CNX-1351 | PI3Kα inhibitor | Probechem Biochemicals

Chemical Structure : CNX-1351

CAS No.: 1276105-89-5

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CNX-1351 (CNX1351)

货号: PC-25282Not For Human Use, Lab Use Only.

CNX-1351 (CNX1351) is a potent, isoform-selective and covalent inhibitor of PI3Kα with IC50 of 6.8 nM, covalently modifies PI3Kα on cysteine 862 (C862).

规格	价格	库存
5 mg	￥880	In stock
10 mg	￥1280	In stock
25 mg	￥2180	In stock
50 mg	￥3580	In stock
100 mg		Get quote

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生物&药学活性

CNX-1351 (CNX1351) is a potent, isoform-selective and covalent inhibitor of PI3Kα with IC50 of 6.8 nM, covalently modifies PI3Kα on cysteine 862 (C862).
CNX-1351 does not covalently modifies PI3Kβ, -γ, and -δ and shows no inhibitory activities.
CNX-1351 inhibits PI3K signaling in SKOV3 cells with EC50 of 10-100 nM in SKOV3 cells, irreversibly inhibits p-AktSer473.
CNX-1351 inhibits cell growth of cance cell with PIK3CA activating mutations, SKOV3 ovarian cancer cells (H1047R) and MCF-7 breast cancer cells (E545K), with IC50 of 77.6 and 54.7 nM respectively.
CNX-1351 (100 mg/kg ip) inhibits p-AktSer473 in mouse spleens and binds to PI3Kα in vivo.

物理化学性质&存储条件

分子量	573.72
分子式	C30H35N7O3S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	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

参考文献

1. Nacht M, et al. J Med Chem. 2013 Feb 14;56(3):712-21.

CNX-1351 (CNX1351)

生物&药学活性

物理化学性质&存储条件

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CNX-1351 (CNX1351)

生物&药学活性

物理化学性质&存储条件

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