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PF-4989216
🥰Excellent
Catalog No. T6938Cas No. 1276553-09-3
Alias PF 4989216
PF-4989216 is a potent and selective PI3K inhibitor with IC50 values of 2 nM (p110α), 142 nM (p110β), 65 nM (p110γ), 1 nM (p110δ), and 110 nM (VPS34).
PF-4989216
🥰Excellent
Purity: 99.53%
Catalog No. T6938Alias PF 4989216Cas No. 1276553-09-3
PF-4989216 is a potent and selective PI3K inhibitor with IC50 values of 2 nM (p110α), 142 nM (p110β), 65 nM (p110γ), 1 nM (p110δ), and 110 nM (VPS34).
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 2 mg | $33 | In Stock | |
| 5 mg | $59 | In Stock | |
| 10 mg | $103 | In Stock | |
| 25 mg | $197 | In Stock | |
| 50 mg | $346 | In Stock | |
| 100 mg | $418 | In Stock | |
| 200 mg | $595 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $62 | In Stock |
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Purity:99.53%
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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 | PF-4989216 is a potent and selective PI3K inhibitor with IC50 values of 2 nM (p110α), 142 nM (p110β), 65 nM (p110γ), 1 nM (p110δ), and 110 nM (VPS34). |
| Targets&IC50 | p110α:2 nM, p110γ:65 nM, p110δ:1 nM, p110β:142 nM, VPS34:110 nM |
| In vitro | PF-4989216 significantly inhibits cell viability in SCLC cells with a PIK3CA mutation, such as NCI-H69, NCI-H1048, and Lu99A cells. PF-4989216, via PI3K signaling inhibition, blocks cell-cycle progression and reduces cell transformation in SCLCs. In SCLCs with PIK3CA mutation, PF-4989216 induces BIM-mediated apoptosis. [1] |
| In vivo | In SCID mice bearing NCI-H69 or NCI-H1048 xenograft tumors, PF-4989216 (350 mg/kg, p.o.) inhibits PI3K phosphorylation signaling and induces antitumor activity. [1] |
| Cell Research | SCLC cells are cultured (5,000 cells/well) in a 96-well microtiter plate at 37°C in 5% CO2 in supplier-recommended growth media and compounds are added to each well starting at 10 μM with a 3-fold serial dilution. At 72 hours after compound addition, CellTiter-Glo (CTG) Solution is added per the manufacturer's instructions. Luminescence is read on an Envision plate reader. All experiments are run in duplicate and have been repeated at least three times.(Only for Reference) |
| Alias | PF 4989216 |
| Molecular Weight | 380.4 |
| Formula | C18H13FN6OS |
| Cas No. | 1276553-09-3 |
| Smiles | Fc1cc(ccc1-c1c(sc(N2CCOCC2)c1C#N)-c1ncn[nH]1)C#N |
| Relative Density. | no data available |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
| Solubility Information | Ethanol: 7 mg/mL (18.4 mM), Heating is recommended. H2O: < 1 mg/mL (insoluble or slightly soluble) DMSO: 71 mg/mL (186.6 mM) | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
DMSO
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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (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.
(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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