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1800070-77-2

1800070-77-2 structure
1800070-77-2 structure
  • Name: Borussertib
  • Chemical Name: Borussertib
  • CAS Number: 1800070-77-2
  • Molecular Formula: C36H32N6O3
  • Molecular Weight: 596.68
  • Catalog: Signaling Pathways PI3K/Akt/mTOR Akt
  • Create Date: 2019-06-01 15:36:56
  • Modify Date: 2024-01-03 17:40:13
  • 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].

Name Borussertib
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].
Related Catalog
Target

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

[1]. Niklas Uhlenbrock, et al. Structural and chemical insights into the covalentallosteric inhibition of the protein kinase Akt. Chem Sci., 2019, 10, 3573.

Molecular Formula C36H32N6O3
Molecular Weight 596.68
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