CNX1351
中文名称 | CNX1351 |
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中文同义词 | 1-[4-[[2-(1H-吲唑-4-基)-4-(4-吗啉基)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;PI3K ALPHA抑制剂(CNX-1351);化合物CNX1351;1-(4-((2-(1H-吲唑-4-基)-4-吗啉噻吩并[3,2-D]嘧啶-6-基)甲基)哌嗪-1-基)-6-甲基庚-5-烯-1,4-二酮 |
英文名称 | CNX-1351 |
英文同义词 | 1-[4-[[2-(1H-Indazol-4-yl)-4-(4-morpholinyl)thieno[3,2-d]pyrimidin-6-yl]methyl]-1-piperazinyl]-6-methyl-5-heptene-1,4-dione CNX1351;CNX-1351, >=98%;CNX-1351;1-[4-[[2-(1H-Indazol-4-yl)-4-(4-morpholinyl)thieno[3,2-d]pyrimidin-6-yl]methyl]-1-piperazinyl]-6-methyl-5-heptene-1,4-dione;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;CS-1069;CNX-1351; CNX 1351; CNX1351;CNX1351cas |
CAS号 | 1276105-89-5 |
分子式 | C30H35N7O3S |
分子量 | 573.71 |
EINECS号 | |
相关类别 | 小分子抑制剂;小分子抑制剂,天然产物;细胞生物学试剂;Inhibitors |
Mol文件 | 1276105-89-5.mol |
结构式 |
CNX1351 性质
密度 | 1.328±0.06 g/cm3(Predicted) |
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储存条件 | Store at -20°C |
溶解度 | DMSO:33.33 mg/mL(58.10 mM;需要超声波) |
形态 | 粉末 |
酸度系数(pKa) | 12.22±0.40(Predicted) |
颜色 | 白色至黄色 |
PI3Kα 6.8 nM (IC 50 ) |
PI3Kβ 166 nM (IC 50 ) |
PI3Kδ 240.3 nM (IC 50 ) |
PI3Kγ 3020 nM (IC 50 ) |
CNX-1351 is able to potently (EC 50 <100 nM) and specifically inhibit signaling in PI3Kα-dependent cancer cell lines, and this leads to a potent antiproliferative effect (GI 50 <100 nM). CNX-1351 inhibits PI3K signaling in SKOV3 cells, with potency (EC 50 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 (GI 50 of 78 and 55 nM, respectively).
CNX-1351 inhibits p-Akt Ser473 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-Akt Ser473 or for PI3Kα occupancy. Inhibition of PI3K signaling is detected as a decrease in P-Akt Ser473 at 1 and 4 h after last dose.
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/08/19 | HY-16596 | CNX-1351 | 1 mg | 545元 | |
2024/08/19 | HY-16596 | CNX1351 CNX-1351 | 1276105-89-5 | 5mg | 1183元 |