CNX-1351 1276105-89-5

简要描述：CNX-1351 1276105-89-5
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.

产品型号：abs47027965
厂商性质：生产厂家
更新时间：2026-01-09
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详细介绍

品牌	absin	CAS	1276105-89-5
分子式	C30H35N7O3S	纯度	98%
分子量	573.709	货号	abs47027965
规格	10mg	供货周期	现货
主要用途	is a potent and isoform-selective	应用领域	化工,生物产业,农林牧渔,制药/生物制药,综合

CNX-1351 1276105-89-5

产品描述
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.
纯度	98%
储存/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
别名	CNX1351
可溶性/溶解性	DMSO : 100 mg/mL (174.30 mM; Need ultrasonic)
生物活性
靶点	PI3Kα ；PI3Kβ； PI3Kδ； PI3Kγ
In vitro(体外研究)	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(体内研究)	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.

研究领域
研究领域	CancerTumor biomarkers Drug DiscoverySmall Molecule DrugLead Compound Discovery

CNX-1351 1276105-89-5温馨提示：本产品仅作科研实验使用，不支持临床等研究

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