T0070907 |
Catalog No.GC12820
One-Click Copy Product Info
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T0070907 is a potent and selective peroxisome proliferator-activated receptor γ (PPARγ) antagonist with an IC50 value of 1nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 313516-66-4
Sample solution is provided at 25 µL, 10mM.
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T0070907 is a potent and selective peroxisome proliferator-activated receptor γ (PPARγ) antagonist with an IC50 value of 1nM[1]. T0070907 is an anti-microtubule drug that can reduce α and β tubulin in colon cancer cells[2]. T0070907 can inhibit adipogenesis and induce rapid apoptosis of immature adipocytes[3].
In vitro, T0070907 (0.1-20μM) treatment of breast cancer MB-231 cells for 48h inhibited cell migration and invasion in a dose-dependent manner[4]. T0070907 (50μM) treatment of liver cancer HepG2 and Hep3B cells for 48h prevented cell reattachment to extracellular matrix (ECM) proteins and induced cell anoikis[5].
In vivo, oral administration of T0070907 (1, 5mg/kg/day) for 4 weeks to mice bearing HT-29 cell xenografts significantly reduced the number of liver tumor metastases and the size of tumor tissue in mice[6].
References:
[1] Lee G, Elwood F, McNally J, et al. T0070907, a selective ligand for peroxisome proliferator-activated receptor γ, functions as an antagonist of biochemical and cellular activities[J]. Journal of Biological Chemistry, 2002, 277(22): 19649-19657.
[2] An Z, Yu J R, Park W Y. T0070907 inhibits repair of radiation-induced DNA damage by targeting RAD51[J]. Toxicology In Vitro, 2016, 37: 1-8.
[3] Kawahara A, Haraguchi N, Tsuchiya H, et al. Peroxisome proliferator-activated receptor γ (PPARγ)-independent specific cytotoxicity against immature adipocytes induced by PPARγ antagonist T0070907[J]. Biological and Pharmaceutical Bulletin, 2013, 36(9): 1428-1434.
[4] Zaytseva Y Y, Wallis N K, Southard R C, et al. The PPARγ antagonist T0070907 suppresses breast cancer cell proliferation and motility via both PPARγ-dependent and-independent mechanisms[J]. Anticancer research, 2011, 31(3): 813-823.
[5] Schaefer K L, Wada K, Takahashi H, et al. Peroxisome proliferator-activated receptor γ inhibition prevents adhesion to the extracellular matrix and induces anoikis in hepatocellular carcinoma cells[J]. Cancer Research, 2005, 65(6): 2251-2259.
[6] Schaefer K L, Takahashi H, Morales V M, et al. PPARγ inhibitors reduce tubulin protein levels by a PPARγ, PPARδ and proteasome‐independent mechanism, resulting in cell cycle arrest, apoptosis and reduced metastasis of colorectal carcinoma cells[J]. International journal of cancer, 2007, 120(3): 702-713.
| Cell experiment [1]: | |
Cell lines | MB-231 cells |
Preparation Method | Transwell inserts (8μm pore size) were coated with collagen type I. Cells were pre-treated with 0.1, 1, 10, 20μM T0070907 or empty vehicle for 48h, then trypsinized and resuspended in serum-free DMEM containing 1% bovine serum albumin (BSA) to achieve a density of 3×105 cells/mL. Inserts were placed in wells containing normal growth media. A volume of 200μL of cell suspension was added to the upper chamber and incubated at 37˚C with 5% CO2 for 6h. After incubation, the upper side of membrane was washed and wiped-off using cotton swabs and then cells on the lower membrane surface were fixed with methanol and stained with 0.5% crystal violet. The images of five random fields per well were taken using ×40 objective and the number of migrated cells was counted. |
Reaction Conditions | 0.1, 1, 10, 20μM; 48h |
Applications | T0070907 treatment reduced cell migration in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Male severe combined immunodeficiency (SCID) mice |
Preparation Method | Male severe combined immunodeficiency (SCID) mice, 6 weeks of age, were maintained in a specific pathogen-free environment. At day 0, 2×106 HT-29 cells were injected into the spleen. After inoculation, the mice were randomized into 2 treatment groups and 1 control group. Starting at day 1 and daily thereafter, T0070907 (1 or 5mg/kg/day) or control (1% DMSO vehicle) was administered orally. These con centrations were chosen based on initial pilot experiments to detect morbidity based on T0070907 alone. At 1 or 5 mg/kg/day, no increased morbidity (based on grooming, activity and food intake) was noted in mice with or without injected tumor cells. Four weeks later, the number and size of metastatic lesions in the liver were determined. |
Dosage form | 1, 5mg/kg/day; 4 weeks; p.o. |
Applications | Mice treated with 1mg/kg/day of T0070907 orally had half the number of metastatic foci, and the average tumor volume was only 30% of that seen with control mice. A small increase in efficacy was seen when the dose of drug was increased to 5mg/kg/day. |
References: | |
| Cas No. | 313516-66-4 | SDF | |
| Chemical Name | 2-chloro-5-nitro-N-pyridin-4-ylbenzamide | ||
| Canonical SMILES | C1=CC(=C(C=C1[N+](=O)[O-])C(=O)NC2=CC=NC=C2)Cl | ||
| Formula | C12H8ClN3O3 | M.Wt | 277.66 |
| Solubility | ≥ 27.8 mg/mL in DMSO, ≥ 4.77 mg/mL in EtOH with ultrasonic and warming | 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 | 3.6015 mL | 18.0076 mL | 36.0153 mL |
| 5 mM | 720.3 μL | 3.6015 mL | 7.2031 mL |
| 10 mM | 360.2 μL | 1.8008 mL | 3.6015 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 saline, 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% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)