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TIC10 Analogue

Cat. No. M20592
TIC10 Analogue Structure
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Biological Activity

TIC10 Analogue is an analogue of TIC10, which inactivates Akt and ERK to induce TRAIL through Foxo3a, possesses superior drug properties: delivery across the blood-brain barrier, superior stability and improved pharmacokinetics. Phase 1/2.

Chemical Information
Molecular Weight 386.49
Formula C24H26N4O
CAS Number 41276-02-2
Solubility (25°C) DMSO 11 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] Samuel Jacques, et al. Genetics. Imipridone Anticancer Compounds Ectopically Activate the ClpP Protease and Represent a New Scaffold for Antibiotic Development

[2] Paul R Graves, et al. ACS Chem Biol. Mitochondrial Protease ClpP is a Target for the Anticancer Compounds ONC201 and Related Analogues

[3] Masayuki Yamaji, et al. Cancer Med. Novel ATP-competitive Akt inhibitor afuresertib suppresses the proliferation of malignant pleural mesothelioma cells

[4] Paul Oguadinma, et al. Bioorg Med Chem Lett. NMR strategies to support medicinal chemistry workflows for primary structure determination

[5] Joshua E Allen, et al. Oncotarget. Discovery and clinical introduction of first-in-class imipridone ONC201

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Keywords: TIC10 Analogue supplier, Akt, inhibitors, activators


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