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1276105-89-5

中文名稱 CNX1351
英文名稱 CNX-1351
CAS 1276105-89-5
分子式 C30H35N7O3S
分子量 573.71
MOL 文件 1276105-89-5.mol
更新日期 2024/06/12 17:31:27
1276105-89-5 結(jié)構(gòu)式 1276105-89-5 結(jié)構(gòu)式

基本信息

中文別名
PI3K ALPHA抑制劑(CNX-1351)
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
英文別名
CS-1069
CNX-1351
CNX-1351, >=98%
CNX-1351
CNX 1351
CNX1351
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
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
所屬類別
生物化工:激動劑抑制劑

物理化學(xué)性質(zhì)

密度1.328±0.06 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度DMSO : 33.33 mg/mL (58.10 mM; Need ultrasonic)
酸度系數(shù)(pKa)12.22±0.40(Predicted)
形態(tài)粉末
顏色White to yellow

安全數(shù)據(jù)

危險(xiǎn)性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險(xiǎn)性描述H315-H319

常見問題列表

生物活性
CNX-1351 是一種有效的選擇性 PI3Kα 抑制劑,IC50 為 6.8 nM。
靶點(diǎn)

PI3Kα

6.8 nM (IC 50 )

PI3Kβ

166 nM (IC 50 )

PI3Kδ

240.3 nM (IC 50 )

PI3Kγ

3020 nM (IC 50 )

體外研究

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).

體內(nèi)研究

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.

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