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
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Cited by 27 Publications

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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  MV7GeY5kfGmxbjDBd5NigQ>? NYLvc3M4OSEQvF2= MkDnNlQhcA>? NIPhR2pqdmO{ZXHz[ZMhfGinIHHieY5l[W6lZTDv[kBJTVJ|IHHu[EBqdmS3Y3XzJJRp\SCyaH;zdIhwenmuYYTpc44hMGGldHn2ZZRqd25rIH;mJIJwfGhiRVfGVkBidmRiSFXSNy=> MkHNNlQ3Pjd|N{[=
MDA-MB-468  NWLI[IJQTnWwY4Tpc44hSXO|YYm= NHjD[3cyKM7:TR?= NWi4XY8{OjRiaB?= NY[2So5QcW6lcnXhd4V{KHSqZTDhZpVv\GGwY3Wgc4YhUEWUMx?= NUXtepJCOjR4NkezO|Y>
HCC70  M1nSWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWrKWZJwOSEQvF2= MVu1JIQ> M{HWT4VvcGGwY3XzJJRp\SCjboTpdJJwdGmoZYLheIl3\SC{ZYPwc45{\Q>? MXKyOFY3PzN5Nh?=
MDA-MB-468  NEH6W45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm[3NUDPxE1? MVi1JIQ> Mljz[Y5p[W6lZYOgeIhmKGGwdHnwdo9tcW[ncnH0bZZmKHKnc4DvcpNm M3nlR|I1PjZ5M{e2
PC-3 MVHGeY5kfGmxbjDBd5NigQ>? M3fmdlAvODB|OD2yMlUh|ryP NFWwNFEyKGh? MWPEUXNQ M1LOVYlv\HWlZYOgZUBld3OnLXTldIVv\GWwdDDpcoNz\WG|ZTDpckBCc3RicHjvd5Bpd3K7bHH0bY9vKGG2IHLveIghXGi{M{C4xsApXDNyODmgZY5lKFOnckS3Ny=> MkSxNlMzQDd3NkO=
BT474M1 NWG3SoY{TnWwY4Tpc44hSXO|YYm= NUntR3dTOC5yMEO4MVIvPSEQvF2= NXrBXVVGOSCq M1r6ZmROW09? NEHFd|NqdmS3Y3XzJIEh\G:|ZT3k[ZBmdmSnboSgbY5kemWjc3WgbY4hSWu2IIDoc5NxcG:{eXzheIlwdiCjdDDic5RpKFSqckOwPOKhMFR|MEipJIFv\CCVZYK0O|M> NXnjeGt6OjN{OEe1OlM>
IGROV-1 M4HwOmZ2dmO2aX;uJGF{e2G7 MmTsNE4xODN6LUKuOUDPxE1? M4W4WlEhcA>? NF7uNY9FVVOR MVrpcoR2[2W|IHGg[I9{\S2mZYDlcoRmdnRiaX7jdoVie2ViaX6gRYt1KHCqb4PwbI9zgWyjdHnvckBifCCkb4ToJHRpejNyONMgLHQ{ODhrIHHu[EBU\XJ2N{O= NFr4XGQzOzJ6N{W2Ny=>
PC-3 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jnZVEwPS9zMDFOwG0> NVzyZYtuOjRxNEivO|IhcA>? NUjpVYxoTE2VTx?= M2XOdYRwe2VvZHXw[Y5l\W62bImgbY5kemWjc3XzJJRp\SCJMPMAl2cyyqCyaHHz[UBxd3C3bHH0bY9vyqB? NITRNm0zOzJ6N{W2Ny=>
MCF7-neo/HER2 M33PO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUixM|UwOTBizszN MYKyOE81QC95MjDo NInHfFNFVVOR M1TjR4Rwe2VvZHXw[Y5l\W62bImgbY5kemWjc3XzJJRp\SCJMPMAl2cyyqCyaHHz[UBxd3C3bHH0bY9vyqB? M{DjVFI{Ojh5NU[z
BT474M1 NHzKR4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFv6RmgyNzVxMUCg{txO NYLrO2dMOjRxNEivO|IhcA>? NEHQPZJFVVOR Mkiy[I9{\S2mZYDlcoRmdnSueTDpcoNz\WG|ZYOgeIhmKEdy4pETS|HDqHCqYYPlJJBweHWuYYTpc47DqA>? MnK1NlMzQDd3NkO=
PC-3 NWXlN2NESXCxcITvd4l{KEG|c3H5 NYfJTmRUOS93L{GwJO69VQ>? NWjyRYNIOTVxNEivO|IhcA>? M1S1S2ROW09? MV;jZZV{\XNiYTDkc5NmNSCjbnSgeIlu\S2mZYDlcoRmdnRiaX7jdoVie2ViaX6gZZBweHSxdHnjJIFv\CCwZXPyc5Rq[yCyb4D1cIF1cW:wcx?= NYnHZWk6OjN{OEe1OlM>
MCF7-neo/HER2 MXTBdI9xfG:|aYOgRZN{[Xl? MkDrNU82NzFyIN88US=> NUKyN5F2OTVxNEivO|IhcA>? M{Do[mROW09? M1PQSYNifXOnczDhJIRwe2VvIHHu[EB1cW2nLXTldIVv\GWwdDDpcoNz\WG|ZTDpckBieG:ydH;0bYMh[W6mIH7lZ5JwfGmlIIDvdJVt[XSrb37z NWnR[JJDOjN{OEe1OlM>
BT474M1 Mm[xRZBweHSxc3nzJGF{e2G7 M1zzclEwPS9zMDFOwG0> M2fGPVE2NzR6L{eyJIg> MUXEUXNQ Mnr2Z4F2e2W|IHGg[I9{\S1iYX7kJJRqdWVvZHXw[Y5l\W62IHnuZ5Jm[XOnIHnuJIFxd3C2b4TpZ{BidmRibnXjdo91cWNicH;weYxifGmxboO= MU[yN|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]
- 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
Formula

C24H32ClN5O2

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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID