CNX-1351 free base · Synonyms: CNX 1351 · CNX1351

CNX-1351 is a potent and isoform-selective targeted covalent PI3Kα inhibitor.

For research use only. Not for human or veterinary use.

Target PI3K

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

CNX-1351 structure

CAS No.: 1276105-89-5

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
100 mg	USD 580.00	BP-02123-100mg	In stock	Get quote
250 mg	USD 1,050.00	BP-02123-250mg	In stock	Get quote
500 mg	USD 1,560.00	BP-02123-500mg	In stock	Get quote
1 g	USD 2,520.00	BP-02123-1g	In stock	Get quote
2 g	USD 3,800.00	BP-02123-2g	In stock	Get quote

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Description

CNX-1351 is a potent and isoform-selective targeted covalent PI3Kα inhibitor with IC50 of 6.8 nM.

Biological activity

In Vitro CNX-1351 is able to potently (EC50<100 nM) and specifically inhibit signaling in PI3Kα-dependent cancer cell lines, and this leads to a potent antiproliferative effect (GI50<100 nM). CNX-1351 inhibits PI3K signaling in SKOV3 cells, with potency (EC50 of 10-100 nM) similar to that of the pan-PI3K inhibitor. To investigate the functional consequence of inhibiting PI3Kα in cells, two cell lines with different PIK3CA activating mutations, SKOV3 ovarian cancer cells (H1047R) and MCF-7 breast cancer cells (E545K), are treated with CNX-1351 and growth is monitored. Both PIK3CA-driven cell lines are growth inhibited by exposure to CNX-1351 for 96 h (GI50 of 78 and 55 nM, respectively). In Vivo CNX-1351 inhibits p-AktSer473 in mouse spleens and bonds to PI3Kα in vivo. CNX-1351 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). Spleens are harvested from the mice at the indicated times after the last dose (1-24 h) and interrogated by immunoblot for P-AktSer473 or for PI3Kα occupancy. Inhibition of PI3K signaling is detected as a decrease in P-AktSer473 at 1 and 4 h after last dose.

Identifiers

SMILES: C\C(C)=C\C(=O)CCC(=O)N1CCN(CC2=CC3=NC(=NC(N4CCOCC4)=C3S2)C2=CC=CC3=C2C=NN3)CC1
InChIKey: DLNUPKDFXMWRFP-UHFFFAOYSA-N

Specifications

MW (average): 573.7090
Formula: C₃₀H₃₅N₇O₃S
CAS No.: 1276105-89-5
Physical state: Solid
Color: white to yellow
Shipping: 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: Powder -20℃ 3 years; 4℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO, >50mg/mL

Documents

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.

Same target

Search PI3K

Same research area

Search Cancer