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CFI-400945 fumarate

Chemical Structure : CFI-400945 fumarate

CAS No.: 1616420-30-4

CFI-400945 fumarate (CFI400945, Ocifisertib)

Catalog No.: PC-63238Not For Human Use, Lab Use Only.

CFI-400945 (Ocifisertib) fumarate is a potent, highly selective, orally available PLK4 inhibitor with Ki of 0.26 nM and IC50 of 2.8 nM, does not significantly inhibits PLK1/2/3 at 50 uM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

CFI-400945 (Ocifisertib) fumarate is a potent, highly selective, orally available PLK4 inhibitor with Ki of 0.26 nM and IC50 of 2.8 nM, does not significantly inhibits PLK1/2/3 at 50 uM.
CFI-400945 causes dysregulated centriole duplication, mitotic defects, and cell death in multiple cancer cell lines (A549 GI50=5 nM, OVCAR-3 GI50=18 nM).
CFI-400945 significantly inhibits human cancer xenografts; causes polyploidy, growth inhibition, and apoptotic death of murine and human lung cancer cells, despite expression of mutated KRAS or p53, produces supernumerary centrosomes and mitotic defects in lung cancer cells.

Physicochemical Properties

M.Wt 650.732
Formula C37H38N4O7
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 166.66 mg/mL

Chemical Name/SMILES

Spiro[cyclopropane-1,3'-[3H]indol]-2'(1'H)-one, 2-[3-[(1E)-2-[4-[[(2R,6S)-2,6-dimethyl-4-morpholinyl]methyl]phenyl]ethenyl]-1H-indazol-6-yl]-5'-methoxy-, (1R,2S)-, fumarate

References

1. Sampson PB, et al. J Med Chem. 2015 Jan 8;58(1):147-69.

2. Mason JM, et al. Cancer Cell. 2014 Aug 11;26(2):163-76.

3. Lohse I, et al. Oncotarget. 2017 Jan 10;8(2):3064-3071.

4. Kawakami M, et al. Proc Natl Acad Sci U S A. 2018 Feb 20;115(8):1913-1918.

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