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PF-2771

Catalog No. T12434   CAS 2070009-55-9

PF-2771 is a potent and selective centromere protein E (CENP-E) inhibitor. PF-2771 inhibits CENP-E motor activity with an IC 50 of 16.1 nM. PF-2771 is used as an anticancer agent.

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PF-2771 Chemical Structure
PF-2771, CAS 2070009-55-9
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100 mg 6-8 weeks $ 1,490.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description PF-2771 is a potent and selective centromere protein E (CENP-E) inhibitor. PF-2771 inhibits CENP-E motor activity with an IC 50 of 16.1 nM. PF-2771 is 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 and results in tumor regression in SCID mice with AA1077 mammary tumors [1].
Molecular Weight 554.08
Formula C29H36ClN5O4
CAS No. 2070009-55-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 32 mg/mL (57.75 mM)

TargetMolReferences and Literature

1. Kung PP, et al. Chemogenetic evaluation of the mitotic kinesin CENP-E reveals a critical role in triple-negative breast cancer. Mol Cancer Ther. 2014 Aug;13(8):2104-15.

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Keywords

PF-2771 2070009-55-9 Cytoskeletal Signaling Kinesin PF 2771 PF2771 inhibitor inhibit

 

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