CAY10749
- Product Name
- CAY10749
- CAS No.
- 2337386-47-5
- Chemical Name
- CAY10749
- Synonyms
- CAY10749;PARP/PI3K-IN-1;PARP/PI3K IN 1,PARP/PI-3K-IN-1,PARP/PI3KIN1;4-(3-(2-(6-Amino-4-(trifluoromethyl)pyridin-3-yl)-4-morpholino-5678-tetrahydropyrido-[34-d]pyrimidine-7-carbonyl)-4-fluorobenzyl)phthalazin-1(2H)-one;4-[[3-[[2-[6-amino-4-(trifluoromethyl)-3-pyridinyl]-5,8-dihydro-4-(4-morpholinyl)pyrido[3,4-d]pyrimidin-7(6H)-yl]carbonyl]-4-fluorophenyl]methyl]-1(2H)-phthalazinone
- CBNumber
- CB86197920
- Formula Weight
- 0
- MOL File
- Mol file
CAY10749 Property
- storage temp.
- Store at -20°C
- solubility
- DMF: 11mg/mL,DMF:PBS (pH 7.2) (1:2): 0.3mg/mL,DMSO: 10mg/mL
- form
- A crystalline solid
- color
- White to off-white
N-Bromosuccinimide Price
- Product number
- HCH0116614
- Product name
- 2-(3-(1-BENZOYLAMINO-2,2,2-TRICHLORO-ETHYL)-THIOUREIDO)-BENZOIC ACID METHYL ESTER
- Purity
- 95.00%
- Packaging
- 5MG
- Price
- $499.95
- Updated
- 2021/12/16
CAY10749 Chemical Properties,Usage,Production
Biological Activity
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.
References
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)
CAY10749 Preparation Products And Raw materials
Raw materials
Preparation Products
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