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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
5mg USD 388  USD388 In stock
10mg USD 776  USD776 In stock
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Quality Control
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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 513.59
Formula C28H31N7O3
CAS Number 1893397-65-3
Purity 98.89%
Solubility DMSO ≥ 7 mg/mL
Storage at -20°C
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
Abmole Inhibitor Catalog 2017




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

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