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BQU57

Cat. No. M20607
BQU57 Structure
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Biological Activity

BQU57, a derivative of RBC8, is a selective GTPase Ral inhibitor relative to the GTPases Ras and RhoA.

Chemical Information
Molecular Weight 334.10
Formula C16H13F3N4O
CAS Number 1637739-82-2
Solubility (25°C) DMSO 66 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] Katie A Thies, et al. Breast Cancer Res. The small G-protein RalA promotes progression and metastasis of triple-negative breast cancer

[2] Siddhi Inchanalkar, et al. Mol Pharm. Polymer Nanovesicle-Mediated Delivery of MLN8237 Preferentially Inhibits Aurora Kinase A To Target RalA and Anchorage-Independent Growth in Breast Cancer Cells

[3] Chao Yan, et al. Nature. Discovery and characterization of small molecules that target the GTPase Ral

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  Catalog
Abmole Inhibitor Catalog




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