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Borussertib 

Cat. No.: HY-122913 Purity: 98.19%
Handling Instructions

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.

For research use only. We do not sell to patients.

Borussertib Chemical Structure

Borussertib Chemical Structure

CAS No. : 1800070-77-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 459 In-stock
Estimated Time of Arrival: December 31
1 mg USD 120 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 550 In-stock
Estimated Time of Arrival: December 31
25 mg USD 990 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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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].

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (41.90 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6759 mL 8.3797 mL 16.7594 mL
5 mM 0.3352 mL 1.6759 mL 3.3519 mL
10 mM 0.1676 mL 0.8380 mL 1.6759 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.49 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.49 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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KeyWords:

Borussertib | Akt | PKB | Protein kinase B | Inhibitor | inhibitor | inhibit

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Product name:
Borussertib
Cat. No.:
HY-122913
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