CNX-1351
CNX-1351 Basic information
- Product Name:
- CNX-1351
- Synonyms:
-
- 1-[4-[[2-(1H-Indazol-4-yl)-4-(4-morpholinyl)thieno[3,2-d]pyrimidin-6-yl]methyl]-1-piperazinyl]-6-methyl-5-heptene-1,4-dione CNX1351
- CNX-1351, >=98%
- CNX-1351
- 1-[4-[[2-(1H-Indazol-4-yl)-4-(4-morpholinyl)thieno[3,2-d]pyrimidin-6-yl]methyl]-1-piperazinyl]-6-methyl-5-heptene-1,4-dione
- 1-(4-((2-(1H-indazol-4-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)methyl)piperazin-1-yl)-6-methylhept-5-ene-1,4-dione
- CS-1069
- CNX-1351; CNX 1351; CNX1351
- CNX1351cas
- CAS:
- 1276105-89-5
- MF:
- C30H35N7O3S
- MW:
- 573.71
- Product Categories:
-
- Inhibitors
- Mol File:
- 1276105-89-5.mol
CNX-1351 Chemical Properties
- Density
- 1.328±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO : 33.33 mg/mL (58.10 mM; Need ultrasonic)
- form
- Powder
- pka
- 12.22±0.40(Predicted)
- color
- White to yellow
CNX-1351 Usage And Synthesis
Uses
CNX-1351 is a potent and isoform-selective targeted covalent PI3Kα inhibitor with IC50 of 6.8 nM.
Biological Activity
CNX-1351 is a potent and selective PI3Kα inhibitor with IC50 of 6.8 nM.
in vivo
CNX-1351 inhibits p-Akt Ser473 in mouse spleens and bonds to PI3Kα in vivo. It is delivered into the intraperitoneal cavity of nude mice at 100 mg/kg once a day for 5 consecutive days (n=3 mice per group).
target
| PI3Kα 6.8 nM (IC 50 ) | PI3Kβ 166 nM (IC 50 ) | PI3Kδ 240.3 nM (IC 50 ) | PI3Kγ 3020 nM ( IC 50 ) |
IC 50
PI3Kα: 6.8 nM (IC50); PI3Kβ: 166 nM (IC50); PI3Kδ: 240.3 nM (IC50); PI3Kγ: 3020 nM (IC50)
References
[1] Nacht M, et al. Discovery of a potent and isoform-selective targeted covalent inhibitor of the lipid kinase PI3Kα. J Med Chem. 2013 Feb 14;56(3):712-21. DOI:10.1021/jm3008745
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