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Telaglenastat hydrochloride

Cat. No. M21510
Telaglenastat hydrochloride Structure
Synonym:

CB-839 hydrochloride

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Quality Control & Documentation
Biological Activity

Telaglenastat (CB-839) hydrochloride is a pioneering (first-in-class), selective, reversible, orally active glutaminase 1 (GLS1) inhibitor. Telaglenastat hydrochloride has IC50 values of 23 nM and 28 nM for endogenous glutaminase in the kidney and brain of mice, respectively. Telaglenastat hydrochloride also induces autophagy and has strong antitumor activity.

Chemical Information
Molecular Weight 608.04
Formula C26H25ClF3N7O3S
CAS Number 1874231-60-3
Solubility (25°C) N/A
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.

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