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GDC0084
Catalog No. T3705Cas No. 1382979-44-3
Alias RG7666, Paxalisib, GDC-0084, GDC 0084
GDC0084 (RG7666) is a PI3K inhibitor with potential antineoplastic activity. GDC0084 (RG7666) specifically inhibits PI3K in the PI3K/AKT kinase (or protein kinase B) signaling pathway, thereby inhibiting the activation of the PI3K signaling pathway. This may result in the inhibition of both cell growth and survival in susceptible tumor cell populations.
GDC0084
Catalog No. T3705Alias RG7666, Paxalisib, GDC-0084, GDC 0084Cas No. 1382979-44-3
GDC0084 (RG7666) is a PI3K inhibitor with potential antineoplastic activity. GDC0084 (RG7666) specifically inhibits PI3K in the PI3K/AKT kinase (or protein kinase B) signaling pathway, thereby inhibiting the activation of the PI3K signaling pathway. This may result in the inhibition of both cell growth and survival in susceptible tumor cell populations.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 2 mg | $36 | In Stock | |
| 5 mg | $56 | In Stock | |
| 10 mg | $89 | In Stock | |
| 25 mg | $178 | In Stock | |
| 50 mg | $297 | In Stock | |
| 100 mg | $562 | In Stock |
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Purity:99.37%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | GDC0084 (RG7666) is a PI3K inhibitor with potential antineoplastic activity. GDC0084 (RG7666) specifically inhibits PI3K in the PI3K/AKT kinase (or protein kinase B) signaling pathway, thereby inhibiting the activation of the PI3K signaling pathway. This may result in the inhibition of both cell growth and survival in susceptible tumor cell populations. |
| Targets&IC50 | PI3Kβ:46 nM(Ki app), PI3Kδ:3 nM(Ki app), mTOR:70 nM(Ki app), PI3Kγ:10 nM(Ki app), PI3Kα:2 nM(Ki app) |
| In vitro | In human microsomal and stem cell cultures, GDC-0084 showed good metabolic stability and inhibited pAKT, a key signal of the PI3K pathway, in normal brain tissues.GDC-0084 inhibited the proliferation of a variety of glioma cells (IC50: 0.3-1.1 μM).The binding rate of GDC-0084 to plasma proteins was low, and the free fraction of GDC-0084 in CD-1 mouse plasma was 29.5±2.0%. was 29.5±2.7% (n=3,5 μM), while the binding rate to brain tissue was higher in CD-1 mice with a free fraction of only 6.7±1% (n=3). |
| In vivo | In human microsomal and stem cell cultures, GDC-0084 showed good metabolic stability and inhibited pAKT, a key signal of the PI3K pathway, in normal brain tissues.GDC-0084 inhibited the proliferation of a variety of glioma cells (IC50: 0.3-1.1 μM).The binding rate of GDC-0084 to plasma proteins was low, and the free fraction of GDC-0084 in CD-1 mouse plasma was 29.5±2.0%. was 29.5±2.7% (n=3,5 μM), while the binding rate to brain tissue was higher in CD-1 mice with a free fraction of only 6.7±1% (n=3). |
| Cell Research | For transport studies, cells are seeded on 24-well Millicell plates 4 days prior to use(polyethylene terephtalate membrane, 1 μm pore size) at a seeding density of 1.3×105 cells/ml). GDC-0084 is tested at 5 μM in the apical-tobasolateral (A-B) and basolateral-to-apical (B-A) directions. The compound is dissolved in transport buffer consisting of Hanks' balanced salt solution with 10 mM HEPES. Lucifer Yellow is used as the paracellular and monolayer integrity marker. GDC-0084 concentrations in the donor and receiving compartments are determined by liquid chromatography-tandem mass spectrometry (LC-MS/MS) analysis. The apparent permeability (Papp), in the apical to A-B and B-A directions, is calculated after 2-hour incubation.(Only for Reference) |
| Alias | RG7666, Paxalisib, GDC-0084, GDC 0084 |
| Molecular Weight | 382.42 |
| Formula | C18H22N8O2 |
| Cas No. | 1382979-44-3 |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
| Solubility Information | H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: < 1 mg/mL (insoluble or slightly soluble) DMSO: 3.82 mg/mL (10 mM), Sonication is recommended.  | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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