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Borussertib 

目录号: HY-122913
产品使用指南

Borussertib 是蛋白激酶 Akt 的一线共价变构抑制剂,其对 AktwtIC50 值为 0.8 nM,Ki 值为 2.2 nM。

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Borussertib Chemical Structure

Borussertib Chemical Structure

CAS No. : 1800070-77-2

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Description

Borussertib is a covalent-allosteric and first-in-class inhibitor of protein kinase Akt, with an IC50 of 0.8 nM and a Ki of 2.2 nM for Aktwt[1].

IC50 & Target[1]

Aktwt

0.8 nM (IC50)

Aktwt

2.2 nM (Ki)

In Vitro

Borussertib exhibits excellent cellular activity in the nanomolar range with superior profile against clinical candidate Akt inhibitors as well as the cytostatic drug doxorubicin. The EC50 values are 191±90 nM, 48±15 nM, 5±1 nM, 277±90 nM, 373±54 nM, 7770±641 nM in AN3CA (endometrium), T47D (breast), ZR-75-1 (breast), MCF-7 (breast), BT-474 (breast) and KU-19-19 (bladder) cell lines, respectively[1].

References
Molecular Weight

596.68

Formula

C₃₆H₃₂N₆O₃

CAS No.

1800070-77-2

SMILES

C=CC(NC1=CC=C(N2)C(N(C3CCN(CC4=CC=C(C5=NC6=C(C(NC=C6)=O)C=C5C7=CC=CC=C7)C=C4)CC3)C2=O)=C1)=O

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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产品名称:
Borussertib
目录号:
HY-122913
需求量:

Borussertib

Cat. No.: HY-122913