Ipatasertib (GDC-0068)

For research use only.

Catalog No.S2808 Synonyms: RG7440

67 publications

Ipatasertib (GDC-0068) Chemical Structure

CAS No. 1001264-89-6

Ipatasertib (GDC-0068, RG7440) 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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Selleck's Ipatasertib (GDC-0068) has been cited by 67 publications

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Biological Activity

Description Ipatasertib (GDC-0068, RG7440) 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  MWfGeY5kfGmxbjDBd5NigQ>? NIfRO2wyKM7:TR?= NG[4NWczPCCq NWTkVHJtcW6lcnXhd4V{KHSqZTDhZpVv\GGwY3Wgc4YhUEWUMzDhcoQhcW6mdXPld{B1cGVicHjvd5Bpd3K7bHH0bY9vKCijY4TpeoF1cW:wKTDv[kBjd3SqIFXHSnIh[W6mIFjFVlM> NULa[5BLOjR4NkezO|Y>
MDA-MB-468  M12wV2Z2dmO2aX;uJGF{e2G7 MWixJO69VQ>? M2nVeVI1KGh? MV;pcoNz\WG|ZYOgeIhmKGGkdX7kZY5k\SCxZjDISXI{ M3nWXFI1PjZ5M{e2
HCC70  NWezTpFLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPhZmQyKM7:TR?= NWPP[5FQPSCm MXPlcohidmOnczD0bIUh[W62aYDyc4xq\mW{YYTpeoUhemW|cH;ud4U> MW[yOFY3PzN5Nh?=
MDA-MB-468  NW\iZlY4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzDZWYyKM7:TR?= NX7ab5p6PSCm M1LPdYVvcGGwY3XzJJRp\SCjboTpdJJwdGmoZYLheIl3\SC{ZYPwc45{\Q>? M4PWV|I1PjZ5M{e2
PC-3 NHLnTIRHfW6ldHnvckBCe3OjeR?= Mn\SNE4xODN6LUKuOUDPxE1? NFLIcVkyKGh? M3GwdGROW09? M2XWSolv\HWlZYOgZUBld3OnLXTldIVv\GWwdDDpcoNz\WG|ZTDpckBCc3RicHjvd5Bpd3K7bHH0bY9vKGG2IHLveIghXGi{M{C4xsApXDNyODmgZY5lKFOnckS3Ny=> MWKyN|I5PzV4Mx?=
BT474M1 NYrwd4FDTnWwY4Tpc44hSXO|YYm= M17GbVAvODB|OD2yMlUh|ryP Ml7xNUBp MkW5SG1UVw>? M2Hye4lv\HWlZYOgZUBld3OnLXTldIVv\GWwdDDpcoNz\WG|ZTDpckBCc3RicHjvd5Bpd3K7bHH0bY9vKGG2IHLveIghXGi{M{C4xsApXDNyODmgZY5lKFOnckS3Ny=> M4\4OlI{Ojh5NU[z
IGROV-1 Mnz2SpVv[3Srb36gRZN{[Xl? NHH0WJkxNjByM{itNk42KM7:TR?= MXyxJIg> NVvwSoNSTE2VTx?= M1jYWolv\HWlZYOgZUBld3OnLXTldIVv\GWwdDDpcoNz\WG|ZTDpckBCc3RicHjvd5Bpd3K7bHH0bY9vKGG2IHLveIghXGi{M{C4xsApXDNyODmgZY5lKFOnckS3Ny=> MYeyN|I5PzV4Mx?=
PC-3 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEWx[ZAyNzVxMUCg{txO MoXkNlQwPDhxN{KgbC=> NX7rOWR5TE2VTx?= NUjJem5E\G:|ZT3k[ZBmdmSnboTsfUBqdmO{ZXHz[ZMhfGinIFew5qCUTzIEoIDoZZNmKHCxcIXsZZRqd28EoB?= MWmyN|I5PzV4Mx?=
MCF7-neo/HER2 NUfBe3lkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX7WeY1WOS93L{GwJO69VQ>? NIe0PZgzPC92OD:3NkBp NV;6W5RYTE2VTx?= MnP6[I9{\S2mZYDlcoRmdnSueTDpcoNz\WG|ZYOgeIhmKEdy4pETS|HDqHCqYYPlJJBweHWuYYTpc47DqA>? NUfGclBuOjN{OEe1OlM>
BT474M1 M1vLOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\EUlEwPS9zMDFOwG0> M2XTWFI1NzR6L{eyJIg> M3m1UGROW09? MWXkc5NmNWSncHXu[IVvfGy7IHnuZ5Jm[XOnczD0bIUhTzEkgKPHNeKheGijc3WgdI9xfWyjdHnvcuKh M{nCfFI{Ojh5NU[z
PC-3 NXznUVBLSXCxcITvd4l{KEG|c3H5 NV\LO25IOS93L{GwJO69VQ>? MkC4NVUwPDhxN{KgbC=> NVLreollTE2VTx?= MmS0Z4F2e2W|IHGg[I9{\S1iYX7kJJRqdWVvZHXw[Y5l\W62IHnuZ5Jm[XOnIHnuJIFxd3C2b4TpZ{BidmRibnXjdo91cWNicH;weYxifGmxboO= NEj4PGszOzJ6N{W2Ny=>
MCF7-neo/HER2 Ml7pRZBweHSxc3nzJGF{e2G7 MXuxM|UwOTBizszN M1vzNVE2NzR6L{eyJIg> MXnEUXNQ M3m0O4NifXOnczDhJIRwe2VvIHHu[EB1cW2nLXTldIVv\GWwdDDpcoNz\WG|ZTDpckBieG:ydH;0bYMh[W6mIH7lZ5JwfGmlIIDvdJVt[XSrb37z NEfn[nYzOzJ6N{W2Ny=>
BT474M1 NVzq[24{SXCxcITvd4l{KEG|c3H5 NESyXXUyNzVxMUCg{txO NH\uTlYyPS92OD:3NkBp M{XQfmROW09? NInGb29k[XW|ZYOgZUBld3OnLTDhcoQhfGmvZT3k[ZBmdmSnboSgbY5kemWjc3WgbY4h[XCxcITveIlkKGGwZDDu[YNzd3SrYzDwc5B2dGG2aX;udy=> NGPRXWwzOzJ6N{W2Ny=>

... 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]
- Collapse
  • Animal Models: Female nude mice bearing LNCaP, PC3, KPL-4, or MCF7 tumor xenografts
  • Dosages: ~100 mg/kg/day
  • Administration: Orally
    (Only for Reference)

Solubility (25°C)

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

* 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
Smiles CC1CC(C2=C1C(=NC=N2)N3CCN(CC3)C(=O)C(CNC(C)C)C4=CC=C(C=C4)Cl)O

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01090960 Completed Drug: GDC-0068 Solid Cancers Genentech Inc. March 2010 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID