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TBK1/IKKε-IN-5

Cat. No. M9546
TBK1/IKKε-IN-5 Structure
Synonym:

ABM-7653; TBK1/IKK-epsilon-IN-5

Size Price Availability Quantity
1mg USD 190  USD190 In stock
5mg USD 390  USD390 In stock
10mg USD 625  USD625 In stock
25mg USD 1240  USD1240 In stock
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Quality Control & Documentation
Biological Activity

TBK1/IKKε-IN-5 (compound 1) is a dual TBK1 and IKKε inhibitor, with IC50 values of 1 nM and 5.6 nM for TBK1 and IKKε, respectively. TBK1/IKKε inhibition enhances response to PD-1 blockade, which effectively predicts tumor response in vivo. TBK1/IKKε-IN-5 (compound 1) effectively blocks immune suppressive cytokine elaboration by CT26 cell line spheroids, without cytotoxic effects, and enhances secretion of IL-2 and IFN-γ from purified CD4+ and CD8+ T cells from healthy human donors and IL-2 from Jurkat human T-cell leukemia cells.

Chemical Information
Molecular Weight 513.59
Formula C28H31N7O3
CAS Number 1893397-65-3
Solubility (25°C) DMSO ≥ 7 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Russell W Jenkins, et al. Cancer Discov. Ex Vivo Profiling of PD-1 Blockade Using Organotypic Tumor Spheroids.

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  Catalog
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Keywords: TBK1/IKKε-IN-5, ABM-7653; TBK1/IKK-epsilon-IN-5 supplier, IκB/IKK, inhibitors, activators


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