WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406246
CAS#: 1276105-89-5
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
Name: CNX-1351
CAS#: 1276105-89-5
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
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
Appearance: solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
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.
