Referencia número: HY-122913

Borussertib

1 Cited Publications

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Borussertib, a chemical probe, is a covalent-allosteric and first-in-class inhibitor of protein kinase Akt, with an IC₅₀ of 0.8 nM and a K_i of 2.2 nM for Akt^wt.

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Pureza: 99.18%
No. CAS: 1800070-77-2
Fòrmula: C₃₆H₃₂N₆O₃
Peso molecular:596.68

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Borussertib Chemical Structure

No. CAS: 1800070-77-2

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (1)
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

Borussertib, a chemical probe, is a covalent-allosteric and first-in-class inhibitor of protein kinase Akt, with an IC₅₀ of 0.8 nM and a K_i of 2.2 nM for Akt^wt^[1].

IC₅₀ & Target

IC50: 0.8 nM (Akt^wt)^[1].

Ver todos los productos específicos de isoformas Akt :

Cellular Effect

Cell Line	Type	Value	Description	References
AN3-CA	EC₅₀	191 nM Compound: Borussertib	Antiproliferative activity against human AN3-CA cells assessed as reduction of cell growth measured after 5 days by CellTiter-Glo assay Antiproliferative activity against human AN3-CA cells assessed as reduction of cell growth measured after 5 days by CellTiter-Glo assay	[PMID: 31584233]
AN3-CA	EC₅₀	191 nM Compound: Compound 1	Antiproliferative activity against human AN3-CA cells assessed as reduction in cell viability incubated for 5 days by celltiter-glo assay Antiproliferative activity against human AN3-CA cells assessed as reduction in cell viability incubated for 5 days by celltiter-glo assay	[PMID: 30996949]
BT-474	EC₅₀	373 nM Compound: Compound 1	Antiproliferative activity against human BT-474 cells assessed as reduction in cell viability incubated for 5 days by celltiter-glo assay Antiproliferative activity against human BT-474 cells assessed as reduction in cell viability incubated for 5 days by celltiter-glo assay	[PMID: 30996949]
KU-19-19	EC₅₀	7770 nM Compound: Compound 1	Antiproliferative activity against human KU-19-19 cells assessed as reduction in cell viability incubated for 5 days by celltiter-glo assay Antiproliferative activity against human KU-19-19 cells assessed as reduction in cell viability incubated for 5 days by celltiter-glo assay	[PMID: 30996949]
MCF7	EC₅₀	277 nM Compound: Compound 1	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 5 days by celltiter-glo assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 5 days by celltiter-glo assay	[PMID: 30996949]
T47D	EC₅₀	48 nM Compound: Borussertib	Antiproliferative activity against human T47D cells assessed as reduction of cell growth measured after 5 days by CellTiter-Glo assay Antiproliferative activity against human T47D cells assessed as reduction of cell growth measured after 5 days by CellTiter-Glo assay	[PMID: 31584233]
T47D	EC₅₀	48 nM Compound: Compound 1	Antiproliferative activity against human T47D cells assessed as reduction in cell viability incubated for 5 days by celltiter-glo assay Antiproliferative activity against human T47D cells assessed as reduction in cell viability incubated for 5 days by celltiter-glo assay	[PMID: 30996949]
ZR-75-1	EC₅₀	5 nM Compound: Borussertib	Antiproliferative activity against human ZR-75-1 cells assessed as reduction of cell growth measured after 5 days by CellTiter-Glo assay Antiproliferative activity against human ZR-75-1 cells assessed as reduction of cell growth measured after 5 days by CellTiter-Glo assay	[PMID: 31584233]
ZR-75-1	EC₅₀	5 nM Compound: Compound 1	Antiproliferative activity against human ZR-75-1 cells assessed as reduction in cell viability incubated for 5 days by celltiter-glo assay Antiproliferative activity against human ZR-75-1 cells assessed as reduction in cell viability incubated for 5 days by celltiter-glo assay	[PMID: 30996949]

In Vitro

Borussertib exhibits excellent cellular activity in the nanomolar range，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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

No. CAS 1800070-77-2
Appearance Solid
Peso molecular 596.68
Fòrmula C₃₆H₃₂N₆O₃
Color White to off-white
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
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (1)

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Cell Rep

Shear stress-induced Piezo1 activates CD99L2 to facilitate the initiation of blood circulation. [Abstract]

2026 Mar 30;45(4):117200. PMID: 41915472

Solvente y solubilidad

In Vitro:

DMSO : 25 mg/mL (41.90 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculadora de molaridad

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (271 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

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

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.6759 mL	8.3797 mL	16.7594 mL	41.8985 mL
	5 mM	0.3352 mL	1.6759 mL	3.3519 mL	8.3797 mL
	10 mM	0.1676 mL	0.8380 mL	1.6759 mL	4.1899 mL
	15 mM	0.1117 mL	0.5586 mL	1.1173 mL	2.7932 mL
	20 mM	0.0838 mL	0.4190 mL	0.8380 mL	2.0949 mL
	25 mM	0.0670 mL	0.3352 mL	0.6704 mL	1.6759 mL
	30 mM	0.0559 mL	0.2793 mL	0.5586 mL	1.3966 mL
	40 mM	0.0419 mL	0.2095 mL	0.4190 mL	1.0475 mL

Keywords

Borussertib

1 Cited Publications

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Borussertib

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Publications Citing Use of MedChemExpress (MCE) Borussertib

Ver todos los productos específicos de isoformas Akt

Actividad biológica

Chemical Information

Publications (1)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Borussertib Related Classifications

HY-122913 Related Classifications