GDC-0068 (RG7440)Pan-AKT inhibitor,highly selective CAS# 1001264-89-6 |
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Quality Control & MSDS
3D structure
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Number of papers citing our products
| 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. |
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| 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. |
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| 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. | ||
| Description | Ipatasertib (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. | |||||
| Targets | Akt1 | Akt2 | Akt3 | |||
| IC50 | 5 nM | 18 nM | 8 nM | |||
| 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
GDC-0068 (RG7440) Molarity Calculator
| 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. | |||||
Abstract
The pharmacodynamics of GDC-0068, an Akt1/2/3 inhibitor, have been studied in preclinical models and patients.
Abstract
The preclinical pharmacology and antitumor activity of GDC-0068, a pan-Akt inhibitor, are described.
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.
Calcutta University
University of Minnesota
University of Maryland School of Medicine
University of Illinois at Chicago
The Ohio State University
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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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