Akt1 and Akt2-IN-1 [893422-47-4]

Catalog number: HY-50862_5mg
Brand: MedChem Express
Packing: 5 mg
Other sizes: Other sizes available
Price: € 442.00
Expected delivery time: 10 days

Product specifications for - Akt1 and Akt2-IN-1 [893422-47-4]

Product group: Chemicals
Category: Other
CAS No.: 893422-47-4
Purity: >98%
Molecular Formula: C33H29N7O
Molecular weight: 539.63
Datasheet: Datasheet
  Research Use Only
UNSPSC: 12352200
Scientific information: 
Scientific info: 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. IC50 value: 3.5 nM (Akt1), 42 nM (Akt2) Target: Akt 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.
Safety information: 
Additional information: 
Synonyms: HY-50862