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PF-2771 is a potent and selective centromere protein E (CENP-E) inhibitor with an IC50 of 16.1 nM, used as an anticancer agent.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 100 mg | $1,490 | 6-8 weeks | 6-8 weeks |
| Description | PF-2771 is a potent and selective centromere protein E (CENP-E) inhibitor with an IC50 of 16.1 nM, used as an anticancer agent. |
| Targets&IC50 | CENP-E:16.1 nM |
| In vitro | PF-2771 is a powerful and selective inhibitor of CENP-E, demonstrating significant inhibition of CENP-E motor activity at an IC50 of 16.1 nM, without affecting ATPase activities of similar kinesins (showing 0% inhibition of Eg5/KSP, chromokinesin, and MCAK at both 1 or 10 μM concentrations). It also displays negligible inhibitory effects on 74 protein kinases (less than 23% inhibition at 1 μM and less than 40% at 10 μM). Notably, PF-2771 is cytotoxic exclusively to basal-like breast cancer cells, with EC50 values below 0.1 μM, while it has no cytotoxic effects on normal and premalignant cell lines (EC50 > 5 μM). Furthermore, at 100 nM, PF-2771 induces a chromosomal congression defect in MDA-MB-468 cells. |
| In vivo | PF-2771 (100 mg/kg, daily i.p.) effectively inhibits CENP-E motor function, resulting in tumor regression in SCID mice with AA1077 mammary tumors [1]. |
| Molecular Weight | 554.08 |
| Formula | C29H36ClN5O4 |
| Cas No. | 2070009-55-9 |
| Relative Density. | 1.22 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 32 mg/mL (57.75 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween-80+45% Saline: 2 mg/mL (3.61 mM), Sonication is recommeded. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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