| Identification | Back Directory | [Name]
CNX-1351 | [CAS]
1276105-89-5 | [Synonyms]
CS-1069
CNX-1351
CNX-1351, >=98%
CNX-1351; CNX 1351; CNX1351
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
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-(4-morpholinyl)thieno[3,2-d]pyrimidin-6-yl]methyl]-1-piperazinyl]-6-methyl-5-heptene-1,4-dione CNX1351 | [Molecular Formula]
C30H35N7O3S | [MDL Number]
MFCD25976872 | [MOL File]
1276105-89-5.mol | [Molecular Weight]
573.71 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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) | [storage]
Store at -20°C | [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 |
|
|