ABT-888 (Veliparib) |
| Catalog No.GC12422 |
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 912444-00-9
Sample solution is provided at 25 µL, 10mM.
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ABT-888, also named as Veliparib, is poly (ADP-ribose) polymerase (PARP) inhibitor and has demonstrated excellent in vivo efficacy in a broad spectrum of preclinical tumor models in combination with a variety of cytotoxic agents. PARP is involved in DNA repair and elevated PARP levels can result in resistance to cytotoxic chemotherapy and radiation. So, PARP inhibitors hold promise as chemotherapy and radiation sensitizers. ABT-888 is also active on microsatellite instability (MSI) cell lines harboring mutations in both MRE11 and RAD50 genes compared to microsatellite stable (MSS) cell lines (wild-type for both genes).
Reference
Shivaani Kummar, Robert Kinders, Martin E. Gutierrez, Larry Rubinstein, Ralph E. Parchment, Lawrence R. Phillips, Jiuping Ji, Anne Monks, Jennifer A. Low, Alice Chen, Anthony J. Murgo, Jerry Collins, Seth M. Steinberg, Helen Eliopoulos, Vincent L. Giranda, Gary Gordon, Lee Helman, Robert Wiltrout, Joseph E. Tomaszewski and James H. Doroshow. Phase 0 Clinical Trial of the Poly (ADP-Ribose) Polymerase Inhibitor ABT-888 in Patients With Advanced Malignancies. Journal of Clinical Oncology. 2009; 27(16): 2705 – 11.
Xiaofeng Li, Juergen Delzer, Richard Voorman, Sonia M. de Morais and Yanbin Lao. Disposition and Drug-Drug Interaction Potential of Veliparib (ABT-888), a Novel and Potent Inhibitor of Poly (ADP-ribose) Polymerase. DRUG METABOLISM AND DISPOSITION. 2011; 39(7): 1161 – 69.
E. Vilar Sanchez, A. Chow, L. Raskin, M. D. Iniesta, B. Mukherjee and S. B. Gruber. Preclinical testing of the PARP inhibitor ABT-888 in microsatellite instable colorectal cancer. Journal of Clinical Oncology. 2009; 27(15S): 11028A.
| Cell experiment: | |
|
Cell lines |
HCT-116 and HT-29 cell lines |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
|
Reaction Conditions |
4 μM; 24 h |
|
Applications |
In HCT-116 and HT-29 cell lines, the ability of ABT-888 to synergize the effect of the anti-cancer agents, SN38 or oxaliplatin, was determined using the SRB assay. PARP activity was significantly reduced in samples treated with SN38 in combination with ABT-888 (>4 fold at 24 h). |
| Animal experiment: | |
|
Animal models |
Female nude athymic mice |
|
Dosage form |
12.5 mg/kg; oral gavage twice daily in 6-hour intervals. |
|
Applications |
HCT116 xenografts were established in 5- to 6-week-old female nude athymic mice by subcutaneous flank injections of 200 mL cell suspension (5*106cells) per flank. This triple-therapy group (RT, CPT-11, and ABT) showed a significantly longer tumor growth delay (TGD) when compared with the tumors treated with RT and CPT-11 but no ABT-888, which had a mean TGD of 14.21 days. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1] Davidson D, Wang Y, Aloyz R, et al. The PARP inhibitor ABT-888 synergizes irinotecan treatment of colon cancer cell lines[J]. Investigational new drugs, 2013, 31(2): 461-468. [2] Shelton J W, Waxweiler T V, Landry J, et al. In vitro and in vivo enhancement of chemoradiation using the oral parp inhibitor ABT-888 in colorectal cancer cells[J]. International Journal of Radiation Oncology* Biology* Physics, 2013, 86(3): 469-476. | |
| Cas No. | 912444-00-9 | SDF | |
| Chemical Name | 1-[3-[4-amino-3-(4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidin-1-yl]prop-2-en-1-one | ||
| Canonical SMILES | CC1(CCCN1)C2=NC3=C(C=CC=C3N2)C(=O)N | ||
| Formula | C13H16N4O | M.Wt | 244.3 |
| Solubility | ≥ 6.1mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.0933 mL | 20.4666 mL | 40.9333 mL |
| 5 mM | 0.8187 mL | 4.0933 mL | 8.1867 mL |
| 10 mM | 0.4093 mL | 2.0467 mL | 4.0933 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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