Ipatasertib dihydrochloride, Inhibitor

Ipatasertib dihydrochloride

Cat. Num. AAA5754895

• Purity: 98.00%
• Synonyms: Ipatasertib dihydrochloride; GDC-0068 dihydrochloride; RG-7440 dihydrochloride; inhibitor

• Purity/Purification: 98.00%
• Form/Format: Solid. Powder

• Solubility: DMSO: 125mg/mL (235.44mM) Need ultrasonic; H2O: 41mg/mL (77.22mM); (<1mg/ml refers to the product slightly soluble or insoluble)
• Formula: C24H34Cl3N5O2
• SMILES: ClC1=CC=C([C@@H](CNC(C)C)C(N2CCN(C3=C([C@H](C)C[C@H]4O)C4=NC=N3)CC2)=O)C=C1.[H]Cl.[H]Cl
• CAS Number: 1396257-94-5
• Target & IC50: Akt1: ic50 5nM; Akt3: ic50 8nM; Akt2: ic50 18nM; PKA: ic50 3100nM
• In Vitro: Ipatasertib is typically efficacious in xenograft models in which Akt is activated because of genetic alterations including PTEN loss, PIK3CA mutations/amplification, or HER2 overexpression. The combination of Ipatasertib with RP-56976 or NSC 241240 is tolerated with less than 5% body weight loss when compared with treatment with each chemotherapeutic agent alone. The daily dosing of Ipatasertib in combination with RP-56976 induces tumor regression and stasis in the PC-3 and MCF7-neo/HER2 xenograft models, at doses where every single agent is ineffective or only causes modest tumor growth delay, when tested in vivo. Similarly, enhanced TGI is observed in the OVCAR3 ovarian cancer xenograft model when Ipatasertib is combined with NSC 241240 [2].
• Preparation and Storage: Store at -20 degree C for 3 years powder; -80 degree C for 2 years in solvent

Structure

Related Product Information for Ipatasertib dihydrochloride, inhibitor

Ipatasertib dihydrochloride is a highly selective and ATP-competitive inhibitor of pan-Akt (IC50s: 5, 18, and 8nM for Akt1, Akt2, and Akt3, respectively).

Product Categories/Family for Ipatasertib dihydrochloride, inhibitor

Cytoskeletal Signaling; Akt; PI3K/Akt/mTOR signaling; Protein Tyrosine Kinase/RTK

References

Blake JF, et al. Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment,of human tumors. J Med Chem. 2012 Sep 27;55(18):8110-27.
Blake JF, et al. Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment,of human tumors. J Med Chem. 2012 Sep 27;55(18):8110-27.
Lin J, et al. Targeting activated Akt with GDC-0068, a novel selective Akt inhibitor that is efficacious in multiple tumor models. Clin Cancer Res. 2013 Apr 1;19(7):1760-72.
Lin J, et al. Targeting activated Akt with GDC-0068, a novel selective Akt inhibitor that is efficacious in multiple tumor models. Clin Cancer Res. 2013 Apr 1;19(7):1760-72.