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PF-2771
Catalog No. T12434Cas No. 2070009-55-9
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.
PF-2771
Catalog No. T12434Cas No. 2070009-55-9
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 | Availability | Quantity |
|---|---|---|---|
| 100 mg | $1,490 | 6-8 weeks |
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Product Introduction
Bioactivity
Chemical Properties
| 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 |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 32 mg/mL (57.75 mM) | ||||||||||||||||||||||||||||||
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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