1. NF-κB
  2. IKK
  3. BAY-985

BAY-985 

Cat. No.: HY-133117 Purity: 99.87%
Handling Instructions

BAY-985 is a highly potent, orally active and selective ATP-competitive dual inhibitor of TBK1 and IKKε with IC50s of 2/30 and 2 nM for TBK1 (low/high ATP) and IKKε, respectively. Antitumor efficacy.

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

BAY-985 Chemical Structure

BAY-985 Chemical Structure

CAS No. : 2409479-29-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 670 In-stock
Estimated Time of Arrival: December 31
5 mg USD 550 In-stock
Estimated Time of Arrival: December 31
10 mg USD 880 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1950 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of BAY-985:

Top Publications Citing Use of Products

View All IKK Isoform Specific Products:

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

BAY-985 is a highly potent, orally active and selective ATP-competitive dual inhibitor of TBK1 and IKKε with IC50s of 2/30 and 2 nM for TBK1 (low/high ATP) and IKKε, respectively. Antitumor efficacy[1].

IC50 & Target[1]

TBK1

2 nM (IC50, low ATP)

TBK1

30 nM (IC50, high ATP)

IKKε

2 nM (IC50)

In Vitro

BAY-985 inhibits FLT3, RSK4, DRAK1, and ULK1 with IC50s of 123, 276, 311, and 7930 nM, respectively[1].
BAY-985 inhibits the cellular phosphorylation of interferon regulatory factor 3 (IRF3) with an IC50 of 74 nM[1].
BAY-985 is active in cellular mechanistic assay and shows anti-proliferative activity in a few cancer cell lines with IC50s of 900 and 7260 nM for SK-MEL2 (NRAS and TP53 mutated) and ACHN (CDKN2A mutated) cells, respectively[1].

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

Cell Proliferation Assay[1]

Cell Line: ACHN and SK-MEL-2 cell lines
Concentration:
Incubation Time: 96 hours
Result: Inhibited proliferation in SK-MEL2 and ACHN cells with IC50s of 900 and 7260 nM, respectively.
In Vivo

BAY-985 (200 mg/kg; p.o.; b.i.d.; 111 days) results in weak antitumor efficacy[1].
BAY-985 shows high clearance (CLb= 4.0 L/h/kg, ca. 95% hepatic extraction), large volume of distribution at steady state (Vss=2.9 L/kg) and a short terminal half-life (t1/2=0.79 h)[1].

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

Animal Model: Female NMRI nude mice bearing SK-MEL-2 human melanoma xenograft model[1]
Dosage: 200 mg/kg
Administration: Applied p.o.; twice daily (b.i.d.) continuously 111 days
Result: Treatment resulted in weak antitumor efficacy with a T/Ctumor weight ratio of 0.6.
The treatment was well tolerated, with a maximum body weight loss of less than 10%.
Molecular Weight

553.58

Formula

C₂₇H₃₀F₃N₉O

CAS No.

2409479-29-2

SMILES

O=C(N1CCN([[email protected]@H](C2=CC(NC3=NC4=CC=C(C5=NC=NC(N(C)C)=C5)C=C4N3)=NC=C2)C)CC1)CC(F)(F)F

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 : 50 mg/mL (90.32 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8064 mL 9.0321 mL 18.0642 mL
5 mM 0.3613 mL 1.8064 mL 3.6128 mL
10 mM 0.1806 mL 0.9032 mL 1.8064 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 (3.76 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.76 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (3.76 mM); Clear solution

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

Purity: 99.87%

  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

BAY-985BAY985BAY 985IKKIκB kinaseI kappa B kinaseTBK1IKKεantitumormelanomaInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
BAY-985
Cat. No.:
HY-133117
Quantity:
MCE Japan Authorized Agent: