PF-07104091 hydrate |
Catalog No.GC62661
One-Click Copy Product Info
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PF-07104091 hydrate es un inhibidor potente y selectivo de CDK2/E1 y GSK3β, con Kis de 1.16 y 537.81 nM, respectivamente. PF-07104091 hidratado tiene actividad antitumoral contra los cánceres con amplificación de ciclina E1 y se utiliza comúnmente para tratar el cáncer de mama HR+/HER2- y el cáncer de ovario.
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
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PF-07104091 hydrate es un inhibidor potente y selectivo de CDK2/E1 y GSK3β, con Kis de 1.16 y 537.81 nM, respectivamente[1]. PF-07104091 hidratado tiene actividad antitumoral contra los cánceres con amplificación de ciclina E1 y se utiliza comúnmente para tratar el cáncer de mama HR+/HER2- y el cáncer de ovario[2].
PF-07104091 (37-3000 nM, 24 h) inhibe la expresión de los biomarcadores t-Rb, t-NCL, pRB S8078/811 y p-NCL T84 en células OVCAR3[1]. PF-07104091 (0.01-10 mM, 3 días) inhibe la proliferación de células tumorales (TOV-21G, HCT116)[3].
PF-07104091 (25, 75, 175 mpk, 25 días; dos veces al día; PO) inhibe el crecimiento tumoral (TGI) en tumores de OVCAR3 en ratones[1]. En un modelo de ratón desnudo con tumor trasplantado HCT116, PF-07104091 (50 mg/kg, 14 días) redujo el volumen tumoral en casi un 69.81% y el peso tumoral en casi un 60.16%[3].
References:
[1].Shen C, Zhang Q, Almaden J, et al. PF-07104091, a first-in-class CDK2-selective inhibitor for the treatment of HR+/HER2-breast cancer and CCNE1 high ovarian cancer[J]. Cancer Research, 2024, 84(6_Supplement): 5709-5709.
[2]. Douglas Carl BEHENNA, et al. Cdk2 inhibitors. WO2020157652A2.
[3]. Liu, Z.; Yang, Y.; Sun, X.; Ma, R.; Zhang, W.; Wang, W.; Yang, G.; Wang, H.; Zhang, J.; Wang, Y.; et al. Discovery of Novel Antitumor Small-Molecule Agent with Dual Action of CDK2/p-RB and MDM2/p53. Molecules 2024, 29, 725.
| Experimentos celulares [1]: | |
Líneas celulares | OVCAR3 |
Método de preparación | Las células OVCAR3 fueron tratadas con PF-07104091 a concentraciones de (37-3000) nM durante 24 horas. |
Condiciones de reacción | PF-07104091 (37, 111, 333, 1000, 3000 nM); 24 h. |
Áreas de aplicación | PF-07104091 inhibe la expresión de los biomarcadores t-Rb, t-NCL, pRB S8078/811 y p-NCL T84 en células OVCAR3. |
| Experimentos con animales [1]: | |
Modelos animales | Modelo de cáncer de ovario. |
Método de preparación | Los tumores OVCAR3 en ratones fueron tratados con PF-07104091 administrado por vía oral (PO) dos veces al día (BID) durante 25 días. |
Forma de dosificación | PF-07104091 (25, 75, 175 mpk); 25 días; dos veces al día; PO. |
Áreas de aplicación | Perfil de inhibición del crecimiento tumoral (TGI) en tumores OVCAR3 en ratones tratados con PF-07104091 administrado por vía oral (PO) dos veces al día (BID). |
Referencias: [1]. Shen C, Zhang Q, Almaden J, et al. PF-07104091, un inhibidor selectivo de CDK2 de primera clase para el tratamiento del cáncer de mama HR+/HER2- y cáncer de ovario con alta expresión de CCNE1 [J]. Cancer Research, 2024, 84(6_Supplement): 5709-5709. | |
| Cas No. | SDF | ||
| Formula | C19H30N6O5 | M.Wt | 422.48 |
| Solubility | Storage | 4°C, away from moisture and light | |
| 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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.367 mL | 11.8349 mL | 23.6698 mL |
| 5 mM | 473.4 μL | 2.367 mL | 4.734 mL |
| 10 mM | 236.7 μL | 1.1835 mL | 2.367 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 saline, 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: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 33 reference(s) in Google Scholar.)