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CNX-1351

    
99.9%

CNX-1351

源葉(MedMol)
S82693 一鍵復制產品信息
1276105-89-5
C30H35N7O3S
573.709
1-[4-[[2-(1H-吲唑-4-基)-4-(4-嗎啉基)噻吩并[3,2-D]嘧啶-6-基]甲基]-1-哌嗪基]-6-甲基-5-庚烯-1,4-二酮; CNX-1351, CAS#1276105-89-5, PI3K抑制劑;;CNX1351; 1-(4-((2-(1H-indazol-4-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)methyl)pipe
貨號 規格 價格 上海 北京 武漢 南京 購買數量
S82693-1mg
99.9% ¥425.00 5 - - -
S82693-5mg
99.9% ¥765.00 7 - - -
S82693-10mg
99.9% ¥1445.00 5 - - -
S82693-25mg
≥99% ¥2465.00 貨期:2-3天 - - -
S82693-50mg
≥99% ¥4335.00 貨期:2-3天 - - -
產品介紹 參考文獻 質檢證書(COA) 摩爾濃度計算器 相關產品

產品介紹

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

產品描述: CNX-1351 is a potent and isoform-selective targeted covalent PI3Kα inhibitor with IC50 of 6.8 nM.
靶點: PI3Kα:6.8 nM (IC50);PI3Kβ:166 nM (IC50);PI3Kδ:240.3 nM (IC50);PI3Kγ:3020 nM (IC50);PI3K
體外研究: 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)
體內研究: 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
參考文獻: 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
保存條件: -20℃
配置溶液濃度參考:
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: 部分產品我司僅能提供部分信息,我司不保證所提供信息的權威性,僅供客戶參考交流研究之用。

參考文獻

質檢證書(COA)

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批號:JS298415 貨號:S20001-25g
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摩爾濃度計算器

質量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)

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