PF-07104091 |
| رقم الكتالوجGC62660 |
PF-07104091 هو مثبط لـ CDK2 / cyclin E1 ، وهو مثبط انتقائي لموقع ATP يستهدف الحالة المفعلة المرتبطة بسيكلين من الكاينات.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2460249-19-6
Sample solution is provided at 25 µL, 10mM.
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PF-07104091 is a CDK2/cyclin E1 inhibitor, a selective ATP-site inhibitor targeting the cyclin-bound activated state of the kinase [1]. PF-07104091(Example 13) inhibited CDK2/cyclin E1, GSK3β, CDK1/cyclin A2, CDK4/cyclin D1, CDK6/cyclin D3 and CDK9, with Kis of 1.16, 537.81, 110, 238, 465 and 117 nM, respectively. PF-07104091 has anti-tumor activity for cyclin E1-amplified cancers. [1].
PF-07104091 inhibited T47D and KPL1 cells with IC50s of 0.785 and 0.603 µM, respectively [2].
The combination of abemaciclib and PF-07104091decreased T47D and KPL1 cells survival compared to either single agent [2].
References:
[1]. Behenna, D. C.; Freeman-Cook, K. D.; Hoffman, R. L.; Nagata, A.; Ninkovic, S.; Sutton, S. C. Preparation of aminopyrazolylcyclopentyl carbamate derivatives for use as CDK2 inhibitors. WO 2020157652, 2020.
[2]. Gharbi S I, Pelletier L A, Espada A, et al. Crystal structure of active CDK4-cyclin D and mechanistic basis for abemaciclib efficacy[J]. npj Breast Cancer, 2022, 8(1): 126.
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Preparation Method |
1000 cell/well were seeded in 384-well plate in 20 µL of RPMI 1640, or DMEM, respectively in 10% FBS at 37 °C, 5%CO2. Assay-ready plates containing 1:3 serial dilutions of compounds in 100% DMSO were prepared using acoustic dispensing technology (ECHO), final starting concentration was 20 µM. Compound-treated plates were incubated for 4 days (2 doubling times) and cell proliferation estimated using PI staining. |
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Reaction Conditions |
0-20µM for 4 days |
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Applications |
PF-07104091 inhibited T47D and KPL1 cells with IC50s of 0.785 and 0.603 µM, respectively. |
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References: [1]: Gharbi S I, Pelletier L A, Espada A, et al. Crystal structure of active CDK4-cyclin D and mechanistic basis for abemaciclib efficacy[J]. npj Breast Cancer, 2022, 8(1): 126. | |
| Cas No. | 2460249-19-6 | SDF | |
| Formula | C19H28N6O4 | M.Wt | 404.46 |
| الذوبان | Storage | Store at -20°C | |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4724 mL | 12.3622 mL | 24.7243 mL |
| 5 mM | 0.4945 mL | 2.4724 mL | 4.9449 mL |
| 10 mM | 0.2472 mL | 1.2362 mL | 2.4724 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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