Ipatasertib (GDC-0068)

Catalog No.S2808 Synonyms: RG7440

Ipatasertib (GDC-0068) Chemical Structure

Molecular Weight(MW): 458

Ipatasertib (GDC-0068) is a highly selective pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 5 nM/18 nM/8 nM in cell-free assays, 620-fold selectivity over PKA. Phase 2.

Size Price Stock Quantity  
In DMSO USD 378 In stock
USD 270 In stock
USD 370 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Cited by 53 Publications

Purity & Quality Control

Choose Selective Akt Inhibitors

Biological Activity

Description Ipatasertib (GDC-0068) is a highly selective pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 5 nM/18 nM/8 nM in cell-free assays, 620-fold selectivity over PKA. Phase 2.
Akt1 [1]
(Cell-free assay)
Akt3 [1]
(Cell-free assay)
Akt2 [1]
(Cell-free assay)
5 nM 8 nM 18 nM
In vitro

Testing against a broad panel of 230 kinases, GDC-0068 only inhibits 3 kinases by >70% at 1 μM concentration (PRKG1α, PRKG1β, and p70S6K, with IC50 of 98 nM, 69 nM, and 860 nM, respectively). GDC-0068 displays >100-fold selectivity for Akt over PKA with IC50 of 3.1 μM. In LNCaP, PC3 and BT474M1 cells, GDC-0068 treatment inhibits the phosphorylation of the Akt substrate, PRAS40 with IC50 of 157 nM, 197 nM, and 208 nM, respectively. Furthermore, GDC-0068 selectively inhibits cell cycle progression and viability of cancer cell lines driven by Akt signaling, including those with defects in the tumor suppressor PTEN, oncogenic mutations in PIK3CA, and amplification of HER2, with strongest effects in HER2+ and Luminal subtypes. [1-4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HCC70  NYi5OFdnTnWwY4Tpc44hSXO|YYm= MnnmNUDPxE1? MUeyOEBp NVK5RYJJcW6lcnXhd4V{KHSqZTDhZpVv\GGwY3Wgc4YhUEWUMzDhcoQhcW6mdXPld{B1cGVicHjvd5Bpd3K7bHH0bY9vKCijY4TpeoF1cW:wKTDv[kBjd3SqIFXHSnIh[W6mIFjFVlM> M1H6XlI1PjZ5M{e2
MDA-MB-468  NEHwWVdHfW6ldHnvckBCe3OjeR?= MlLXNUDPxE1? MV[yOEBp NELOZlRqdmO{ZXHz[ZMhfGinIHHieY5l[W6lZTDv[kBJTVJ| NYHMb|F7OjR4NkezO|Y>
HCC70  M4Hibmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fWclEh|ryP MnvUOUBl M1rzU4VvcGGwY3XzJJRp\SCjboTpdJJwdGmoZYLheIl3\SC{ZYPwc45{\Q>? MXOyOFY3PzN5Nh?=
MDA-MB-468  M3XEdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVGxJO69VQ>? MVS1JIQ> NVrSbog3\W6qYX7j[ZMhfGinIHHueIlxem:uaX\ldoF1cX[nIILld5BwdnOn MkDWNlQ3Pjd|N{[=
PC-3 NFvRdlZHfW6ldHnvckBCe3OjeR?= MnS3NE4xODN6LUKuOUDPxE1? NEfQUmIyKGh? M3PTbGROW09? NIjVd5hqdmS3Y3XzJIEh\G:|ZT3k[ZBmdmSnboSgbY5kemWjc3WgbY4hSWu2IIDoc5NxcG:{eXzheIlwdiCjdDDic5RpKFSqckOwPOKhMFR|MEipJIFv\CCVZYK0O|M> MX[yN|I5PzV4Mx?=
BT474M1 M1Xy[2Z2dmO2aX;uJGF{e2G7 MW[wMlAxOzhvMj61JO69VQ>? MV6xJIg> NGnRe5ZFVVOR NGmzfYNqdmS3Y3XzJIEh\G:|ZT3k[ZBmdmSnboSgbY5kemWjc3WgbY4hSWu2IIDoc5NxcG:{eXzheIlwdiCjdDDic5RpKFSqckOwPOKhMFR|MEipJIFv\CCVZYK0O|M> MWGyN|I5PzV4Mx?=
IGROV-1 MVPGeY5kfGmxbjDBd5NigQ>? MXiwMlAxOzhvMj61JO69VQ>? M{TxRlEhcA>? MkXySG1UVw>? MV;pcoR2[2W|IHGg[I9{\S2mZYDlcoRmdnRiaX7jdoVie2ViaX6gRYt1KHCqb4PwbI9zgWyjdHnvckBifCCkb4ToJHRpejNyONMgLHQ{ODhrIHHu[EBU\XJ2N{O= NWi2fVRxOjN{OEe1OlM>
PC-3 NE\w[YZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHTdoxPOS93L{GwJO69VQ>? MkSzNlQwPDhxN{KgbC=> NYq4UIk6TE2VTx?= M2\0UYRwe2VvZHXw[Y5l\W62bImgbY5kemWjc3XzJJRp\SCJMPMAl2cyyqCyaHHz[UBxd3C3bHH0bY9vyqB? MlnKNlMzQDd3NkO=
MCF7-neo/HER2 NXT5O3hRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVX1fJlJOS93L{GwJO69VQ>? MVmyOE81QC95MjDo NGDjNnRFVVOR NGXFZmJld3OnLXTldIVv\GWwdHz5JIlv[3KnYYPld{B1cGViR{FihLNIOcLicHjhd4UheG:ydXzheIlwdsLi NYC2ZnlPOjN{OEe1OlM>
BT474M1 MoPOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGLjfGQyNzVxMUCg{txO Mnq2NlQwPDhxN{KgbC=> MoW4SG1UVw>? MlzT[I9{\S2mZYDlcoRmdnSueTDpcoNz\WG|ZYOgeIhmKEdy4pETS|HDqHCqYYPlJJBweHWuYYTpc47DqA>? M3HWRVI{Ojh5NU[z
PC-3 NX62W2hvSXCxcITvd4l{KEG|c3H5 NYjlb3V4OS93L{GwJO69VQ>? NVmzXmlVOTVxNEivO|IhcA>? NESzOoRFVVOR NYHjU3lq[2G3c3XzJIEh\G:|ZT2gZY5lKHSrbXWt[IVx\W6mZX70JIlv[3KnYYPlJIlvKGGyb4D0c5Rq[yCjbnSgcoVkem:2aXOgdI9xfWyjdHnvcpM> MmXzNlMzQDd3NkO=
MCF7-neo/HER2 MnHGRZBweHSxc3nzJGF{e2G7 MkXYNU82NzFyIN88US=> NUnXXZhMOTVxNEivO|IhcA>? NYK4V3I2TE2VTx?= MWLjZZV{\XNiYTDkc5NmNSCjbnSgeIlu\S2mZYDlcoRmdnRiaX7jdoVie2ViaX6gZZBweHSxdHnjJIFv\CCwZXPyc5Rq[yCyb4D1cIF1cW:wcx?= NVvBU2NYOjN{OEe1OlM>
BT474M1 MkHkRZBweHSxc3nzJGF{e2G7 M2nUWFEwPS9zMDFOwG0> Mn7QNVUwPDhxN{KgbC=> NF33VnNFVVOR NUThUYQ2[2G3c3XzJIEh\G:|ZT2gZY5lKHSrbXWt[IVx\W6mZX70JIlv[3KnYYPlJIlvKGGyb4D0c5Rq[yCjbnSgcoVkem:2aXOgdI9xfWyjdHnvcpM> MUWyN|I5PzV4Mx?=

