WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406246
Description: CNX-1351 is a selective covalent Inhibitor of PI3Kα. In an end point assay, CNX-1351 potently inhibited PI3Kα and was 20−400 times less potent against β, γ, and δ. CNX-1351 inhibit PI3Kα signaling in cells and shows prolonged inhibition consistent with a covalent mechanism of Action. CNX-1351 inhibits growth of cells dependent on PI3Kα. CNX-1351 also inhibits PI3Kα signaling in vivo and bonds to p110α.
MedKoo Cat#: 406246
Chemical Formula: C30H35N7O3S
Exact Mass: 573.25221
Molecular Weight: 573.71
Elemental Analysis: C, 62.81; H, 6.15; N, 17.09; O, 8.37; S, 5.59
CNX-1351, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.
Synonym: CNX1351; CNX 1351; CNX-1351.
IUPAC/Chemical Name: 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
InChi Key: DLNUPKDFXMWRFP-UHFFFAOYSA-N
InChi Code: InChI=1S/C30H35N7O3S/c1-20(2)16-21(38)6-7-27(39)36-10-8-35(9-11-36)19-22-17-26-28(41-22)30(37-12-14-40-15-13-37)33-29(32-26)23-4-3-5-25-24(23)18-31-34-25/h3-5,16-18H,6-15,19H2,1-2H3,(H,31,34)
SMILES Code: C/C(C)=C/C(CCC(N1CCN(CC2=CC3=NC(C4=CC=CC5=C4C=NN5)=NC(N6CCOCC6)=C3S2)CC1)=O)=O
The following data is based on the product molecular weight 573.71 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
1. Nacht, M., Qiao, L., Sheets, M.P., et al. Discovery of a potent and isoform-selective targeted covalent inhibitor of the lipid kinase PI3Kα. J. Med. Chem. 56(3), 712-721 (2013).
CNX-1351 is a powerful tool compound that will allow several important questions about PI3K biology to be addressed. The selectivity for PI3Kα and the prolonged duration of inhibition will allow the investigation of the role of PI3Kα in different tumor models with different genetic contexts. CNX-1351 is also an Me-Too drug of GDC-0941.