PF-07104091 hydrate |
| Catalog No.GC62661 |
PF-07104091 hydrate is a potent and selective inhibitor of CDK2/E1 and GSK3β with Kis of 1.16 and 537.81 nM, respectively. PF-07104091 hydrate has antitumor activity against cyclin E1-amplified cancers and is commonly used to treat HR+/HER2- breast cancer and ovarian cancer
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
PF-07104091 hydrate is a potent and selective inhibitor of CDK2/E1 and GSK3β with Kis of 1.16 and 537.81 nM[1], respectively. PF-07104091 hydrate has antitumor activity against cyclin E1-amplified cancers and is commonly used to treat HR+/HER2- breast cancer and ovarian cancer[2].
PF-07104091 (37-3000nM, 24h) inhibits the expression of biomarkers t-Rb, t-NCL, pRB S8078/811, and p-NCL T84 in OVCAR3 cells[1].PF-07104091(0.01-10mM, 3day) inhibits the proliferation of tumor cells (TOV-21G, HCT116) [3].
PF-07104091 (25、75、175 mpk，25 day; twice per day;PO) inhibits tumor growth (TGI) of OVCAR3 tumors mice[1] .In nude mouse model of HCT116 transplanted tumor, PF-07104091(50 mg/kg, 14 day) reduced tumor volume by nearly 69.81% and tumor weight by nearly 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.
| Cell experiment [1]: | |
Cell lines | OVCAR3 |
Preparation Method | OVCAR3 cells were treated with （37-3000） nM PF-07104091 for 24 hours. |
Reaction Conditions | PF-07104091（37、111、333、1000、3000） nM；24h |
Applications | PF-07104091 inhibits the expression of biomarkers t-Rb, t-NCL, pRB S8078/811, and p-NCL T84 in OVCAR3 cells. |
| Animal experiment [1]: | |
Animal models | ovarian cancer modle |
Preparation Method | OVCAR3 tumors in mice treated with PF-07104091 orally (PO) twice per day (BID) for 25 day. |
Dosage form | PF-07104091 (25、75、175)mpk;25 day; twice per day；PO |
Applications | Tumor growth inhibition (TGI) profile of OVCAR3 tumors in mice treated with PF-07104091 orally (PO) twice per day (BID). |
References: | |
| 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. |
||
| 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 | 0.4734 mL | 2.367 mL | 4.734 mL |
| 10 mM | 0.2367 mL | 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 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: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 33 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *