PF-2771
Based on 1 Customer Validation
PF-2771 is a potent and selective centromere protein E (CENP-E) inhibitor, inhibiting CENP-E motor activity with an IC50 of 16.1 nM; PF-2771 is used as an anticancer agent.
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- Pureza: 99.66%
- No. CAS: 2070009-55-9
- Fòrmula: C29H36ClN5O4
- Peso molecular:554.08
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Ver todos los productos específicos de isoformas Kinesin
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Actividad biológica
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CENP-E 16.1 nM (IC50) |
PF-2771 is a potent and selective CENP-E inhibitor, inhibiting CENP-E motor activity with an IC50 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 EC50s of < 0.1 μM, and with no cytotoxicity on the normal and premalignant cell lines (EC50 > 5 μM). PF-2771 (100 nM) reusults in a chromosomal congression defect in MDA-MB-468 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 2070009-55-9
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Appearance Solid
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Peso molecular 554.08
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Fòrmula C29H36ClN5O4
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Color White to off-white
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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
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvente y solubilidad
DMSO : ≥ 32 mg/mL (57.75 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.51 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.51 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
Microtubule-activated CENP-E kinesin ATPase activity is measured spectrophotometrically by coupling the hydrolysis of ATP to ADP to NADH oxidation (decrease in 340 nm absorbance) through the activities of pyruvate kinase (PK) and lactate dehydrogenase (LDH). Reactions contained 2 mM phosphoenolpyruvate, 0.28 mM NADH, 5 mM MgCl2, 1 mM DTT, 15 μM taxol, 0.7 μM MT (preformed porcine microtubules), 50 μM ATP, 10 U/mL PK, and 10 U/mL LDH in 15 mM PIPES buffer (pH 7.0). Reactions are initiated with a 20 nM CENP-E addition (Human: 1-342; WT) at 30°C. The IC50 values are determined by a nonlinear, least squares fit of the data to the four-parameter dose-response curve equation. PF-2771 kinesin biochemical selectivity toward other kinesins is tested in triplicate at both 1 and 10 μM PF-2771 in a variant of the CENP-E enzymatic assays that have the following enzyme concentrations: 200 nM chromokinesin motor domain, 200 nM Eg5 motor domain, 226 nM MCAK motor domain. PF-2771 biochemical mechanism is determined by measuring CENP-E enzymatic activity as a function of ATP and PF-2771 concentrations (0, 2.5, 5, 10, 20, 30, 45 nM PF-2771; 1,000, 500, 250, 125, 62.5, 31.2, 15.6, 7.81, 3.90, 1.95, 0.977 μM ATP)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
PF-2771 is added to cells seeded in 96-well plates. The number of cells seeded (1,000-3,000) depended on growth characteristics of each cell type and normalized proliferation rates. Ten different concentrations of compound (PF-2771) used are based on a half-log increment between 1 nM and either 1 or 25 μM. Cells are incubated at 37°C for 7 days before assessing viability with the CellTiter-Glo reagent. Untreated control cells are 80% to 90% confluent after 7 days of culture. Data are fitted into a sigmoidal curve-fitting program to calculate IC50 values[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
HCC1806 tumor cells (3 × 106) are implanted in the mammary fat pad of CB17/lcr.Cg-PrkdcscidLystbg female mice. PF-2771 is administered intraperitoneally (i.p.) to groups of 12 mice at 3, 10, and 30 mg/kg every day for 14 days and at 100 mg/kg every day for 4 days followed by 3 days off and then another 4-day cycle. Tumor volumes are recorded twice weekly by calipers with the final measurement taken 3 days after the last dose. Tumor growth inhibition (TGI) is calculated using the formula 100 × (1 − ΔT/ΔC), where ΔT (treated) and ΔC (control) are the mean tumor volume changes between 1 day after the last dose and the first-day treatment. Time-to-progression endpoint and associated tumor growth delay determinations are calculated using median days to reach to two doublings of initial tumor size. Statistical comparisons are made using one-way ANOVA with Dunnett posttests. Other tumor models had similar methodology except where noted. PDX-AA1077 is a patient-derived xenograft model developed from tumor tissue from a triple-negative patient engrafted to the mammary glands of NSG female mice to create passage 1 tumor-bearing mice. Surgically resected tumor tissue is cut into 2- to 4-mm3 fragments and subcutaneously implanted into the flank of SCID-bg mice. Mice with palpable tumors are randomized before dosing. An HCC1599 tumor cell line xenograft model is established from tumor fragments of established tumors and reimplanted into flank of female SCID mice. When average tumor size reached 250 mm3, animals are randomized into five groups of 10 mice. Animals are treated with vehicle (daily dosing), 10 mg/kg docetaxel (once per week dosing), 25 mg/kg docetaxel (once per week dosing), 20 mg/kg paclitaxel (twice per week dosing), or 100 mg/kg of PF-2771 (every day, i.p.)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (279 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8048 mL | 9.0240 mL | 18.0479 mL | 45.1198 mL |
| 5 mM | 0.3610 mL | 1.8048 mL | 3.6096 mL | 9.0240 mL | |
| 10 mM | 0.1805 mL | 0.9024 mL | 1.8048 mL | 4.5120 mL | |
| 15 mM | 0.1203 mL | 0.6016 mL | 1.2032 mL | 3.0080 mL | |
| 20 mM | 0.0902 mL | 0.4512 mL | 0.9024 mL | 2.2560 mL | |
| 25 mM | 0.0722 mL | 0.3610 mL | 0.7219 mL | 1.8048 mL | |
| 30 mM | 0.0602 mL | 0.3008 mL | 0.6016 mL | 1.5040 mL | |
| 40 mM | 0.0451 mL | 0.2256 mL | 0.4512 mL | 1.1280 mL | |
| 50 mM | 0.0361 mL | 0.1805 mL | 0.3610 mL | 0.9024 mL |
PF-2771 Related Classifications
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