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot

PubMed: 30185800     

Western blotting analysis of PUMA expression in various colon cancer cell lines treated with 10 μM ipatasertib for 24 h.

p-AKT / AKT / p-FoxO3a / FoxO3a / p-p65 / p65 ; 

PubMed: 30185800     

The expressions of P-Akt (S473), P-FoxO3a (S253), P-p65(S536), and PUMA were detected after the treatment of 10 μM ipatasertib in HCT116 at 0, 6, 12, and 24 h after 10 μM ipatasertib treatment. 

Noxa / Bid / Bad / Bim / Bcl-2 / Bcl-xl / Mcl-1; 

PubMed: 30185800     

Noxa, Bid, Bad, Bim, Bcl-2, Bcl-XL, Mcl-1 were detected in HCT-116 cells after ipatasertib for 24 h. 


PubMed: 30185800     

(a, c, e) Western blotting analysis of PUMA and C-Caspase3 expression after the treatment of 10 μM ipatasertib in combination with (a) 20 mg/ml 5-FU or (c) 40 μM Cisplatin or (e) 20 mM Regorafenib alone, or their combinations for 24 h in HCT116. 

p-PRAS40(T246) / PRAS40 / p-ERK / ERK / pFOXO1 / pFOXO3a / pGSK3b(S9) / pAS160(S318) / pBAD(S136) / pS6 / p4E-BP1; 

PubMed: 26469692     

MDA-MB 453 breast cancer cell line (PIK3CAH1047R; Her2 amp) were treated with various concentrations (1 = 0, 2 = 0.012, 3 = 0.037, 4 = 0.11, 5 = 0.33, and 6 = 1 μM) of ARQ 092, ARQ 751, MK-2206 or GDC-0068 for 2 hours. pAKT(S473), pAKT(T308), pPRAS40(T246), pFOXO1(T24) /3a(T36), pGSK3β(S9), pAS160(S318), pBAD(S136), pS6(S235/236) and p4E-BP1(S65) and phospho ERK were assessed by western blot analysis.

30185800 26469692
In vivo Oral administration of GDC-0068 in PC3 prostate tumor xenografts model induces down-regulation of p-PRAS40. In BT474-Tr xenografts, GDC-0068 treatment reduces pS6 and peIF4G levels, re-localizes FOXO3a to nucleus, and induces feedback upregulation of HER3 and pERK. Administration of GDC-0068 exhibits potent antitumor efficacy in multiple xenograft tumor models, including the PTEN-deficient prostate cancer models LNCaP and PC3, the PIK3CA H1047R mutant breast cancer model KPL-4, and MCF7-neo/HER2 tumor model. [1-4]


Animal Research:[1]
- Collapse
  • Animal Models: Female nude mice bearing LNCaP, PC3, KPL-4, or MCF7 tumor xenografts
  • Formulation: Formulated in 0.5% methylcellulose/0.2% Tween-80
  • Dosages: ~100 mg/kg/day
  • Administration: Orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 92 mg/mL (200.87 mM)
Ethanol 92 mg/mL (200.87 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 458


CAS No. 1001264-89-6
Storage powder
in solvent
Synonyms RG7440

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

Akt Signaling Pathway Map

Akt Inhibitors with Unique Features

Related Akt Products

Tags: buy Ipatasertib (GDC-0068) | Ipatasertib (GDC-0068) supplier | purchase Ipatasertib (GDC-0068) | Ipatasertib (GDC-0068) cost | Ipatasertib (GDC-0068) manufacturer | order Ipatasertib (GDC-0068) | Ipatasertib (GDC-0068) distributor
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID