2. Cell Cycle/DNA Damage Epigenetics PI3K/Akt/mTOR Apoptosis
  3. HDAC Akt Apoptosis
  4. Imofinostat

Imofinostat  (Synonyms: ABT-301; MPT0E028; TMU-C-0012)

Cat. No.: HY-124295 Purity: 99.40%
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Imofinostat (ABT-301; MPT0E028) is an orally active and selective HDAC inhibitor with IC50s of 53.0 nM, 106.2 nM, 29.5 nM for HDAC1, HDAC2 and HDAC6, respectively. Imofinostat has a weak inhibitory effect on HDAC8 (IC50 of 2.5 ​​μM), but no inhibitory effect on HDAC4 (IC50>10 μM). Imofinostat reduces the viability of B-cell lymphomas by inducing apoptosis and possesses potent direct Akt targeting ability and reduces Akt phosphorylation in B-cell lymphoma. Imofinostat has a broad-spectrum antitumor activity, including colorectal cancer, B-cell lymphoma, non-small cell lung carcinoma (NSCLC), and pancreatic cancer, while also showing therapeutic potential in non-tumor diseases like emphysema and pulmonary fibrosis.

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

Imofinostat Chemical Structure

Imofinostat Chemical Structure

CAS No. : 1338320-94-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

Imofinostat Related Antibodies

Top Publications Citing Use of Products

View All HDAC Isoform Specific Products:

View All Isoforms
HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

View All Akt Isoform Specific Products:

View All Isoforms
Akt Akt1 Akt2 Akt3

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Imofinostat (ABT-301; MPT0E028) is an orally active and selective HDAC inhibitor with IC50s of 53.0 nM, 106.2 nM, 29.5 nM for HDAC1, HDAC2 and HDAC6, respectively. Imofinostat has a weak inhibitory effect on HDAC8 (IC50 of 2.5 ​​μM), but no inhibitory effect on HDAC4 (IC50>10 μM). Imofinostat reduces the viability of B-cell lymphomas by inducing apoptosis and possesses potent direct Akt targeting ability and reduces Akt phosphorylation in B-cell lymphoma. Imofinostat has a broad-spectrum antitumor activity, including colorectal cancer, B-cell lymphoma, non-small cell lung carcinoma (NSCLC), and pancreatic cancer, while also showing therapeutic potential in non-tumor diseases like emphysema and pulmonary fibrosis[1][2][3][14][5][6].

IC50 & Target[1,2]

HDAC1

53.0 nM (IC50)

HDAC2

106.2 nM (IC50)

HDAC6

29.5 nM (IC50)

HDAC8

2532.6 nM (IC50)

In Vitro

Imofinostat (MPT0E028) (0-10 μM; 48 h) significantly inhibits cell proliferation and induces apoptosis in HCT116 cells[1].
Imofinostat (0-10 μM; 24 h) inhibits cell growth in a concentration-dependent manner. Imofinostat increases the number of cells in the sub-G1 phase of the cell cycle. Imofinostat induces caspase 3 and PARP activation in a concentrationdependent manner, and this apoptosis[1].
Imofinostat (0.3-100 μM; 24 h) induces significant concentration-dependent growth inhibition in Ramos and BJAB cells. Imofinostat increases the subG1 phase population in a time- and concentration-dependent manner. Imofinostat induces caspase-3, -6, -7, -8, -9 activation and PARP cleavage[2].
Imofinostat (0.01-1 μM) pretreated human lung fibroblasts (WI-38) for 30 minutes and then treated with stimulants, which inhibits the expression of CTGF induced by TGF-β, thrombin, and ET-1[5].

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

Imofinostat Related Antibodies

Cell Viability Assay[1]

Cell Line: HCT116 cells
Concentration: 0-10 μM
Incubation Time: 48 h
Result: Inhibited cell growth in a concentration-dependent manner.

Cell Cycle Analysis[1]

Cell Line: HCT116 cells
Concentration: 0.3 μM, 1 μM, 3 μM, 10 μM
Incubation Time: 24 h
Result: Increased the number of cells in the sub-G1 phase of the cell cycle.

Western Blot Analysis[1]

Cell Line: HCT116 cells
Concentration: 1 μM, 3 μM, 10 μM
Incubation Time: 24 h
Result: Induced caspase 3 and PARP activation in a concentration-dependent manner.
Induced hyperacetylation of α-tubulin and histone H3.
In Vivo

