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Tanzisertib

Cat. No. M9388
Tanzisertib Structure
Synonym:

CC-930

Size Price Availability Quantity
5mg USD 118 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

Tanzisertib (CC-930) is a potent JNK1/2/3 inhibitor with IC50s of 61/7/6 nM, respectively. Tanzisertib (1-2 μM) substantially reduces hepatocyte apoptosis and necrosis, abrogates apoptosis and necrosis in FC-loaded WT hepatocytes. 

In vivo, Tanzisertib (10 and 30 mg/kg, p.o.) inhibits the production of TNFa by 23% and 77% in the acute rat LPS-induced TNFa production PK-PD model.

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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 448.44
Formula C21H23F3N6O2
CAS Number 899805-25-5
Purity >98%
Solubility DMSO ≥ 26 mg/mL (warmed)
Storage at -20°C
References

Discovery of CC-930, an orally active anti-fibrotic JNK inhibitor.
Plantevin Krenitsky V, et al. Bioorg Med Chem Lett. 2012 Feb 1;22(3):1433-8. PMID: 22244937.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Tanzisertib, CC-930 supplier, JNK, inhibitors

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