CCT128930 HCl

- Overview
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    Background
    
    CCT128930 HCl is a potent, selective, novel and ATP-competitive inhibitor for AKT2 (IC50= 6 nM). It also has 28-fold and 20-fold selectivity over PKA kinase (IC50= 168 nM) and p70S6K (IC50= 120 nM), respectively.
    Akt (protein kinase B) is a serine/threonine-specific protein kinase that plays a key role in multiple cellular processes such as glucose metabolism, apoptosis, cell proliferation, transcription and cell migration.
    In multi tumor cell line, CCT128930 HCl showed antiproliferative effect and blocked the phosphorylation of various Akt substrates. In PTEN-null human glioblastoma cells (U87MG), CCT128930 HCl treatment led to a G1 arrest associated with Akt pathway suppression. [1]
    In U87MG tumor xenografts, CCT128930 HCl inhibited the phosphorylation of Akt downstream biomarkers. In U87MG, HER-2 positive and IK3CA-mutant BT474 human breast cancer xenografts, antitumor activity were recorded as tumor volume decreased. CCT128930 HCl-treated mouse whisker folliciles in vivo and human hair follicles treated ex vivo exerted prominent reduction in pThr246 PRAS40. [1]
- Properties
  - Alternative Name
    
    4-(4-chlorobenzyl)-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidin-4-amine hydrochloride
    
    CAS Number
    
    885499-61-6 (free base)
    
    Molecular Formula
    
    C18H21Cl2N5
    
    Molecular Weight
    
    378.30
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in H2O; ≥17.1 mg/mL in DMSO; ≥5.17 mg/mL in EtOH with ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

CCT128930 HCl

Background

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