino]phenyl]pyrrolidine-1-carboxamide;BX7;BX795;N-(3-{[5-Iodo-4-({3-[(Thiophen-2-Ylcarbonyl)amino]propyl}amino)pyrimidin-2-Yl]amino}phenyl)pyrrolidine-1-Carboxamide;N-(3-(5-iodo-4-(3-(thiophene-2-carboxamido)propylamino)pyrimidin-2-ylamino)phenyl)pyrrolidine-1-carboxamide;C23H26IN7O2S;N-(3-
SMILES:	IC1=C([H])N=C(N=C1N([H])C([H])([H])C([H])([H])C([H])([H])N([H])C(C1=C([H])C([H])=C([H])S1)=O)N([H])C1C([H])=C([H])C([H])=C(C=1[H])N([H])C(N1C([H])([H])C([H])([H])C([H])([H])C1([H])[H])=O
Formula:	C23H26In7O2S
M.Wt:	591.4677
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

BX795 is a potent and selective PDK1 inhibitor with an IC50 of 6 nM, showing 50-fold selectivity over PKA, PKC, c-Kit, GSK3β etc.

In Vitro:

BX795 effectively blocks PDK1 activity in PC-3 cells, as shown by their ability to block phosphorylation of S6K1, Akt, PKCδ, and GSK3β. BX795 potently inhibits tumor cell growth on plastic with IC50 of 1.6, 1.4, and 1.9 μM for MDA-468, HCT-116 and MiaPaca cells, respectively. In soft agar, BX795 displays higher growth inhibition with IC50 of 0.72, and 0.25 μM for MDA-468, and PC-3 cells, respectively[1]. In addition, BX795, as an inhibitor of the TBK1/IKKε, blocks TBK1- and IKKε-mediated activation of IRF3 and production of IFN-β[2]. In platelet physiological responses, BX795 produces inhibitory effect on 2-MeSADP-induced or collagen-induced aggregation, ATP secretion and thromboxane generation[3].