Olaparib

Olaparib

10 mg

Cat. No.: 54-S12

$74.00

Olaparib is a potent small molecule inhibitor of the nuclear enzyme poly(ADP-ribose) polymerase (PARP). It acts by binding to PARP, inhibiting PARP-mediaed repair of single strand DNA breaks. PARP inhibition may enhance the cytotoxicity of DNA-damaging agents and may reverse tumor cell chemoresistance and radioresistance. PARP catalyzes post-translational ADP-ribosylation of nuclear proteins and can be activated by single-stranded DNA breaks.

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TECHNICAL INFORMATION

Other Names: 4-[[3-[[4-(cyclopropylcarbonyl)-1-piperazinyl]carbonyl]-4-fluorophenyl]methyl]-1(2H)-phthalazinone

Chemical Formula: C24H23FN4N4O3

CAS Number: 763113-22-0

Molecular Weight: 434.46

Purity: >99%

IC50= 1nM

Appearance: Crystalline Solid

Solubility: DMSO (100mM)

 

STORAGE AND HANDLING

Storage: Store at 4°C and protected from light. Following reconstitution, store  aliquots at -20°C. 

Stability: Stock solutions stable at -20°C for up to 2 years.

Shipping Conditions: Shipped at room temperature.

 

PRODUCT USE

Soluble in DMSO. Soluble at 20mg/ml

References

Pessetto | Z.Y. | et al. (2012). Inhibition of BRCT (BRCA1)-phosphoprotein interaction enhances the cytotoxic effect of olaparib in breast cancer cells: a proof of concert study for a synthetic lethal therapeutic option. Breast Cancer Res Threat.

Shimo | T. | et al. (2012). Antitumor and anticancer stem cell activity of a poly ADP-ribose polymerase inhibitors olaparib in breast cancer cells. Breast Cancer.

Ledermann | J. | et al (2012). Olaparib maintenance therapy in platinum-sensitive relapsed ovarian cancer. N. Engl. J. Med. 366:1382-92.

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