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BDP9066

Cat. No. M21369
BDP9066 Structure
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Quality Control & Documentation
Biological Activity

BDP9066 is a selective and potent inhibitor of myotonic dystrophy-associated Cdc-42-binding kinase MRCK, with an IC50 value of 64 nM for MRCKβ and Ki values of 0.0136 nM and 0.0233 nM for MRCKα/β, respectively, measured in SCC12 cells.

Chemical Information
Molecular Weight 348.44
Formula C20H24N6
CAS Number 2226507-04-4
Solubility (25°C) DMSO : 10 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] Vanessa M Ruscetta, et al. Cells. Opportunities and Challenges for the Development of MRCK Kinases Inhibitors as Potential Cancer Chemotherapeutics

[2] Alison M Kurimchak, et al. Sci Signal. Functional proteomics interrogation of the kinome identifies MRCKA as a therapeutic target in high-grade serous ovarian carcinoma

[3] Joanna L Birch, et al. Cancer Res. A Novel Small-Molecule Inhibitor of MRCK Prevents Radiation-Driven Invasion in Glioblastoma

[4] Mathieu Unbekandt, et al. Cancer Res. Discovery of Potent and Selective MRCK Inhibitors with Therapeutic Effect on Skin Cancer

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