Ebvaciclib
Based on 4 publication(s) in Google Scholar
PF-06873600 is a selective and orally bioavailable inhibitor of cyclin-dependent kinase (CDK), with Ki values of 0.09 nM, 0.13 nM and 0.16 nM for CDK2, CDK4 and CDK6, respectively. PF-06873600 has potential antineoplastic activity.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.91%
- No. CAS: 2185857-97-8
- Fòrmula: C20H27F2N5O4S
- Peso molecular:471.52
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Ebvaciclib
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Customer Validation & Images
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WB
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Cell Proliferation/Viability Assay
Actividad biológica
Descripciòn
IC50 & Target
[1]|
CDK2 0.09 nM (Ki) |
CDK4 0.13 nM (Ki) |
CDK6 0.16 nM (Ki) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
0.22 μM
Compound: Ebvaciclib
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Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation
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[PMID: 37060933] |
| MCF7 | IC50 |
48 nM
Compound: PF-06873600
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Antiproliferative activity against human MCF7 cells
Antiproliferative activity against human MCF7 cells
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[PMID: 31477350] |
| MV4-11 | IC50 |
0.57 μM
Compound: Ebvaciclib
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Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell proliferation
Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell proliferation
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[PMID: 37060933] |
| OVCAR-3 | EC50 |
4 nM
Compound: 22; PF-06873600
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Antitumor activity against human OVCAR-3 cells xenografted in mouse assessed as inhibition of RB1 phosphorylation in tumor cells
Antitumor activity against human OVCAR-3 cells xenografted in mouse assessed as inhibition of RB1 phosphorylation in tumor cells
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[PMID: 34110834] |
| OVCAR-3 | EC50 |
45 nM
Compound: 22; PF-06873600
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Antiproliferative activity against human OVCAR-3 cells assessed as inhibition of cell proliferation incubated for 6 days by CyQuant assay
Antiproliferative activity against human OVCAR-3 cells assessed as inhibition of cell proliferation incubated for 6 days by CyQuant assay
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[PMID: 34110834] |
| OVCAR-3 | IC50 |
48 nM
Compound: PF-06873600
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Antiproliferative activity against human OVCAR3 cells
Antiproliferative activity against human OVCAR3 cells
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[PMID: 31477350] |
In Vitro
PF-06873600 (Example 8) is an orally bioavailable, cyclin-dependent kinase (CDK) inhibitor, with potential antineoplastic activity[1]. PF-06873600 selectively targets, binds to and inhibits the activity of CDKs. Inhibition of these kinases leads to cell cycle arrest, induction of apoptosis and inhibition of tumor cell proliferation. CDKs, ATP-dependent serine/threonine kinases that are important regulators of cell cycle progression and cellular proliferation, are frequently overexpressed in tumor cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 2185857-97-8
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Appearance Solid
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Peso molecular 471.52
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Fòrmula C20H27F2N5O4S
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Color White to light yellow
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SMILES
O=C1N([C@H]2[C@](O)(CCC2)C)C3=NC(NC4CCN(CC4)S(C)(=O)=O)=NC=C3C=C1C(F)F
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Synonyms
PF-06873600
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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 6 months -20°C 1 month
Publications (4)
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Journal Impact Factor
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Most Recent
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Br J Cancer
Concurrent inhibition of CDK2 adds to the anti-tumour activity of CDK4/6 inhibition in GIST. [Abstract]2022 Nov;127(11):2072-2085. PMID: 36175617
Ebvaciclib purchased from MedChemExpress. Usage Cited in: Br J Cancer. 2022 Nov;127(11):2072-2085. [Abstract]
Immunoblotting studies showing effects of treatment (24 h) with the combined CDK2/4/6 inhibitor PF-06873600 (125, 250, 500 nM) on pRB1 Ser 795, pRB1 Ser 807/8011, and cyclin A.
Ebvaciclib purchased from MedChemExpress. Usage Cited in: Br J Cancer. 2022 Nov;127(11):2072-2085. [Abstract]
A significant shift in PF-06873600 proliferation IC50 values in the palbociclib-resistant GIST430/654/RB1- sub-line compared to parental GIST430/654 cells as assessed by BrdU incorporation at 24 h.
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Solvente y solubilidad
In Vitro:
DMSO : 83.33 mg/mL (176.73 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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: ≥ 2.08 mg/mL (4.41 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.41 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
In Vivo Dissolution Calculator
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.
Pureza y Documentación
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Ficha de datos (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. US 2018/0044344 A1.
[2]. NCI Drug Dictionary
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1208 mL | 10.6040 mL | 21.2080 mL | 53.0200 mL |
| 5 mM | 0.4242 mL | 2.1208 mL | 4.2416 mL | 10.6040 mL | |
| 10 mM | 0.2121 mL | 1.0604 mL | 2.1208 mL | 5.3020 mL | |
| 15 mM | 0.1414 mL | 0.7069 mL | 1.4139 mL | 3.5347 mL | |
| 20 mM | 0.1060 mL | 0.5302 mL | 1.0604 mL | 2.6510 mL | |
| 25 mM | 0.0848 mL | 0.4242 mL | 0.8483 mL | 2.1208 mL | |
| 30 mM | 0.0707 mL | 0.3535 mL | 0.7069 mL | 1.7673 mL | |
| 40 mM | 0.0530 mL | 0.2651 mL | 0.5302 mL | 1.3255 mL | |
| 50 mM | 0.0424 mL | 0.2121 mL | 0.4242 mL | 1.0604 mL | |
| 60 mM | 0.0353 mL | 0.1767 mL | 0.3535 mL | 0.8837 mL | |
| 80 mM | 0.0265 mL | 0.1326 mL | 0.2651 mL | 0.6628 mL | |
| 100 mM | 0.0212 mL | 0.1060 mL | 0.2121 mL | 0.5302 mL |
Ebvaciclib Related Classifications
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