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FRAX1036

Cat. No. M13705
FRAX1036 Structure
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Biological Activity

FRAX1036 is a PAK inhibitor with Kis of 23.3 nM, 72.4 nM, and 2.4 μM for PAK1, PAK2 and PAK4, respectively.

Chemical Information
Molecular Weight 518.05
CAS Number 1432908-05-8
Solubility (25°C) DMSO 5.3 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] Di Han, et al. Future Med Chem. Computational insight into the mechanisms of action and selectivity of Afraxis PAK inhibitors

[2] Cristina Uribe-Alvarez, et al. Small GTPases. Targeting effector pathways in RAC1 P29S-driven malignant melanoma

[3] Vladislav Korobeynikov, et al. Breast Cancer Res Treat. Combined inhibition of Aurora A and p21-activated kinase 1 as a new treatment strategy in breast cancer

[4] Christina M Knippler, et al. Endocr Relat Cancer. MAPK- and AKT-activated thyroid cancers are sensitive to group I PAK inhibition

[5] Chudi O Ndubaku, et al. ACS Med Chem Lett. Design of Selective PAK1 Inhibitor G-5555: Improving Properties by Employing an Unorthodox Low-pK a Polar Moiety

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  Catalog
Abmole Inhibitor Catalog




Keywords: FRAX1036 supplier, PAK, inhibitors, activators


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