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簡(jiǎn)要描述：CNX-1351 1276105-89-5CNX-1351 is a potent and isoform-selective targeted covalent inhibitor of the lipid kinase PI3Kα with IC50 of 6.8 nM; 20-400 times less potent against β, γ, and δ.
產(chǎn)品型號(hào)：abs47027965廠商性質(zhì)：生產(chǎn)廠家更新時(shí)間：2026-01-09訪 問(wèn) 量：687產(chǎn)品分類
Product Category詳細(xì)介紹
| 品牌 | absin | CAS | 1276105-89-5 |
|---|---|---|---|
| 分子式 | C30H35N7O3S | 純度 | 98% |
| 分子量 | 573.709 | 貨號(hào) | abs47027965 |
| 規(guī)格 | 10mg | 供貨周期 | 現(xiàn)貨 |
| 主要用途 | is a potent and isoform-selective | 應(yīng)用領(lǐng)域 | 化工,生物產(chǎn)業(yè),農(nóng)林牧漁,制藥/生物制藥,綜合 |
CNX-1351 1276105-89-5
| 產(chǎn)品描述 | |
| 描述 | CNX-1351 is a potent and isoform-selective targeted covalent inhibitor of the lipid kinase PI3Kα with IC50 of 6.8 nM; 20-400 times less potent against β, γ, and δ. |
| 純度 | 98% |
| 儲(chǔ)存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 別名 | CNX1351 |
| 可溶性/溶解性 | DMSO : 100 mg/mL (174.30 mM; Need ultrasonic) |
| 生物活性 | |
| 靶點(diǎn) | PI3Kα ；PI3Kβ； PI3Kδ； PI3Kγ |
| In vitro(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). |
| In vivo(體內(nèi)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. |
| 研究領(lǐng)域 | |
| 研究領(lǐng)域 | CancerTumor biomarkers Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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