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.

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In DMSO USD 378 In stock
USD 270 In stock
USD 370 In stock
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Cited by 13 Publications

3 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.

  • The functional significance of the PI3K/Akt pathway in CCR5-mediated DNA damage signaling was assessed using the ATP-competitive, small-molecule pan-Akt inhibitor (ipatasertib) and or the CCR5 inhibitor Maraviroc in doxorubicin-treated cells. Western blot analysis was conducted as shown for SUM-159 cells (B) and MDA-MB-175VII (doxorubicin-resistant breast cancer cells) (D).

    Clin Cancer Res, 2018, 78(7):1657-1671. 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.

Purity & Quality Control

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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  MoHHSpVv[3Srb36gRZN{[Xl? NG[5dJgyKM7:TR?= M{PWSVI1KGh? MW\pcoNz\WG|ZYOgeIhmKGGkdX7kZY5k\SCxZjDISXI{KGGwZDDpcoR2[2W|IITo[UBxcG:|cHjvdplt[XSrb36gLIFkfGm4YYTpc44qKG:oIHLveIghTUeIUjDhcoQhUEWUMx?= MXSyOFY3PzN5Nh?=
MDA-MB-468  Mm[4SpVv[3Srb36gRZN{[Xl? MkXENUDPxE1? NFLkXGIzPCCq NH:0XVBqdmO{ZXHz[ZMhfGinIHHieY5l[W6lZTDv[kBJTVJ| M2\ZZ|I1PjZ5M{e2
HCC70  MknGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nveFEh|ryP NH7pbII2KGR? NV\mXHV4\W6qYX7j[ZMhfGinIHHueIlxem:uaX\ldoF1cX[nIILld5BwdnOn M2rESFI1PjZ5M{e2
MDA-MB-468  NFTlOIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnW5NUDPxE1? NEmxVGI2KGR? M2DVfYVvcGGwY3XzJJRp\SCjboTpdJJwdGmoZYLheIl3\SC{ZYPwc45{\Q>? NGTndVQzPDZ4N{O3Oi=>
PC-3 NHnpbGNHfW6ldHnvckBCe3OjeR?= MXSwMlAxOzhvMj61JO69VQ>? Moq1NUBp Mn:zSG1UVw>? NUWxb5JCcW6mdXPld{BiKGSxc3Wt[IVx\W6mZX70JIlv[3KnYYPlJIlvKEGtdDDwbI9{eGixconsZZRqd25iYYSgZo91cCCWaIKzNFjDqCiWM{C4LUBidmRiU3XyOFc{ M4m3eFI{Ojh5NU[z
BT474M1 NGPhbpRHfW6ldHnvckBCe3OjeR?= NEK0TYgxNjByM{itNk42KM7:TR?= M1TKNVEhcA>? NF\zdpFFVVOR MlPobY5lfWOnczDhJIRwe2VvZHXw[Y5l\W62IHnuZ5Jm[XOnIHnuJGFsfCCyaH;zdIhwenmuYYTpc44h[XRiYn;0bEBVcHJ|MElCpEhVOzB6KTDhcoQhW2W{NEez NFXrXoszOzJ6N{W2Ny=>
IGROV-1 NYf0c2hWTnWwY4Tpc44hSXO|YYm= NUDpTZg5OC5yMEO4MVIvPSEQvF2= MWmxJIg> NVvJVYtDTE2VTx?= M2e2Rolv\HWlZYOgZUBld3OnLXTldIVv\GWwdDDpcoNz\WG|ZTDpckBCc3RicHjvd5Bpd3K7bHH0bY9vKGG2IHLveIghXGi{M{C4xsApXDNyODmgZY5lKFOnckS3Ny=> MYqyN|I5PzV4Mx?=
PC-3 M1PBTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYmxM|UwOTBizszN M1e5OFI1NzR6L{eyJIg> MWHEUXNQ MWLkc5NmNWSncHXu[IVvfGy7IHnuZ5Jm[XOnczD0bIUhTzEkgKPHNeKheGijc3WgdI9xfWyjdHnvcuKh MXeyN|I5PzV4Mx?=
MCF7-neo/HER2 NYCxfYV2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjyNU82NzFyIN88US=> NIjYVZEzPC92OD:3NkBp MoTNSG1UVw>? M1rQdIRwe2VvZHXw[Y5l\W62bImgbY5kemWjc3XzJJRp\SCJMPMAl2cyyqCyaHHz[UBxd3C3bHH0bY9vyqB? NInsNGkzOzJ6N{W2Ny=>
BT474M1 NVvvV|E3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXOxM|UwOTBizszN M{PwelI1NzR6L{eyJIg> NIj1b|RFVVOR M2rRfIRwe2VvZHXw[Y5l\W62bImgbY5kemWjc3XzJJRp\SCJMPMAl2cyyqCyaHHz[UBxd3C3bHH0bY9vyqB? NUPwSHVFOjN{OEe1OlM>
PC-3 MlzLRZBweHSxc3nzJGF{e2G7 NXXGTnBrOS93L{GwJO69VQ>? MVSxOU81QC95MjDo MWnEUXNQ M1fnfoNifXOnczDhJIRwe2VvIHHu[EB1cW2nLXTldIVv\GWwdDDpcoNz\WG|ZTDpckBieG:ydH;0bYMh[W6mIH7lZ5JwfGmlIIDvdJVt[XSrb37z NIjkXY0zOzJ6N{W2Ny=>
MCF7-neo/HER2 NVS4WoxwSXCxcITvd4l{KEG|c3H5 NEPvb2oyNzVxMUCg{txO NIfoVpAyPS92OD:3NkBp NHr5VJhFVVOR NECz[HJk[XW|ZYOgZUBld3OnLTDhcoQhfGmvZT3k[ZBmdmSnboSgbY5kemWjc3WgbY4h[XCxcITveIlkKGGwZDDu[YNzd3SrYzDwc5B2dGG2aX;udy=> M1rMWFI{Ojh5NU[z
BT474M1 NHjvZW1CeG:ydH;zbZMhSXO|YYm= NGHYV4oyNzVxMUCg{txO NHraU3UyPS92OD:3NkBp NXGzVXBbTE2VTx?= NX6ydmp5[2G3c3XzJIEh\G:|ZT2gZY5lKHSrbXWt[IVx\W6mZX70JIlv[3KnYYPlJIlvKGGyb4D0c5Rq[yCjbnSgcoVkem:2aXOgdI9xfWyjdHnvcpM> MYKyN|I5PzV4Mx?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
PUMA ; 

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. 

cleaved-caspase3; 

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]

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
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 31 2013 Phase 2
NCT01896531 Active not recruiting Gastric Cancer Genentech Inc. August 31 2013 Phase 2
NCT01090960 Completed Solid Cancers Genentech Inc. March 2010 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