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GDC-0068 (RG7440)

Pan-AKT inhibitor,highly selective CAS# 1001264-89-6

GDC-0068 (RG7440)

Catalog No. BCC1271----Order now to get a substantial discount!

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Chemical structure

GDC-0068 (RG7440)

3D structure

Chemical Properties of GDC-0068 (RG7440)

Cas No. 1001264-89-6 SDF Download SDF
PubChem ID 24788740 Appearance Powder
Formula C24H32ClN5O2 M.Wt 458
Type of Compound N/A Storage Desiccate at -20°C
Synonyms Ipatasertib; RG7440
Solubility DMSO : ≥ 28 mg/mL (61.14 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name (2S)-2-(4-chlorophenyl)-1-[4-[(5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl]piperazin-1-yl]-3-(propan-2-ylamino)propan-1-one
SMILES CC1CC(C2=C1C(=NC=N2)N3CCN(CC3)C(=O)C(CNC(C)C)C4=CC=C(C=C4)Cl)O
Standard InChIKey GRZXWCHAXNAUHY-NSISKUIASA-N
Standard InChI InChI=1S/C24H32ClN5O2/c1-15(2)26-13-19(17-4-6-18(25)7-5-17)24(32)30-10-8-29(9-11-30)23-21-16(3)12-20(31)22(21)27-14-28-23/h4-7,14-16,19-20,26,31H,8-13H2,1-3H3/t16-,19-,20-/m1/s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of GDC-0068 (RG7440)

DescriptionIpatasertib (GDC-0068) is a highly selective inhibitor of Akt for Akt1/2/3 with IC50 of 5 nM/18 nM/8 nM, 620-fold selectivity over PKA.
TargetsAkt1Akt2Akt3   
IC505 nM18 nM8 nM    

Protocol

Cell experiment [1]:

Cell lines

PC-3, BT474M1 and IGROV-1 cell lines

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reacting condition

1 h; 25 μmol/L

Applications

The biologic activity of GDC-0068 was evaluated in cell-based assays in vitro . Similar to other ATP-competitive Akt inhibitors, GDC-0068 induced a dose-dependent increase in Akt phosphorylation at both Thr308 (T308) and Ser 473 (S473) residues in all cell lines tested, including lines in which the PI3K/Akt pathway is activated, such as PC-3 (PTEN homozygous deletion mutant, prostate), BT474M1 (PIK3CAK111N mutant and HER2-amplified, breast), IGROV-1 (PTENT319fsX1/Y155C and PIK3CA1069 W, ovarian).

Animal experiment [1]:

Animal models

Nude mice

Dosage form

100 mg//kg; Oral taken

Application

The in vitro sensitivity profile of GDC-0068 was recapitulated in vivo in xenograft models representing a spectrum of cancer types including prostate, breast, ovarian, colorectal, non–small cell lung, glioblastoma, and melanoma. GDC-0068 was typically efficacious in xenograft models in which Akt was activated because of genetic alterations including PTEN loss, PIK3CA mutations/amplifications, or HER2 overexpression. In these models, tumor growth delay, stasis, or regression was achieved at or below 100 mg/kg daily oral dose, which was the maximum dose tested in immunocompromised mice that was well tolerated.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Lin J, Sampath D, Nannini M A, et al. Targeting activated Akt with GDC-0068, a novel selective Akt inhibitor that is efficacious in multiple tumor models[J]. Clinical Cancer Research, 2013, 19(7): 1760-1772.

GDC-0068 (RG7440) Dilution Calculator

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Preparing Stock Solutions of GDC-0068 (RG7440)

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.1834 mL 10.917 mL 21.8341 mL 43.6681 mL 54.5852 mL
5 mM 0.4367 mL 2.1834 mL 4.3668 mL 8.7336 mL 10.917 mL
10 mM 0.2183 mL 1.0917 mL 2.1834 mL 4.3668 mL 5.4585 mL
50 mM 0.0437 mL 0.2183 mL 0.4367 mL 0.8734 mL 1.0917 mL
100 mM 0.0218 mL 0.1092 mL 0.2183 mL 0.4367 mL 0.5459 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

Research Update of GDC-0068 (RG7440)

1. Evaluation and clinical analyses of downstream targets of the Akt inhibitor GDC-0068. Clin Cancer Res. 2013 Dec 15;19(24):6976-86. doi: 10.1158/1078-0432.CCR-13-0978. Epub 2013 Oct 18.
Abstract
The pharmacodynamics of GDC-0068, an Akt1/2/3 inhibitor, have been studied in preclinical models and patients.
3. Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors. J Med Chem. 2012 Sep 27;55(18):8110-27. Epub 2012 Sep 18.
Abstract
GDC-0068 is an orally-available anticancer agent that dose-dependently exerts pharmacodynamics effects on downstream biomarkers and exhibits a roust antitumor response in xenograft models.

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Background on GDC-0068 (RG7440)

GDC-0068 (RG7440) is a highly selective small molecule inhibitor of Akt with IC50s of 5, 18 and 8 nM for Akt1, Akt2 and Akt3. The PI3K-AKT pathway regulates cell growth, survival and tumorigenesis. GDC-0068 binds to and blocks the activation of AKT, which result in cell cycle arrest, inhibition of tumor cell proliferation and induction of tumor cell death. PI3K-AKT is pathway frequently activated in tumors, thus tumors with PTEN or PI3K mutations, which lead to activation of AKT are with high sensitivity to GDC-0068. GDC-0068 is now used for the treatment of human cancers.

References:

1. Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors. JF Blake, R Xu, JR Bencsik, D Xiao… - Journal of medicinal  2012

2. Lin J, Sampath D, Nannini MA, et al: Targeting activated Akt with GDC-0068, a novel selective Akt inhibitor that is efficacious in multiple tumor models. Clin Canc Res 2013, 19:1760–1772.

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Description

Ipatasertib (GDC-0068) is a highly selective and ATP-competitive pan-Akt inhibitor with IC50s of 5, 18 and 8 nM for Akt1, Akt2 and Akt3, respectively.

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