Borussertib |CAS:1800070-77-2 Probechem Biochemicals

Chemical Structure : Borussertib

CAS No.: 1800070-77-2

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Borussertib

货号: PC-36126Not For Human Use, Lab Use Only.

Borussertib is a potent, first-in-class, covalent-allosteric AKT inhibitor with IC50 of 0.8 nM and Ki of 2.2 nM for WT Akt.

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5 mg	￥2880	In stock
10 mg	￥4580	In stock
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生物&药学活性

Borussertib is a potent, first-in-class, covalent-allosteric AKT inhibitor with IC50 of 0.8 nM and Ki of 2.2 nM for WT Akt.
Borussertib specifically binds to two non-catalytic cysteines in AKT at 120 positions 296 and 310.
Borussertib exhibits pronounced sensitivity to breast cancer cell line ZR-75-1 with EC50 of 5 nM, 7- to 12-fold higher potency compared to reversible allosteric inhibitor miransertib and MK-2206.
Borussertib demonstrated strong antiproliferative activity in cancer cell lines harboring genetic alterations within the PTEN, PI3K, and RAS signaling pathways.
Borussertib displayed antitumor activity in combination with the MEK inhibitor trametinib in patient-derived xenograft models of mutant KRAS pancreatic and colon cancer.

物理化学性质&存储条件

分子量	596.691
分子式	C36H32N6O3
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	N-(2-oxo-3-(1-(4-(5-oxo-3-phenyl-5,6-dihydro-1,6-naphthyridin-2-yl)benzyl)piperidin-4-yl)-2,3-dihydro-1H-benzo[d]imidazol-5-yl)acrylamide

参考文献

1. Weisner J, et al. Cancer Res. 2019 Mar 11. pii: canres.2861.2018.

Borussertib

生物&药学活性

物理化学性质&存储条件

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Borussertib

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