AZD 2281 (Olaparib, KU-0059436) is a novel, potent orally active PARP (poly ADP-ribose polymerase) inhibitorwith IC50 of 5 and 1 nM for PARP-1and PARP-2 respectively. AZD 2281 (Olaparib, KU-0059436) acts as an inhibitor of the enzyme Poly ADP ribose polymerase (PARP) and is one of the first PARP inhibitors.It induces cancer specific synthetic lethality in homologous recombination repair defective cells, including BRCA-deficient tumors.
BMC Biol. 2021 May 20;19(1):108.
Very long intergenic non-coding (vlinc) RNAs directly regulate multiple genes in cis and trans
AZD2281 (Olaparib) purchased from AbMole
Int J Biol Sci. 2021 Jan 31;17(3):689-701.
Preclinical evaluation of radiation therapy of BRCA1-associated mammary tumors using a mouse model
AZD2281 (Olaparib) purchased from AbMole
Cell. 2019 Jun 13;177(7):1903-1914.e14.
Visualizing Engrafted Human Cancer and Therapy Responses in Immunodeficient Zebrafish.
AZD2281 (Olaparib) purchased from AbMole
Clin Cancer Res. 2019 Mar 1;25(5):1664-1675.
The Ewing Family of Tumors Relies on BCL-2 and BCL-XL to Escape PARP Inhibitor Toxicity.
AZD2281 (Olaparib) purchased from AbMole
Int J Biol Sci. 2018 Oct 3;14(13):1769-1781.
Inhibition of AKT suppresses the initiation and progression of BRCA1-associated mammary tumors.
AZD2281 (Olaparib) purchased from AbMole
Cell Experiment | |
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Cell lines | SW620 colorectal cell line |
Preparation method | Potentiation of MMS Cytotoxicity by 47 Determined by the Use of Sulforhodamine B Cell Growth Assays. SW620 cells were seeded in 96-well plates and were left to attach overnight. Cells were preincubated with vehicle control (DMSO) or with a single concentration of KU-0059436 (1, 3, 10, 30, 100 or 300 nM) for 1 h before the addition of increasing concentrations of MMS. Cells were incubated in the presence of each drug combination for 4 days before cell growth was quantified by the use of an SRB assay.44 Data were calculated from triplicate wells as the mean percentage of cell growth relative to KU-0059436-only wells, and (SE and IC50 were calculated by the use of XL-FIT 4 software. SW620 cells showed <24% growth inhibition (>76% cell growth) when only KU-0059436 was used at concentrations below 300 nM (data not shown). |
Concentrations | 1, 3, 10, 100 and 300 nM |
Incubation time | 4 days |
Animal Experiment | |
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Animal models | mouse bearing SW620 xenografted tumors |
Formulation | methylcellulose/PBS |
Dosages | 10 mg/kg once daily for 5 consecutive days |
Administration | orally |
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.
Molecular Weight | 434.46 |
Formula | C24H23FN4O3 |
CAS Number | 763113-22-0 |
Purity | 99.86% |
Solubility | DMSO 80 mg/mL |
Storage | at -20°C |
[5] Marchetti et al. Expert Opin Investig Drugs. Olaparib , PARP1 inhibitor in ovarian cancer.
Related PARP Products |
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KSQ-4279
Usp1-in-1 (Formula I), an allosteric INHIBITOR of USP1, has been used IN cancer studies alone or IN combination with PARP inhibition. |
Fluzoparib (SHR3162)
Fluzoparib (SHR3162) is an effective oral active PARP1 inhibitor (IC50=1.46±0.72 nM) with superior antitumor activity. Fluzoparib selectively inhibited the proliferation of homologous recombination repair (HR) deficient cells and sensitized HR deficient cells to cytotoxic drugs. Fluzoparib has good pharmacokinetic properties in vivo and can be used in cancer research. |
AZD5305
AZD5305 is a potent and oral active, second-generation PARP (highly selective PARP1) inhibitor. |
BRCA1-IN-2
BRCA1-IN-2 is a cell-permeable protein-protein interaction (PPI) inhibitor for BRCA1, with IC50 of 0.31 μM and Kd of 0.3 μM. |
RBN-2397
RBN-2397 is a potent and orally active NAD+ competitive inhibitor of PARP7 (IC50<3 nM). |
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