T0070907
目录号 : GC12820
T0070907是一种有效的选择性过氧化物酶体增殖物激活受体γ（PPARγ）拮抗剂，IC50值为1nM。
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.
T0070907是一种有效的选择性过氧化物酶体增殖物激活受体γ（PPARγ）拮抗剂，IC50值为1nM[1]。T0070907是一种抗微管药物，能够降低结肠癌细胞中的α和β微管蛋白[2]。T0070907能够抑制脂肪生成，诱导未成熟脂肪细胞快速凋[3]。
在体外，T0070907（0.1-20μM）处理乳腺癌MB-231细胞48h，以剂量依赖性方式抑制了细胞迁移和侵袭[4]。T0070907（50μM）处理肝癌HepG2和Hep3B细胞48h，阻止了细胞与细胞外基质（ECM）蛋白的再附着，诱导了细胞的失巢凋亡[5]。
在体内，T0070907（1, 5mg/kg/day）通过口服治疗HT-29细胞异种移植小鼠4周，显著减少了小鼠体内肝脏肿瘤转移灶的数量，减小了肿瘤组织的大小[6]。
| 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 | |
| 化学名 | 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 | ||
| 分子式 | C12H8ClN3O3 | 分子量 | 277.66 |
| 溶解度 | ≥ 27.8 mg/mL in DMSO, ≥ 4.77 mg/mL in EtOH with ultrasonic and warming | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.6015 mL | 18.0076 mL | 36.0153 mL |
| 5 mM | 0.7203 mL | 3.6015 mL | 7.2031 mL |
| 10 mM | 0.3602 mL | 1.8008 mL | 3.6015 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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