2. NF-κB
  3. IKK
  4. BAY-985

BAY-985, a chemical probe, 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.

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BAY-985

BAY-985 構造式

CAS 番号 : 2409479-29-2

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 548 在庫あり
Solution
10 mM * 1 mL in DMSO USD 548 在庫あり
Solid
1 mg $214 在庫あり
5 mg $450 在庫あり
10 mg $675 在庫あり
25 mg $1147 在庫あり
50 mg $1605 在庫あり
100 mg $2245 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Based on 4 publication(s) in Google Scholar

Other Forms of BAY-985:

BAY-985 関連抗体

Top Publications Citing Use of Products

IKK アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
IKK-α IKK-β IKK IKKε TBK1

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  • 純度とドキュメンテーション

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製品説明

BAY-985, a chemical probe, 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)

Cellular Effect
Cell Line Type Value Description References
ACHN IC50
7260 1
Compound: 34; BAY-985
Antiproliferative activity against human ACHN cells harboring CDKN2A mutation assessed as reduction in cell viability after 96 hrs by CellTiter-Glo luminescence assay
Antiproliferative activity against human ACHN cells harboring CDKN2A mutation assessed as reduction in cell viability after 96 hrs by CellTiter-Glo luminescence assay
[PMID: 31859507]
Sf21 IC50
123 1
Compound: 34; BAY-985
Inhibition of recombinant human N-terminal GST-tagged FLT3 (564 to end residues) expressed in sf21 cells using biotin labelled Ahx-GGEEEEYFELVKKKK peptide as substrate preincubated with enzyme for 15 mins followed by substrate addition and further incubat
Inhibition of recombinant human N-terminal GST-tagged FLT3 (564 to end residues) expressed in sf21 cells using biotin labelled Ahx-GGEEEEYFELVKKKK peptide as substrate preincubated with enzyme for 15 mins followed by substrate addition and further incubat
[PMID: 31859507]
ACHN IC50
7260 1
Compound: 34; BAY-985
Antiproliferative activity against human ACHN cells harboring CDKN2A mutation assessed as reduction in cell viability after 96 hrs by CellTiter-Glo luminescence assay
Antiproliferative activity against human ACHN cells harboring CDKN2A mutation assessed as reduction in cell viability after 96 hrs by CellTiter-Glo luminescence assay
[PMID: 31859507]
Sf21 IC50
123 1
Compound: 34; BAY-985
Inhibition of recombinant human N-terminal GST-tagged FLT3 (564 to end residues) expressed in sf21 cells using biotin labelled Ahx-GGEEEEYFELVKKKK peptide as substrate preincubated with enzyme for 15 mins followed by substrate addition and further incubat
Inhibition of recombinant human N-terminal GST-tagged FLT3 (564 to end residues) expressed in sf21 cells using biotin labelled Ahx-GGEEEEYFELVKKKK peptide as substrate preincubated with enzyme for 15 mins followed by substrate addition and further incubat
[PMID: 31859507]
Sf21 IC50
276 1
Compound: 34; BAY-985
Inhibition of recombinant full length human His6-tagged RSK4 expressed in baculovirus infected sf21 cells using biotin labelled Ahx-KKLNRTLSFAEPG peptide as substrate preincubated with enzyme for 15 mins followed by substrate addition and further incubate
Inhibition of recombinant full length human His6-tagged RSK4 expressed in baculovirus infected sf21 cells using biotin labelled Ahx-KKLNRTLSFAEPG peptide as substrate preincubated with enzyme for 15 mins followed by substrate addition and further incubate
[PMID: 31859507]
Sf21 IC50
276 1
Compound: 34; BAY-985
Inhibition of recombinant full length human His6-tagged RSK4 expressed in baculovirus infected sf21 cells using biotin labelled Ahx-KKLNRTLSFAEPG peptide as substrate preincubated with enzyme for 15 mins followed by substrate addition and further incubate
Inhibition of recombinant full length human His6-tagged RSK4 expressed in baculovirus infected sf21 cells using biotin labelled Ahx-KKLNRTLSFAEPG peptide as substrate preincubated with enzyme for 15 mins followed by substrate addition and further incubate
[PMID: 31859507]
SK-MEL-2 IC50
900 1
Compound: 34; BAY-985
Antiproliferative activity against human SK-MEL-2 cells harboring NRAS/TP53 mutation assessed as reduction in cell viability after 96 hrs by CellTiter-Glo luminescence assay
Antiproliferative activity against human SK-MEL-2 cells harboring NRAS/TP53 mutation assessed as reduction in cell viability after 96 hrs by CellTiter-Glo luminescence assay
[PMID: 31859507]
ACHN IC50
7260 1
Compound: 34; BAY-985
Antiproliferative activity against human ACHN cells harboring CDKN2A mutation assessed as reduction in cell viability after 96 hrs by CellTiter-Glo luminescence assay
Antiproliferative activity against human ACHN cells harboring CDKN2A mutation assessed as reduction in cell viability after 96 hrs by CellTiter-Glo luminescence assay
[PMID: 31859507]
SK-MEL-2 IC50
900 1
Compound: 34; BAY-985
Antiproliferative activity against human SK-MEL-2 cells harboring NRAS/TP53 mutation assessed as reduction in cell viability after 96 hrs by CellTiter-Glo luminescence assay
Antiproliferative activity against human SK-MEL-2 cells harboring NRAS/TP53 mutation assessed as reduction in cell viability after 96 hrs by CellTiter-Glo luminescence assay
[PMID: 31859507]
SK-MEL-2 IC50
900 1
Compound: 34; BAY-985
Antiproliferative activity against human SK-MEL-2 cells harboring NRAS/TP53 mutation assessed as reduction in cell viability after 96 hrs by CellTiter-Glo luminescence assay
Antiproliferative activity against human SK-MEL-2 cells harboring NRAS/TP53 mutation assessed as reduction in cell viability after 96 hrs by CellTiter-Glo luminescence assay
[PMID: 31859507]
Sf21 IC50
123 1
Compound: 34; BAY-985
Inhibition of recombinant human N-terminal GST-tagged FLT3 (564 to end residues) expressed in sf21 cells using biotin labelled Ahx-GGEEEEYFELVKKKK peptide as substrate preincubated with enzyme for 15 mins followed by substrate addition and further incubat
Inhibition of recombinant human N-terminal GST-tagged FLT3 (564 to end residues) expressed in sf21 cells using biotin labelled Ahx-GGEEEEYFELVKKKK peptide as substrate preincubated with enzyme for 15 mins followed by substrate addition and further incubat
[PMID: 31859507]
Sf21 IC50
276 1
Compound: 34; BAY-985
Inhibition of recombinant full length human His6-tagged RSK4 expressed in baculovirus infected sf21 cells using biotin labelled Ahx-KKLNRTLSFAEPG peptide as substrate preincubated with enzyme for 15 mins followed by substrate addition and further incubate
Inhibition of recombinant full length human His6-tagged RSK4 expressed in baculovirus infected sf21 cells using biotin labelled Ahx-KKLNRTLSFAEPG peptide as substrate preincubated with enzyme for 15 mins followed by substrate addition and further incubate
[PMID: 31859507]
体外実験

