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Apitolisib (GDC-0980)

Cat. No. M1727
Apitolisib (GDC-0980) Structure
Synonym:

RG7422; GNE 390

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 70  USD70 In stock
5mg USD 67  USD67 In stock
10mg USD 100  USD100 In stock
50mg USD 310  USD310 In stock
100mg USD 470  USD470 In stock
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Quality Control & Documentation
Biological Activity

Apitolisib (GDC-0980; GNE 390; RG 7422) is a potent, highly selective, oral, dual inhibitor of class I PI3K and mTOR. Apitolisib (GDC-0980) demonstrates broad preclinical activity in breast, ovarian, lung, and prostate cancer models. Apitolisib (GDC-0980) can potently inhibit for isoforms of p110 including p110-alpha, p110-beta, p110-gamma and p110-delta. The IC50 value for inhibition of  p110-alpha, p110-beta, p110-gamma and p110-delta by GDC-0980 is 5 nM,27 nM,7 nM and 14 nM. Besides the inhibition of Phosphoinositide 3-kinase, GDC-0980 also show strong inhibition to mTOR, which is a downstream target of akt but not only in PI3K signaling pathway. The Ki value for mTOR is 17 nM.

Customer Product Validations & Biological Datas
Source Biochem Biophys Res Commun (2014). Figure 3. GDC-0980
Method Western blotting
Cell Lines PANC-1 cells and Capan-1 cells
Concentrations 1 μM
Incubation Time 24 h
Results Western blotting results in Fig. 1B showed clearly that GDC-0980 (1 μM) dramatically inhibited phosphorylation of AKT (Ser-473 and Thr-308) and S6K1 (Thr-389) in both PANC-1 cells and Capan-1 cells.
Protocol (for reference only)
Cell Experiment
Cell lines NSCLS cell lines, colon cancer cell lines and etc.
Preparation method Cell viability assays Three hundred and eighty-four–well plates were seeded with 2,000 cells/well in a volume of 54 μL per well followed by incubation at 37°C under 5% CO2 overnight (∼16 hours). Compounds were diluted in dimethyl sulfoxide to generate the desired stock concentrations then added in a volume of 6 μL per well. All treatments were tested in quadruplicate. After 4 days incubation, relative numbers of viable cells were estimated using CellTiter-Glo (Promega) and total luminescence was measured on a Wallac Multilabel Reader (PerkinElmer). The concentration of drug resulting in 50% inhibition of cell viability (IC50) or 50% maximal effective concentration (EC50) was determined using Prism software (GraphPad). For cell lines that failed to achieve an IC50 the highest concentration tested (20 μmol/L) is listed.
Concentrations 0~5µM
Incubation time 4 days
Animal Experiment
Animal models MCF7-neo/HER2 tumor-bearing mice
Formulation 0.5% methylcellulose with 0.2% Tween-80
Dosages 7.5 mg/kg
Administration oral gavage
Chemical Information
Molecular Weight 498.6
Formula C23H30N8O3S
CAS Number 1032754-93-0
Solubility (25°C) DMSO 15 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Salphati et al. Drug Metab Dispos. Preclinical Assessment of the Absorption and Disposition of the Phosphatidylinositol 3-Kinase/Mammalian Target of Rapamycin Inhibitor GDC-0980 and Prediction of Its Pharmacokinetics and Efficacy in Human.

[2] Wallin et al. Mol Cancer Ther. GDC-0980 is a novel class I PI3K/mTOR kinase inhibitor with robust activity in cancer models driven by the PI3K pathway.

[3] Sutherlin et al. J Med Chem. Discovery of a potent, selective, and orally available class I phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) kinase inhibitor (GDC-0980) for the treatment of cancer.

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Keywords: Apitolisib (GDC-0980), RG7422; GNE 390 supplier, PI3K, inhibitors, activators


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