2. Cell Cycle/DNA Damage Apoptosis
  3. DNA Alkylator/Crosslinker Apoptosis
  4. (-)-Irofulven

(-)-Irofulven  (Synonyms: MGI 114; 6-Hydroxymethylacylfulvene; NSC 683863)

Cat. No.: HY-14429 Purity: 98.86%
COA Handling Instructions

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(-)-Irofulven (MGI 114), an Illudin S analog, is a DNA alkylating agent. (-)-Irofulven inhibits the replication of DNA, induces tumor cells apoptosis, and has potent antitumor activity.

For research use only. We do not sell to patients.

(-)-Irofulven Chemical Structure

(-)-Irofulven Chemical Structure

CAS No. : 158440-71-2

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1 mg USD 880 In-stock
5 mg USD 2200 In-stock
10 mg USD 3300 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

(-)-Irofulven Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

(-)-Irofulven (MGI 114), an Illudin S analog, is a DNA alkylating agent. (-)-Irofulven inhibits the replication of DNA, induces tumor cells apoptosis, and has potent antitumor activity[1][2].

In Vitro

(-)-Irofulven (2.8 μM; 1 hour) induces p53-dependent cell cycle arrest[1].
(-)-Irofulven (0.8 μM, 0.9 μM and 2.8 μM; 1 hour) induces CHK2 activation is related to p53 status in cells[1].
(-)-Irofulven inhibits DNA replication and induces chromosome aberrations (breaks and radials)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

(-)-Irofulven Related Antibodies

Cell Cycle Analysis[1]

Cell Line: A2780, CAOV3 and HCT116 cells
Concentration: 2.8 μM
Incubation Time: 1 hour
Result: p53 wild-type cells mainly arrested at G1/S phases, while p53-mutated or p53-null cells arrested at S and G2/M phases.

Western Blot Analysis[1]

Cell Line: A2780, CAOV3 and HCT116 cells
Concentration: 0.8 μM, 0.9 μM and 2.8 μM
Incubation Time: 1 hour
Result: Induced the Thr 68 phosphorylation of CHK2 kinase in cells.
In Vivo

(-)-Irofulven (7 mg/kg; i.p; on days 1-5 and 8-12) produces a statistically significant increase in the median survival of mice bearing tumor cells[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male and female athymic BALB/c mice (nu/nu genotype, 6 weeks old or older) injected with human glioblastoma multiforme[2].
Dosage: 7 mg/kg
Administration: i.p; on days 1-5 and 8-12
Result: Was active against all tumor lines.
Molecular Weight

246.30

Formula

C15H18O3
CAS No.
Appearance

Solid

Color

Yellow to orange

SMILES

CC(C1(CC1)[C@@](O)(C2=O)C)=C3C2=CC(C)=C3CO
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (203.00 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 4.0601 mL 20.3004 mL 40.6009 mL
5 mM 0.8120 mL 4.0601 mL 8.1202 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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 (10.15 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (10.15 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
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.
Purity & Documentation

Purity: 98.86%

COA (254 KB) HNMR (240 KB) LCMS (256 KB)

Handling Instructions (2659 KB)
References

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 4.0601 mL 20.3004 mL 40.6009 mL 101.5022 mL
5 mM 0.8120 mL 4.0601 mL 8.1202 mL 20.3004 mL
10 mM 0.4060 mL 2.0300 mL 4.0601 mL 10.1502 mL
15 mM 0.2707 mL 1.3534 mL 2.7067 mL 6.7668 mL
20 mM 0.2030 mL 1.0150 mL 2.0300 mL 5.0751 mL
25 mM 0.1624 mL 0.8120 mL 1.6240 mL 4.0601 mL
30 mM 0.1353 mL 0.6767 mL 1.3534 mL 3.3834 mL
40 mM 0.1015 mL 0.5075 mL 1.0150 mL 2.5376 mL
50 mM 0.0812 mL 0.4060 mL 0.8120 mL 2.0300 mL
60 mM 0.0677 mL 0.3383 mL 0.6767 mL 1.6917 mL
80 mM 0.0508 mL 0.2538 mL 0.5075 mL 1.2688 mL
100 mM 0.0406 mL 0.2030 mL 0.4060 mL 1.0150 mL
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(-)-Irofulven Related Classifications

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:

(-)-Irofulven158440-71-2MGI 114 6-Hydroxymethylacylfulvene NSC 683863MGI114MGI-114NSC683863NSC 683863NSC-683863DNA Alkylator/CrosslinkerApoptosisDNAAlkylatingIlludin-Santitumorp53CHK2Inhibitorinhibitorinhibit

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