A pan-Akt inhibitor
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GDC-0068

Item No. 18412

Technical Information
Formal Name
(2S)-(4-chlorophenyl)-1-[4-[(5R,7R)-6,7-dihydro-7-hydroxy-5-methyl-5H-cyclopentapyrimidin-4-yl]-1-piperazinyl]-3-[(1-methylethyl)amino]-1-propanone
CAS Number
1001264-89-6
Synonyms
  • Ipatasertib
  • RG-7440
Molecular Formula
C24H32ClN5O2
Formula Weight
Purity
≥98%
A crystalline solid
DMF: 25 mg/mlDMF:PBS(pH 7.2)(1:1): 0.5 mg/mlDMSO: 15 mg/mlEthanol: 20 mg/ml
λmax
258 nm
SMILES
ClC1=CC=C([C@H](C(N2CCN(C3=NC=NC4=C3[C@H](C)C[C@H]4O)CC2)=O)CNC(C)C)C=C1
InChi Code
InChI=1S/C24H32ClN5O2/c1-15(2)26-13-19(17-4-6-18(25)7-5-17)24(32)30-10-8-29(9-11-30)23-21-16(3)12-20(31)22(21)27-14-28-23/h4-7,14-16,19-20,26,31H,8-13H2,1-3H3/t16-,19-,20-/m1/s1
InChi Key
GRZXWCHAXNAUHY-NSISKUIASA-N
Origin
Synthetic
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    GDC-0068 is a selective, ATP-competitive, pan-Akt inhibitor that targets Akt1, 2, and 3 with IC50 values of 5, 18, and 8 nM, respectively in cell-free assays.1 It is 620-fold selective for Akt over protein kinase A and has been shown to block Akt signaling selectively in cultured tumor cell lines characterized by activated Akt, halting cell cycle progression and reducing cell viability.1 In multiple tumor xenograft models, oral administration of GDC-0068 at 100 mg/kg/day can lead to delayed tumor growth and regression.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Lin, J., Sampath, D., Nannini, M.A., et alTargeting activated Akt with GDC-0068, a novel selective Akt inhibitor that is efficacious in multiple tumor models. Clin. Cancer Res. 19(7), 1760-1772 (2016).