A2806-5mg | BX-912 [702674-56-4] Clinisciences

Background

BX-912 is a potent and selective inhibitor of 3-phosphoinositide-dependent kinase 1 (PDK1) with IC50 value of 26nM [1]. BX-912 has shown 9-fold selectivity for PDK1 relative to PKA and 105-fold selectivity against PKC [1].

BX-912 has been revealed to suppress the MDA-468 cells (one kind of breast tumor cell expressing high levels of activated Akt) growth and increase caspase-3/7 activity. On the contrary, BX-912 had no effect on caspase-3/7 activation in normal primary PrECs and primary HMECs. Moreover, BX-912 has been demonstrated to induce cell cycle arrest of MDA-468 cells at the G2/M phase [1].

References:
[1] Feldman RI1, Wu JM, Polokoff MA, Kochanny MJ, Dinter H, Zhu D, Biroc SL, Alicke B, Bryant J, Yuan S, Buckman BO, Lentz D, Ferrer M, Whitlow M, Adler M, Finster S, Chang Z, Arnaiz DO. Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1. J Biol Chem. 2005 May 20;280(20):19867-74. Epub 2005 Mar 16.

Chemical Properties

Physical Appearance	A solid
Storage	Store at -20°C
M.Wt	471.35
Cas No.	702674-56-4
Formula	C₂₀H₂₃BrN₈O
Solubility	≥23.55 mg/mL in DMSO; insoluble in H2O; ≥10.25 mg/mL in EtOH
Chemical Name	N-[3-[[5-bromo-4-[2-(1H-imidazol-5-yl)ethylamino]pyrimidin-2-yl]amino]phenyl]pyrrolidine-1-carboxamide
SDF	Download SDF
Canonical SMILES	C1CCN(C1)C(=O)NC2=CC=CC(=C2)NC3=NC=C(C(=N3)NCCC4=CN=CN4)Br
Shipping Condition	Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips	We do not recommend long-term storage for the solution, please use it up soon.

Biological Activity

Description	BX-912 is a potent, ATP-competitive inhibitor of PDK-1 with IC50 value of 26 nM.
Targets	PDK-1
IC50	26 nM

Quality Control

Purity = 95.55%

Chemical structure

BX-912 [702674-56-4]

Referentie A2806-5mg

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