1. PROTAC Epigenetics Cell Cycle/DNA Damage
  2. PROTACs Aurora Kinase
  3. JB170

JB170 is a potent and highly specific PROTAC-mediated AURORA-A (Aurora Kinase) degrader (DC50=28 nM) by linking Alisertib, to the Cereblon-binding molecule Thalidomide. JB170 preferentially binds AURORA-A (EC50=193 nM) over AURORA-B (EC50=1.4 µM). JB170-mediated S-phase arrest is caused specifically by AURORA-A depletion. JB170 has excellent ability to inhibit non-catalytic function of AURORA-A kinase.

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

JB170 Chemical Structure

JB170 Chemical Structure

CAS No. : 2705844-82-0

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 848 In-stock
Solution
10 mM * 1 mL in DMSO USD 848 In-stock
Solid
5 mg USD 480 In-stock
10 mg USD 800 In-stock
25 mg USD 1550 In-stock
50 mg USD 2400 In-stock
100 mg USD 3600 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

JB170 is a potent and highly specific PROTAC-mediated AURORA-A (Aurora Kinase) degrader (DC50=28 nM) by linking Alisertib, to the Cereblon-binding molecule Thalidomide. JB170 preferentially binds AURORA-A (EC50=193 nM) over AURORA-B (EC50=1.4 µM). JB170-mediated S-phase arrest is caused specifically by AURORA-A depletion. JB170 has excellent ability to inhibit non-catalytic function of AURORA-A kinase[1].

IC50 & Target[1]

Aurora A

28 nM (DC50)

Aurora A

99 nM (Kd)

Aurora A

193 nM (EC50)

Cereblon

 

In Vitro

JB170 (1 μM; 24-72 hours; MV4-11 cells) mediates Aurora-A depletion inhibiting cancer cell survival[1].
JB170 (0.01-10 μM; 6 hours; MV4-11 cells) reduces AURORA-A levels [1].
JB170 (0.5 μM; 12 hours; MV4-11 cells) delays/arrests S-phase progression[1].
JB170 (0.5 μM; 0-72 hours; MV4-11 cells) induces apoptosis is exclusively caused by targeting AURORA-A[1].
JB170 (0.1 μM; 0-9 hours; IMR5 cells) shows rapid AURORA-A depletion. JB170 (0~1 μM; 6 hours; MV4-11 cells) strongly attenuates in mutants with respect to AURORA-A. JB170 (0.1 μM; 18 hours; MV4-11 cells) does not activate AURORA-A. JB170 (0~1 μM; 24 hours; IMR5 cells) largely abrogates AURORA-AT217D depletion. JB170 (1 μM; 4 days; IMR5 cells) mediates Aurora-A depletion inhibiting cancer cell survival. JB170 (IMR5 cells) reduces AURORA-A levels by lowering AURORA-A mRNA levels[1].

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

Cell Viability Assay[1]

Cell Line: MV4-11 cells
Concentration: 1 µM
Incubation Time: 24-72 hours
Result: After 72 hours, the number of viable cells was 32% of control levels.

Western Blot Analysis[1]

Cell Line: MV4-11 cells
Concentration: 0.01~10 μM
Incubation Time: 6 hours
Result: Substantial degradation was observed at 100 nM and 1 µM.

Apoptosis Analysis[1]

Cell Line: MV4-11 cells
Concentration: 0.5 µM
Incubation Time: 0~72 hours
Result: Apoptosis was exclusively caused by targeting AURORA-A.

Cell Cycle Analysis[1]

Cell Line: MV4-11 cells
Concentration: 0.5 µM
Incubation Time: 12 hours
Result: Delayed or arrested S-phase progression.
Molecular Weight

963.36

Formula

C48H44ClFN8O11

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

FC1=CC=CC(OC)=C1C2=NCC3=C(C4=C2C=C(C=C4)Cl)N=C(NC5=CC=C(C(OC)=C5)C(NCCOCCOCCNC(COC6=C7C(C(N(C7=O)C8CCC(NC8=O)=O)=O)=CC=C6)=O)=O)N=C3

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 : 100 mg/mL (103.80 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.0380 mL 5.1902 mL 10.3803 mL
5 mM 0.2076 mL 1.0380 mL 2.0761 mL
View the Complete Stock Solution Preparation Table

* 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • Dilution Calculator

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

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In Vivo:

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

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    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (2.60 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.0380 mL 5.1902 mL 10.3803 mL 25.9508 mL
5 mM 0.2076 mL 1.0380 mL 2.0761 mL 5.1902 mL
10 mM 0.1038 mL 0.5190 mL 1.0380 mL 2.5951 mL
15 mM 0.0692 mL 0.3460 mL 0.6920 mL 1.7301 mL
20 mM 0.0519 mL 0.2595 mL 0.5190 mL 1.2975 mL
25 mM 0.0415 mL 0.2076 mL 0.4152 mL 1.0380 mL
30 mM 0.0346 mL 0.1730 mL 0.3460 mL 0.8650 mL
40 mM 0.0260 mL 0.1298 mL 0.2595 mL 0.6488 mL
50 mM 0.0208 mL 0.1038 mL 0.2076 mL 0.5190 mL
60 mM 0.0173 mL 0.0865 mL 0.1730 mL 0.4325 mL
80 mM 0.0130 mL 0.0649 mL 0.1298 mL 0.3244 mL
100 mM 0.0104 mL 0.0519 mL 0.1038 mL 0.2595 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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JB170
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