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

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1 Customer Review

  • Inhibition of AKT signaling abolishes MKK4 phosphorylation on Ser78 in injured axons. Cultures of sensory neurons were treated with 5 µM MK-2206 or 5 µM GDC-0068 for 1 hr prior to axotomy. Axonal proteins harvested at indicated time points after axotomy were subjected to immunoblot analysis.

    Cell, 2015, 160(1-2): 161-76 . Ipatasertib (GDC-0068) purchased from Selleck.

Purity & Quality Control

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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.
Targets
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  M2HlU2Z2dmO2aX;uJGF{e2G7 M4KxSlEh|ryP M{jke|I1KGh? MXvpcoNz\WG|ZYOgeIhmKGGkdX7kZY5k\SCxZjDISXI{KGGwZDDpcoR2[2W|IITo[UBxcG:|cHjvdplt[XSrb36gLIFkfGm4YYTpc44qKG:oIHLveIghTUeIUjDhcoQhUEWUMx?= M3f1XVI1PjZ5M{e2
MDA-MB-468  MYjGeY5kfGmxbjDBd5NigQ>? NIPZcI0yKM7:TR?= NUnSUWY3OjRiaB?= NY[3Now{cW6lcnXhd4V{KHSqZTDhZpVv\GGwY3Wgc4YhUEWUMx?= M320[VI1PjZ5M{e2
HCC70  NV3zU|ZlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPVSGIyKM7:TR?= NETCXVY2KGR? M3:3XoVvcGGwY3XzJJRp\SCjboTpdJJwdGmoZYLheIl3\SC{ZYPwc45{\Q>? M{Gx[FI1PjZ5M{e2
MDA-MB-468  MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWexJO69VQ>? NUX0THQ4PSCm M3nnfoVvcGGwY3XzJJRp\SCjboTpdJJwdGmoZYLheIl3\SC{ZYPwc45{\Q>? MW[yOFY3PzN5Nh?=
PC-3 MlTYSpVv[3Srb36gRZN{[Xl? NX7ub4VkOC5yMEO4MVIvPSEQvF2= NWrpOJR5OSCq Ml7lSG1UVw>? MmD1bY5lfWOnczDhJIRwe2VvZHXw[Y5l\W62IHnuZ5Jm[XOnIHnuJGFsfCCyaH;zdIhwenmuYYTpc44h[XRiYn;0bEBVcHJ|MElCpEhVOzB6KTDhcoQhW2W{NEez MXmyN|I5PzV4Mx?=
BT474M1 NFfjdG9HfW6ldHnvckBCe3OjeR?= Mn3QNE4xODN6LUKuOUDPxE1? MlHjNUBp NF25cHVFVVOR M3zIV4lv\HWlZYOgZUBld3OnLXTldIVv\GWwdDDpcoNz\WG|ZTDpckBCc3RicHjvd5Bpd3K7bHH0bY9vKGG2IHLveIghXGi{M{C4xsApXDNyODmgZY5lKFOnckS3Ny=> NGfa[5czOzJ6N{W2Ny=>
IGROV-1 M3\tVWZ2dmO2aX;uJGF{e2G7 NV;ld3hYOC5yMEO4MVIvPSEQvF2= M2r1N|EhcA>? NHr5UmlFVVOR NVjnbY9IcW6mdXPld{BiKGSxc3Wt[IVx\W6mZX70JIlv[3KnYYPlJIlvKEGtdDDwbI9{eGixconsZZRqd25iYYSgZo91cCCWaIKzNFjDqCiWM{C4LUBidmRiU3XyOFc{ M4W3UVI{Ojh5NU[z
PC-3 M2n3Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3P6W|EwPS9zMDFOwG0> MlfWNlQwPDhxN{KgbC=> M3LMTGROW09? NVr3boFb\G:|ZT3k[ZBmdmSnboTsfUBqdmO{ZXHz[ZMhfGinIFew5qCUTzIEoIDoZZNmKHCxcIXsZZRqd28EoB?= NXPkXoxqOjN{OEe1OlM>
MCF7-neo/HER2 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1LQfFEwPS9zMDFOwG0> NIXSbW8zPC92OD:3NkBp NW\XeVlRTE2VTx?= NXzEeJFu\G:|ZT3k[ZBmdmSnboTsfUBqdmO{ZXHz[ZMhfGinIFew5qCUTzIEoIDoZZNmKHCxcIXsZZRqd28EoB?= NGC3VnozOzJ6N{W2Ny=>
BT474M1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWf4bVdWOS93L{GwJO69VQ>? MXGyOE81QC95MjDo NEK0PFJFVVOR M2jzVoRwe2VvZHXw[Y5l\W62bImgbY5kemWjc3XzJJRp\SCJMPMAl2cyyqCyaHHz[UBxd3C3bHH0bY9vyqB? M4rJRVI{Ojh5NU[z
PC-3 M1;vRmFxd3C2b4Ppd{BCe3OjeR?= MojWNU82NzFyIN88US=> MW[xOU81QC95MjDo NFLDV5NFVVOR MlTYZ4F2e2W|IHGg[I9{\S1iYX7kJJRqdWVvZHXw[Y5l\W62IHnuZ5Jm[XOnIHnuJIFxd3C2b4TpZ{BidmRibnXjdo91cWNicH;weYxifGmxboO= MmHpNlMzQDd3NkO=
MCF7-neo/HER2 MXfBdI9xfG:|aYOgRZN{[Xl? NVjXfVhTOS93L{GwJO69VQ>? MVmxOU81QC95MjDo MVnEUXNQ M4DMfYNifXOnczDhJIRwe2VvIHHu[EB1cW2nLXTldIVv\GWwdDDpcoNz\WG|ZTDpckBieG:ydH;0bYMh[W6mIH7lZ5JwfGmlIIDvdJVt[XSrb37z NXLzWFJXOjN{OEe1OlM>
BT474M1 MUPBdI9xfG:|aYOgRZN{[Xl? NV\JSlZLOS93L{GwJO69VQ>? MoGxNVUwPDhxN{KgbC=> M{P4e2ROW09? MofOZ4F2e2W|IHGg[I9{\S1iYX7kJJRqdWVvZHXw[Y5l\W62IHnuZ5Jm[XOnIHnuJIFxd3C2b4TpZ{BidmRibnXjdo91cWNicH;weYxifGmxboO= MXOyN|I5PzV4Mx?=

... Click to View More Cell Line Experimental Data

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]

Protocol

Animal Research
+ Expand
  • 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 <1 mg/mL

* 1 mg/ml means slightly soluble or 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
Formula

C24H32ClN5O2

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

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01896531 Active, not recruiting Gastric Cancer Genentech, Inc. August 2013 Phase 2
NCT01485861 Active, not recruiting Prostate Cancer Genentech, Inc. December 2011 Phase 1|Phase 2
NCT01362374 Active, not recruiting Solid Cancers Genentech, Inc. July 2011 Phase 1
NCT01090960 Completed Solid Cancers Genentech, Inc. March 2010 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID