Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
100 mg | 6-8 weeks | $ 1,490.00 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 32 mg/mL (57.75 mM)
You can also refer to dose conversion for different animals. More
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PF-2771 2070009-55-9 Cytoskeletal Signaling Kinesin PF 2771 PF2771 inhibitor inhibit