2. GPCR/G Protein Apoptosis
  3. Arf Family GTPase Apoptosis
  4. Ran-IN-1

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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Ran-IN-1

Ran-IN-1 構造式

CAS 番号 : 2301869-11-2

容量 価格（税別） 在庫状況 数量
5 mg $1200 在庫あり
10 mg $1800 在庫あり
25 mg $3245 在庫あり
50 mg $5192 在庫あり
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200 mg   お問い合わせ  

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Ran-IN-1 関連抗体

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製品説明

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[1].

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.

Ran-IN-1 関連抗体

Western Blot Analysis[1]

Cell Line: TOV112D cells
Concentration: 50, 100 and 150 μM
Incubation Time: 1 h
Result: Reduced Ran-GTP levels in TOV112D cells in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: TOV112D cells and ARPE cells
Concentration: 40 µM
Incubation Time: 6 days
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, 32 days) delays tumor growth and prolongs survival in a chemotherapy-resistant ovarian cancer xenograft model in 6-week-old NRG mice[1].
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.

Animal Model: NRG mice (6-week-old)[1]
Dosage: 200 mg/kg
Administration: i.p.; daily; 32 days
Result: Significantly delayed tumor growth of this aggressive model and prolonged mouse survival.
分子量

517.56

分子式

C27H26F3NO4S
CAS 番号
Appearance

Solid

Color

White to off-white

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
輸送条件

Room temperature in continental US; may vary elsewhere.
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9321 mL 9.6607 mL 19.3214 mL
5 mM 0.3864 mL 1.9321 mL 3.8643 mL
10 mM 0.1932 mL 0.9661 mL 1.9321 mL
View the 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.

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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.

  • Protocol 1

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.83 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
純度とドキュメンテーション
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
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
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Ran-IN-1 Related Classifications

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Ran-IN-12301869-11-2Arf Family GTPaseApoptosisADP-ribosylation Factor (ARF) Family GTPaseEOCnormal diploid cellsRan GTPaseaneuploid ovarian cancer cellsolaparibDNA repairTOV112DInhibitorinhibitorinhibit

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