CNX1351
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- CAS号:
- 1276105-89-5
- 英文名:
- CNX-1351
- 英文别名:
- CS-1069;CNX-1351;CNX1351cas;CNX-1351, >=98%;CNX-1351; CNX 1351; CNX1351;CNX1351,inhibit,PI3K,Phosphoinositide 3-kinase,Inhibitor,CNX 1351,CNX-1351;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;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;5-Heptene-1,4-dione, 1-[4-[[2-(1H-indazol-4-yl)-4-(4-morpholinyl)thieno[3,2-d]pyrimidin-6-yl]methyl]-1-piperazinyl]-6-methyl-;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
- 中文名:
- CNX1351
- 中文别名:
- 化合物CNX1351;PI3K ALPHA抑制剂(CNX-1351);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
- CBNumber:
- CB12668207
- 分子式:
- C30H35N7O3S
- 分子量:
- 573.71
- MOL File:
- 1276105-89-5.mol
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CNX1351化学性质
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密度:
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1.328±0.06 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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DMSO : 33.33 mg/mL (58.10 mM; Need ultrasonic)
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形态:
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Powder
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酸度系数(pKa):
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12.22±0.40(Predicted)
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CNX1351性质、用途与生产工艺
CNX-1351 是一种有效的选择性 PI3Kα 抑制剂，IC50 为 6.8 nM。
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PI3Kα
6.8 nM (IC
50
)
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PI3Kβ
166 nM (IC
50
)
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PI3Kδ
240.3 nM (IC
50
)
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PI3Kγ
3020 nM (IC
50
)
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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.
CNX1351
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/01/25 | HY-16596 | CNX-1351 | | 1 mg | 545元 |
| 2024/01/25 | HY-16596 | CNX1351
CNX-1351 | 1276105-89-5 | 5mg | 1200元 |
1276105-89-5, CNX1351 相关搜索:
- Inhibitors
- 原料药
- 细胞生物学试剂
- 小分子抑制剂，天然产物
- 小分子抑制剂
- C30H35N7O3S
- 化合物CNX1351
- PI3K ALPHA抑制剂(CNX-1351)
- 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
- 1276105-89-5
- 5-Heptene-1,4-dione, 1-[4-[[2-(1H-indazol-4-yl)-4-(4-morpholinyl)thieno[3,2-d]pyrimidin-6-yl]methyl]-1-piperazinyl]-6-methyl-
- CNX1351,inhibit,PI3K,Phosphoinositide 3-kinase,Inhibitor,CNX 1351,CNX-1351
- CNX1351cas
- CNX-1351; CNX 1351; CNX1351
- CS-1069
- 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
- 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
- CNX-1351
- CNX-1351, >=98%
- 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