Imofinostat (MPT0E028) (50-200 mg/kg; oral gavage; once a day for 15 days) delays and inhibits tumor growth in a dose-dependent manner in nude mice xenografted with human colorectal cancer HCT116 cells, with complete tumor regression observed in 3 mice at 200 mg/kg, without significant body weight changes or other adverse effects[1].
Imofinostat (100 mg/kg; oral gavage; once daily;) significantly prolongs survival in NOD/SCID mice bearing human B-cell lymphoma Ramos cells[2].
Imofinostat (50-200 mg/kg; oral gavage; once daily; 31 days) inhibits tumor growth in a dose-dependent manner, activates caspase 3 and PARP, and increases acetylation levels of histone H3 and α-tubulin in nude mice xenografted with BJAB cells, without significant body weight changes[2].
Imofinostat (25-100 mg/kg; oral gavage; once daily; 20 days) reduces pulmonary fibrosis in a dose-dependent manner, decreases expression of CTGF, fibronectin, α-SMA, and collagen, and inhibits phosphorylation of ERK, JNK, and p38 in Bleomycin (HY-17565A)-induced C57BL/6 mouse model[5].
Imofinostat (25 mg/kg; oral gavage; once daily; continuous administration) significantly reduces tumor volume, increases cleaved caspase-3 levels, downregulates EGFR expression, and causes no weight loss or adverse effects in AsPC-1 pancreatic cancer xenograft nude mice[6].

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

Animal Model: Nude mice (female, 17.2-22.0 g, 8 weeks old) subcutaneously injected with HCT116 cells in the right flank[1].
Dosage: 50, 100, or 200 mg/kg
Administration: Oral gavage; once a day; for 15 days
Result: Tumor growth was significantly delayed and inhibited in a dose-dependent manner.
No significant body weight changes or adverse effects were observed in treatment groups.
Animal Model: NOD/SCID mice (male, 5 weeks old) engrafted with Ramos cells via tail vein injection[2].
Dosage: 100 mg/kg
Administration: Oral gavage, daily until study end.
Result: Prolonged survival compared to the control group.
Animal Model: Nude mice (male, 20-24 g, 5 weeks old) subcutaneously injected with BJAB cells mixed with Matrigel[2].
Dosage: 50, 100, or 200 mg/kg
Administration: Oral gavage, daily for 31 days.
Result: Tumor growth was inhibited in a dose-dependent manner. Caspase 3 and PARP were activated, and acetylation of histone H3 and α-tubulin was increased in treated groups. Akt phosphorylation was inhibited, and no significant body weight changes were observed.
Animal Model: C57BL/6 mice (female, 8 weeks old) intratracheally administered bleomycin (0.3 U/kg) to induce pulmonary fibrosis[5].
Dosage: 25, 50, or 100 mg/kg
Administration: Oral gavage, daily from day 1 to day 20.
Result: Reduced fibrosis score, decreased expression of CTGF, fibronectin, α-SMA, and collagen, and inhibited phosphorylation of ERK, JNK, and p38 in a dose-dependent manner.
Animal Model: Balb/c-nude mice (male, 4 weeks old) subcutaneously injected with AsPC-1 cells[6].
Dosage: 25 mg/kg
Administration: Oral gavage, daily, for 25 days
Result: Tumor volume was significantly reduced. Cleaved caspase-3 levels were increased, and EGFR expression was downregulated in tumor tissues. No weight loss or adverse effects were observed.
Clinical Trial
Molecular Weight

344.38

Formula

C17H16N2O4S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(/C=C/C1=CC2=C(C=C1)N(CC2)S(=O)(C3=CC=CC=C3)=O)NO
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (290.38 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 2.9038 mL 14.5188 mL 29.0377 mL
5 mM 0.5808 mL 2.9038 mL 5.8075 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 (sealed storage, away from moisture and light). 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
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Concentration
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Volume
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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 (7.26 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 (7.26 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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

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
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 (sealed storage, away from moisture and light). 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 2.9038 mL 14.5188 mL 29.0377 mL 72.5942 mL
5 mM 0.5808 mL 2.9038 mL 5.8075 mL 14.5188 mL
10 mM 0.2904 mL 1.4519 mL 2.9038 mL 7.2594 mL
15 mM 0.1936 mL 0.9679 mL 1.9358 mL 4.8396 mL
20 mM 0.1452 mL 0.7259 mL 1.4519 mL 3.6297 mL
25 mM 0.1162 mL 0.5808 mL 1.1615 mL 2.9038 mL
30 mM 0.0968 mL 0.4840 mL 0.9679 mL 2.4198 mL
40 mM 0.0726 mL 0.3630 mL 0.7259 mL 1.8149 mL
50 mM 0.0581 mL 0.2904 mL 0.5808 mL 1.4519 mL
60 mM 0.0484 mL 0.2420 mL 0.4840 mL 1.2099 mL
80 mM 0.0363 mL 0.1815 mL 0.3630 mL 0.9074 mL
100 mM 0.0290 mL 0.1452 mL 0.2904 mL 0.7259 mL
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Imofinostat 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:

Imofinostat1338320-94-7ABT-301 MPT0E028 TMU-C-0012ABT301ABT 301HDACAktApoptosisHistone deacetylasesPKBProtein kinase BHDAC1HDAC2HDAC6colorectal cancerB-cell lymphomanon-small cell lung carcinoma (NSCLC)Inhibitorinhibitorinhibit

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