货号	规格	价格	上海	北京	珠海	重庆	武汉
S82693-1mg买3赠1	99.90%	￥400.00 S82693-1mg ￥400.00 现货（买3赠1）	5 5	-	-	-	-
S82693-5mg买3赠1	99.90%	￥765.00 S82693-5mg ￥765.00 现货（买3赠1）	6 6	-	-	-	-
S82693-10mg促销	99.90%	￥1420.00 ￥1130.00 S82693-10mg ￥1130.00 现货	5 5	-	-	-	-
S82693-25mg促销	≥99%	￥2460.00 ￥1960.00 S82693-25mg ￥1960.00 2-3天	0 货期：2-3天	-	-	-	-
S82693-50mg促销	≥99%	￥4330.00 ￥3460.00 S82693-50mg ￥3460.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

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

靶点：

PI3Kα:6.8 nM (IC50);PI3Kβ:166 nM (IC50);PI3Kδ:240.3 nM (IC50);PI3Kγ:3020 nM (IC50);PI3K

体外研究：

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)

体内研究：

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

参考文献：

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.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.743 ml	8.715 ml	17.43 ml
5 mM	0.349 ml	1.743 ml	3.486 ml
10 mM	0.174 ml	0.872 ml	1.743 ml
50 mM	0.035 ml	0.174 ml	0.349 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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