Akt1 and Akt2-IN-1|cas: 893422-47-4|DC Chemicals

Cas No.:	893422-47-4
SMILES:	C1=CC=C(C2=NNC(C3CCN(CC4C=CC(C5N=C6C=CNC(=O)C6=CC=5C5C=CC=CC=5)=CC=4)CC3)=N2)N=C1
Formula:	C₃₃H₂₉N₇O
M.Wt:	539.63
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

Akt1 and Akt2-IN-1 is an allosteric inhibitor of Akt1 (IC50 = 3.5 nM) and Akt2 (IC50 = 42 nM), with potent and balanced activity.in vitro: Akt1 and Akt2-IN-1 is dependent on the PH-domain for Akt inhibition, is selective for Akt1/2 over Akt3 (IC50 = 1900 nM), and is highly selective over other members of the AGC family of kinases (>50 lM vs PKA, PKC, SGK). Akt1 and Akt2-IN-1 has moderate activity in an hERG binding assay (IC50 = 5610 nM) and is a substrate for human P-glycoprotein (MDR1 Directional Transport Ratio (B to A/A to B) = 17.6). Akt1 and Akt2-IN-1 also shows good physical properties with a human plasma protein binding of 97.3% and a logP = 3.51. in vivo: Akt1 and Akt2-IN-1 has potent inhibitory activity against Akt1 and Akt 2 in vivo in a mouse lung and efficacy in a tumor xenograft model. Akt1 and Akt2-IN-1 shows good pharmacokinetics in rat with a low clearance of 4.6 mL/min/kg and a half-life of 3.8 h.

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101

Cat. No.	Product name	Field of application
DC8695	Akt1 and Akt2-IN-1	Akt1 and Akt2-IN-1 is an allosteric inhibitor of Akt1 (IC50 = 3.5 nM) and Akt2 (IC50 = 42 nM), with potent and balanced activity.