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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2 Customer Reviews

  • 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.

    In vitro evaluation of BAR activity in A549-BAR cell line. (A) Bioluminescence activity was quantified 1 hour after treatment in response to various compounds at two concentrations (n = 6). (B) Western blotting analysis after 1 hour of treatment showing the expression of pAKT (Ser473), AKT, pPRAS40 (Thr246), RAS40, pGSK3β (Ser9), GSK3β, pEGFR (Tyr1068), EGFR, and β-Actin of whole cell lysates.

    Neoplasia, 2017, 19(4):310-320. Ipatasertib (GDC-0068) purchased from Selleck.

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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  MWXGeY5kfGmxbjDBd5NigQ>? M1\l[|Eh|ryP MVmyOEBp M{fhbYlv[3KnYYPld{B1cGViYXL1coRidmOnIH;mJGhGWjNiYX7kJIlv\HWlZYOgeIhmKHCqb4PwbI9zgWyjdHnvckAp[WO2aY\heIlwdilib3[gZo91cCCHR1\SJIFv\CCKRWKz NFHNeWIzPDZ4N{O3Oi=>
MDA-MB-468  NWXxTGpwTnWwY4Tpc44hSXO|YYm= MYixJO69VQ>? NVzidXUyOjRiaB?= NXvJ[o5vcW6lcnXhd4V{KHSqZTDhZpVv\GGwY3Wgc4YhUEWUMx?= NVzyXlRCOjR4NkezO|Y>
HCC70  NH\aZ2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXWxJO69VQ>? M4LOWFUh\A>? M1H0bYVvcGGwY3XzJJRp\SCjboTpdJJwdGmoZYLheIl3\SC{ZYPwc45{\Q>? MV2yOFY3PzN5Nh?=
MDA-MB-468  NUPpeolqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2L3dFEh|ryP MnvsOUBl NXfzOmNr\W6qYX7j[ZMhfGinIHHueIlxem:uaX\ldoF1cX[nIILld5BwdnOn M4nl[FI1PjZ5M{e2
PC-3 NEC4SGVHfW6ldHnvckBCe3OjeR?= NYn3OY1jOC5yMEO4MVIvPSEQvF2= M1L0W|EhcA>? M4D1UmROW09? NHnMTnRqdmS3Y3XzJIEh\G:|ZT3k[ZBmdmSnboSgbY5kemWjc3WgbY4hSWu2IIDoc5NxcG:{eXzheIlwdiCjdDDic5RpKFSqckOwPOKhMFR|MEipJIFv\CCVZYK0O|M> Ml3RNlMzQDd3NkO=
BT474M1 MUnGeY5kfGmxbjDBd5NigQ>? NFHv[|IxNjByM{itNk42KM7:TR?= MVWxJIg> NFjUZ|BFVVOR NVXvR3p1cW6mdXPld{BiKGSxc3Wt[IVx\W6mZX70JIlv[3KnYYPlJIlvKEGtdDDwbI9{eGixconsZZRqd25iYYSgZo91cCCWaIKzNFjDqCiWM{C4LUBidmRiU3XyOFc{ M4fNblI{Ojh5NU[z
IGROV-1 MWTGeY5kfGmxbjDBd5NigQ>? NIjkZoUxNjByM{itNk42KM7:TR?= M4HhR|EhcA>? NWC2SItFTE2VTx?= MXXpcoR2[2W|IHGg[I9{\S2mZYDlcoRmdnRiaX7jdoVie2ViaX6gRYt1KHCqb4PwbI9zgWyjdHnvckBifCCkb4ToJHRpejNyONMgLHQ{ODhrIHHu[EBU\XJ2N{O= MVKyN|I5PzV4Mx?=
PC-3 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlH1NU82NzFyIN88US=> NHv4VXYzPC92OD:3NkBp NYXHO4dMTE2VTx?= MYnkc5NmNWSncHXu[IVvfGy7IHnuZ5Jm[XOnczD0bIUhTzEkgKPHNeKheGijc3WgdI9xfWyjdHnvcuKh Mkn5NlMzQDd3NkO=
MCF7-neo/HER2 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYS5W28xOS93L{GwJO69VQ>? NIDXclEzPC92OD:3NkBp NUf0NnpqTE2VTx?= MUfkc5NmNWSncHXu[IVvfGy7IHnuZ5Jm[XOnczD0bIUhTzEkgKPHNeKheGijc3WgdI9xfWyjdHnvcuKh M4PSO|I{Ojh5NU[z
BT474M1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYKxM|UwOTBizszN NFL3OWMzPC92OD:3NkBp MU\EUXNQ NHzLXotld3OnLXTldIVv\GWwdHz5JIlv[3KnYYPld{B1cGViR{FihLNIOcLicHjhd4UheG:ydXzheIlwdsLi MnW5NlMzQDd3NkO=
PC-3 NHuw[nlCeG:ydH;zbZMhSXO|YYm= NVroOFU1OS93L{GwJO69VQ>? MUmxOU81QC95MjDo MljJSG1UVw>? Mm\FZ4F2e2W|IHGg[I9{\S1iYX7kJJRqdWVvZHXw[Y5l\W62IHnuZ5Jm[XOnIHnuJIFxd3C2b4TpZ{BidmRibnXjdo91cWNicH;weYxifGmxboO= NXPaRZlUOjN{OEe1OlM>
MCF7-neo/HER2 NVPNWWNwSXCxcITvd4l{KEG|c3H5 MWWxM|UwOTBizszN NFu1XlAyPS92OD:3NkBp MnLrSG1UVw>? NFr0bo1k[XW|ZYOgZUBld3OnLTDhcoQhfGmvZT3k[ZBmdmSnboSgbY5kemWjc3WgbY4h[XCxcITveIlkKGGwZDDu[YNzd3SrYzDwc5B2dGG2aX;udy=> MYeyN|I5PzV4Mx?=
BT474M1 NYe0b2o{SXCxcITvd4l{KEG|c3H5 M2i1d|EwPS9zMDFOwG0> MUexOU81QC95MjDo MnXQSG1UVw>? M{LpVYNifXOnczDhJIRwe2VvIHHu[EB1cW2nLXTldIVv\GWwdDDpcoNz\WG|ZTDpckBieG:ydH;0bYMh[W6mIH7lZ5JwfGmlIIDvdJVt[XSrb37z MViyN|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:[1]
+ 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 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
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