[CAS NO. 2070009-55-9] PF-2771
PRODUCTS SPECIFICATIONS [2070009-55-9]
DESCRIPTION [2070009-55-9]
Overview
| MDL | MFCD29472296 |
|---|---|
| Molecular Weight | 554.08 |
| Molecular Formula | C29H36ClN5O4 |
| SMILES | ClC1=CC(C(N[C@@H](CC2=CC=C(C3=CN(C)C(C(C)=O)=N3)C=C2)CNC(CN(C)C)=O)=O)=CC=C1OC(C)C |
Summary
PF-2771 is a potent and selective centromere protein E (CENP-E) inhibitor, inhibiting CENP-E motor activity with an IC 50 of 16.1 nM; PF-2771 is used as an anticancer agent.
IC50 & Target
|
CENP-E 16.1 nM (IC 50 ) |
In Vitro
PF-2771 is a potent and selective CENP-E inhibitor, inhibiting CENP-E motor activity with an IC 50 of 16.1 nM. PF-2771 shows no inhibitory effect on the ATPase activities of highly related kinesins (0% inhibition of Eg5/KSP, chromokinesin, and MCAK at both 1 or 10 μM PF-2771). PF-2771 exhibits inactive activity against 74 protein kinases (all < 23% inhibition with 1 μM PF-2771, < 40% with 10 μM PF-2771). PF-2771 is cytotoxic to the basal-like breast cancer tumor cell survival, with EC 50 s of < 0.1 μM, and with no cytotoxicity on the normal and premalignant cell lines (EC 50 > 5 μM). PF-2771 (100 nM) reusults in a chromosomal congression defect in MDA-MB-468 cells [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
PF-2771 (100 mg/kg, every day i.p.) potently inhibits CENP-E motor function, and causes tumor regression in SCID mice bearing AA1077 mammary tumors [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 32 mg/mL ( 57.75 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.8048 mL | 9.0240 mL | 18.0479 mL |
| 5 mM | 0.3610 mL | 1.8048 mL | 3.6096 mL |
| 10 mM | 0.1805 mL | 0.9024 mL | 1.8048 mL |