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CFI-400945

Cat. No. M20605
CFI-400945 Structure
Size Price Availability Quantity
5mg USD 150  USD150 In stock
25mg USD 490  USD490 In stock
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Quality Control & Documentation
Biological Activity

CFI-400945 is an orally active, potent and selective polo-like kinase 4(PLK4) inhibitor with Ki value of 0.26 nM.

Chemical Information
Molecular Weight 534.65
Formula C33H34N4O3
CAS Number 1338806-73-7
Solubility (25°C) DMSO 100 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] Cerise Yuen-Ki Chan, et al. Hepatology. Polo-like kinase 4 inhibitor CFI-400945 suppresses liver cancer through cell cycle perturbation and eliciting antitumor immunity

[2] Maaged Abdullah, et al. Chem Biol Drug Des. Identification of 3D motifs based on sequences and structures for binding to CFI-400945, and deep screening-based design of new lead molecules for PLK-4

[3] Sophie L Kerschner-Morales, et al. J Cancer Res Clin Oncol. Anticancer effects of the PLK4 inhibitors CFI-400945 and centrinone in Ewing's sarcoma cells

[4] Zachary W Veitch, et al. Br J Cancer. Safety and tolerability of CFI-400945, a first-in-class, selective PLK4 inhibitor in advanced solid tumours: a phase 1 dose-escalation trial

[5] Karen Oegema, et al. Proc Natl Acad Sci U S A. CFI-400945 is not a selective cellular PLK4 inhibitor

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