Ipatasertib dihydrochloride

  • Chemical Properties
CAS No. 1396257-94-5 Cat. No. BCP23821
Name Ipatasertib dihydrochloride
Synonyms GDC0068 2HCl;Ipatasertib 2HCl;GDC0068 dihydrochloride;GDC-0068 dihydrochloride; RG-7440 dihydrochloride;
Formula C24H34Cl3N5O2 M. Wt 530.92
  • Biological Activity
Description Ipatasertib is typically efficacious in xenograft models in which Akt is activated because of genetic alterations including PTEN loss, PIK3CA mutations/amplifications, or HER2 overexpression. In these models, tumor growth delay, stasis, or regression is achieved at or below 100 mg/kg daily oral dose, which is the maximum dose tested in immunocompromised mice that is well tolerated. When tested in vivo, daily dosing of Ipatasertib in combination with Docetaxel induces tumor regression and stasis in the PC-3 and MCF7-neo/HER2 xenograft models, at doses where each single agent is ineffective or only causes modest tumor growth delay. Similarly, increased TGI is observed in the OVCAR3 ovarian cancer xenograft model when Ipatasertib is combined with Carboplatin. The combination of Ipatasertib with Docetaxel or Carboplatin is tolerated with less than 5% body weight loss when compared with treatment with each chemotherapeutic agent alone.
Pathways PI3K/Akt/mTOR 
Targets AKT 

Structure

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