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1A-116

Cat. No. M14051
1A-116 Structure
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Biological Activity

1A-116 is a Rac1 inhibitor, with antitumoral and antimetastatic effects in several types of cancer, such as breast cancer. 1A-116 prevents Rac1-regulated processes involved in the primary tumorigenesis and metastastic processes .

Chemical Information
Molecular Weight 307.31
CAS Number 1430208-73-3
Solubility (25°C) DMSO 90 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] Laura Luca Trebucq, et al. Timing of Novel Drug 1A-116 to Circadian Rhythms Improves Therapeutic Effects against Glioblastoma

[2] Nazareno Gonzlez, et al. Computational and in vitro Pharmacodynamics Characterization of 1A-116 Rac1 Inhibitor: Relevance of Trp56 in Its Biological Activity

[3] Maia Cabrera, et al. Pharmacological Rac1 inhibitors with selective apoptotic activity in human acute leukemic cell lines

[4] N Gonzalez, et al. Pharmacological inhibition of Rac1-PAK1 axis restores tamoxifen sensitivity in human resistant breast cancer cells

[5] Iakov N Rudenko, et al. Is inhibition of kinase activity the only therapeutic strategy for LRRK2-associated Parkinson's disease?

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Keywords: 1A-116 supplier, Ras, inhibitors, activators


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