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Tanzisertib

Cat. No. M9388
Tanzisertib Structure
Synonym:

CC-930

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 95  USD95 In stock
10mg USD 160  USD160 In stock
25mg USD 345  USD345 In stock
50mg USD 640  USD640 In stock
100mg USD 1100  USD1100 In stock
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Quality Control & Documentation
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.

Chemical Information
Molecular Weight 448.44
Formula C21H23F3N6O2
CAS Number 899805-25-5
Solubility (25°C) DMSO ≥ 26 mg/mL (warmed)
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] Plantevin Krenitsky V, et al. Bioorg Med Chem Lett. Discovery of CC-930, an orally active anti-fibrotic JNK inhibitor.

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


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