CAY10749 |
| Katalog-Nr.GC47055 |
Cay10749 (Verbindung 15) ist ein potenter PARP/PI3K-Inhibitor mit PIC50-Werten von 8,22, 8,44, 8,25, 6,54, 8,13, 6,08 fÜr PARP-1, PARP-2, PI3K&7777#945; offlineefficient_models_2022q2.md.en_de_2022q1.mdCAY10749 is a highly effective anticancer compound targeted against a wide range of oncologic diseases.en_de_2022q1.md
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2337386-47-5
Sample solution is provided at 25 µL, 10mM.
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CAY10749 is a dual inhibitor of poly(ADP-ribose) polymerase (PARP) and PI3K (IC50s = 6.03, 3.63, 5.62, and 7.41 nM for PARP1, PARP2, PI3Kα, and PI3Kδ, respectively).1 It is selective for these enzymes over PI3Kβ and PI3Kγ (IC50s = 288.4 and 831.76 nM, respectively), as well as a panel of 374 additional kinases at 1 µM. CAY10749 (1 µM) induces dsDNA break formation in a neutral comet assay and apoptosis in MDA-MB-468 breast cancer cells. It inhibits proliferation of eight cancer cell lines, including pancreatic, ovarian, lymphoma, leukemia, and lung cancer cells, with IC50 values ranging from 398.11 to 2,818.38 nM. CAY10749 (50 mg/kg twice per day) reduces tumor growth by 73.4% in an MDA-MB-468 mouse xenograft model.
1.Wang, J., Li, H., He, G., et al.Discovery of novel dual poly(ADP-ribose)polymerase (PARP) and phosphoinositide 3-kinase (PI3K) inhibitors as a promising strategy for cancer therapyJ. Med. Chem.63(1)122-139(2019)
| Cas No. | 2337386-47-5 | SDF | |
| Canonical SMILES | O=C1C2=CC=CC=C2C(CC3=CC(C(N4CC5=NC(C6=CN=C(N)C=C6C(F)(F)F)=NC(N7CCOCC7)=C5CC4)=O)=C(F)C=C3)=NN1 | ||
| Formula | C33H28F4N8O3 | M.Wt | 660.6 |
| Löslichkeit | DMF: 11mg/mL,DMF:PBS (pH 7.2) (1:2): 0.3mg/mL,DMSO: 10mg/mL | 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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.5138 mL | 7.5689 mL | 15.1378 mL |
| 5 mM | 0.3028 mL | 1.5138 mL | 3.0276 mL |
| 10 mM | 0.1514 mL | 0.7569 mL | 1.5138 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
Average Rating: 5 (Based on Reviews and 7 reference(s) in Google Scholar.)
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