Ran-IN-1
Based on 1 Customer Validation
Ran-IN-1 is a specific inhibitor of Ran GTPase. Ran-IN-1 selectively induces cytotoxicity and apoptosis in aneuploid ovarian cancer cells and also inhibits DNA repair. Ran-IN-1 exhibits antitumor activity and is useful for research on tumors such as epithelial ovarian cancer.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.89%
- CAS 番号: 2301869-11-2
- 分子式: C27H26F3NO4S
- 分子量:517.56
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
体外実験
Ran-IN-1 (Compound M36) (50-200 μM; 1 h) reduces Ran-GTP levels in TOV112D cells in a dose-dependent manner and increases Ran's thermal stability at a specific temperature[1].
Ran-IN-1 (0-40 μM) inhibits colony formation in TOV112D cells (IC50 = 10.02 ± 0.36 μM)[1].
Ran-IN-1 (40 μM; 96 h) suppresses the survival of aneuploid epithelial ovarian cancer (EOC) cells, such as TOV112D, TOV1949, and OV1946[1].
Ran-IN-1 (40 µM; 6 days) induces apoptosis in TOV112D cells, with no notable effect in ARPE cells[1].
Ran-IN-1 (20-50 μM) induces NR1D1 expression in aneuploid EOC cells (TOV112D and OV1946), increases levels of DNA damage markers, and suppresses the DDR pathway[1].
Ran-IN-1 (20 µM; 72 h) induces accumulation of DNA damage in TOV112D cells (increased p-γH2AX foci) and suppresses both homologous recombination (reduced Rad51 foci) and non-homologous end joining (reduced 53BP1 foci) pathways[1].
Ran-IN-1 (10-20 μM; 0-6 days) inhibits the homologous recombination pathway in epithelial ovarian cancer cell lines and exhibits synergistic effects with Olaparib (HY-10162)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:TOV112D cells
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Concentration:50, 100 and 150 μM
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Incubation Time:1 h
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Result:Reduced Ran-GTP levels in TOV112D cells in a dose-dependent manner.
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Cell Line:TOV112D cells and ARPE cells
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Concentration:40 µM
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Incubation Time:6 days
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Result:Increased the levels of cleaved PARP in TOV112D cells.
Did not affect the levels of cleaved PARP in ARPE cells.
体内実験
Ran-IN-1 (200 mg/kg; intraperitoneal injection; single dose) achieves a plasma peak concentration of 100 µM at 30 minutes, remains at approximately 10 µM after 6 hours, and is still detectable after 24 hours in 6-week-old female CD1 mice, demonstrating acceptable pharmacokinetic properties[1].
Compound M36 (200 mg/kg; intraperitoneal injection; daily except weekends; 3 weeks) is well tolerated in 6-week-old female NRG mice, with no adverse effects on body weight gain[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NRG mice (6-week-old)[1]
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Dosage:200 mg/kg
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Administration:i.p.; daily; 32 days
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Result:Significantly delayed tumor growth of this aggressive model and prolonged mouse survival.
化学情報
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CAS 番号 2301869-11-2
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性状 Solid
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分子量 517.56
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分子式 C27H26F3NO4S
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Color White to off-white
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SMILES
FC1=CC=C(COC[C@@H]2[C@@H](OCC3=CC=C(F)C=C3)[C@@H](OCC4=CC=C(F)C=C4)[C@H](C(N)=S)O2)C=C1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
体外:
DMSO : 100 mg/mL (193.21 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.83 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
プロトコル
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Mammalian live/dead viability and cytotoxicity staining
Live/dead viability and cytotoxicity staining assays are based on the simultaneous detection of intracellular esterase activity in metabolically active (viable) cells and membrane integrity loss in non-viable cells. In commonly used dual-staining approaches, membrane-permeant fluorogenic substrates are converted by intracellular esterases into fluorescent products in live cells, while impermeant DNA-binding dyes selectively enter cells with compromised plasma membranes and label nucleic acids in dead or dying cells, enabling discrimination between viable and non-viable populations by fluorescence microscopy or flow cytometry.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
純度とドキュメンテーション
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データシート (282 KB)
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SDS (254 KB)
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.9321 mL | 9.6607 mL | 19.3214 mL | 48.3036 mL |
| 5 mM | 0.3864 mL | 1.9321 mL | 3.8643 mL | 9.6607 mL | |
| 10 mM | 0.1932 mL | 0.9661 mL | 1.9321 mL | 4.8304 mL | |
| 15 mM | 0.1288 mL | 0.6440 mL | 1.2881 mL | 3.2202 mL | |
| 20 mM | 0.0966 mL | 0.4830 mL | 0.9661 mL | 2.4152 mL | |
| 25 mM | 0.0773 mL | 0.3864 mL | 0.7729 mL | 1.9321 mL | |
| 30 mM | 0.0644 mL | 0.3220 mL | 0.6440 mL | 1.6101 mL | |
| 40 mM | 0.0483 mL | 0.2415 mL | 0.4830 mL | 1.2076 mL | |
| 50 mM | 0.0386 mL | 0.1932 mL | 0.3864 mL | 0.9661 mL | |
| 60 mM | 0.0322 mL | 0.1610 mL | 0.3220 mL | 0.8051 mL | |
| 80 mM | 0.0242 mL | 0.1208 mL | 0.2415 mL | 0.6038 mL | |
| 100 mM | 0.0193 mL | 0.0966 mL | 0.1932 mL | 0.4830 mL |
Ran-IN-1 関連分類
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