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L-778123

Cat. No. M42399
L-778123 Structure
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Biological Activity

L-778123 is an inhibitor of FPTase and GGPTase-I with IC50 of 2 nM and 98 nM in enzyme inhibition determination.

Chemical Information
Molecular Weight 405.88
Formula C22H20ClN5O
CAS Number 183499-57-2
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] Tanmoy Saha et al. Nat Nanotechnol. Intercellular nanotubes mediate mitochondrial trafficking between cancer and immune cells

[2] Saeed Ghasemi et al. Adv Pharm Bull. Comparison of Cytotoxic Activity of L778123 as a Farnesyltranferase Inhibitor and Doxorubicin against A549 and HT-29 Cell Lines

[3] M Bayés et al. Methods Find Exp Clin Pharmacol. Gateways to clinical trials

[4] M Bayés et al. Methods Find Exp Clin Pharmacol. Gateways to clinical trials

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Keywords: L-778123 supplier, Farnesyl Transferase, inhibitors, activators


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