CNX1351PI3Kα inhibitor CAS# 1276105-89-5 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
Cas No. | 1276105-89-5 | SDF | Download SDF |
PubChem ID | 58441401 | Appearance | Powder |
Formula | C30H35N7O3S | M.Wt | 573.71 |
Type of Compound | N/A | Storage | Desiccate at -20°C |
Solubility | DMSO : 33.33 mg/mL (58.10 mM; Need ultrasonic) | ||
Chemical Name | 1-[4-[[2-(1H-indazol-4-yl)-4-morpholin-4-ylthieno[3,2-d]pyrimidin-6-yl]methyl]piperazin-1-yl]-6-methylhept-5-ene-1,4-dione | ||
SMILES | CC(=CC(=O)CCC(=O)N1CCN(CC1)CC2=CC3=C(S2)C(=NC(=N3)C4=C5C=NNC5=CC=C4)N6CCOCC6)C | ||
Standard InChIKey | DLNUPKDFXMWRFP-UHFFFAOYSA-N | ||
Standard InChI | 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) | ||
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. |
Description | CNX-1351 is a potent and isoform-selective targeted covalent PI3Kα inhibitor with IC50 of 6.8 nM.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)[1].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[1]. References: |
CNX1351 Dilution Calculator
CNX1351 Molarity Calculator
1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
1 mM | 1.743 mL | 8.7152 mL | 17.4304 mL | 34.8608 mL | 43.576 mL |
5 mM | 0.3486 mL | 1.743 mL | 3.4861 mL | 6.9722 mL | 8.7152 mL |
10 mM | 0.1743 mL | 0.8715 mL | 1.743 mL | 3.4861 mL | 4.3576 mL |
50 mM | 0.0349 mL | 0.1743 mL | 0.3486 mL | 0.6972 mL | 0.8715 mL |
100 mM | 0.0174 mL | 0.0872 mL | 0.1743 mL | 0.3486 mL | 0.4358 mL |
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. |
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CNX1351 is a potent and selective inhibitor of PI3Kα with IC50 value of 6.8 nM [1] [2].
Phosphoinositide 3-kinases (PI3Ks) are a family of lipid kinases that phosphorylating the 3’-hydroxyl group of phosphatidylinositol-4,5-bisphosphate (PIP2) to produce phosphatidylinositol-3,4,5-trisphosphate (PIP3). PI3Ks plays important roles in cell proliferation, survival, differentiation and metabolism [1] [2].
CNX1351 is a specific and covalent PI3Kα inhibitor. CNX1351 time-dependently and irreversibly inhibited PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ with IC50 values of 6.8, 166.0, 240.3 and 3020.0 nM, respectively. In SKOV3 ovarian cancer cells with a mutation in PIK3CA that resulted in a constitutively activated PI3Kα, CNX1351 inhibited PI3K signaling with EC50 values of 10-100 nM. In MCF-7 breast cancer cells (E545K) and SKOV3 ovarian cancer cells (H1047R) with different PIK3CA activating mutations, CNX1351 inhibited cell growth with GI50 values of 55 and 78 nM, respectively [1].
In nude mice, CNX1351 (100 mg/kg ip) irreversibly bonded to p110α and inhibited P-AktSer473 expression [1].
References:
[1]. Nacht M, Qiao L, Sheets MP, et al. Discovery of a potent and isoform-selective targeted covalent inhibitor of the lipid kinase PI3Kα. J Med Chem, 2013, 56(3): 712-721.
[2]. Jeong Y, Kwon D, Hong S. Selective and potent small-molecule inhibitors of PI3Ks. Future Med Chem, 2014, 6(7): 737-756.
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