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].

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

BAY-985 関連抗体

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.
体内実験

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].

MedChemExpress (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%.
分子量

553.58

分子式

C27H30F3N9O
CAS 番号
Appearance

Solid

Color

Light yellow to yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 50 mg/mL (90.32 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 1.8064 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
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, 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.

  • Molarity Calculator

  • Dilution Calculator

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

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一般には略語で表示されます：C1V1 = C2V2

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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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (3.76 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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g

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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% 
+
%
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%
Saline
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.
純度とドキュメンテーション

純度: 99.69%

COA (246 KB) HNMR (241 KB) LCMS (96 KB)

取扱説明書 (2659 KB)
参考文献

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, 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 1.8064 mL 9.0321 mL 18.0642 mL 45.1606 mL
5 mM 0.3613 mL 1.8064 mL 3.6128 mL 9.0321 mL
10 mM 0.1806 mL 0.9032 mL 1.8064 mL 4.5161 mL
15 mM 0.1204 mL 0.6021 mL 1.2043 mL 3.0107 mL
20 mM 0.0903 mL 0.4516 mL 0.9032 mL 2.2580 mL
25 mM 0.0723 mL 0.3613 mL 0.7226 mL 1.8064 mL
30 mM 0.0602 mL 0.3011 mL 0.6021 mL 1.5054 mL
40 mM 0.0452 mL 0.2258 mL 0.4516 mL 1.1290 mL
50 mM 0.0361 mL 0.1806 mL 0.3613 mL 0.9032 mL
60 mM 0.0301 mL 0.1505 mL 0.3011 mL 0.7527 mL
80 mM 0.0226 mL 0.1129 mL 0.2258 mL 0.5645 mL
  • No file chosen (Maximum size is: 1024 Kb)
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BAY-985 Related Classifications

  • Molarity Calculator

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The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
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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.

Keywords:

BAY-9852409479-29-2BAY985BAY 985IKKIκB kinaseI kappa B kinaseTBK1IKKεantitumormelanomaInhibitorinhibitorinhibit

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