Cat. No.: HY-124295

Imofinostat

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

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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.

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Pureté: 99.40%
CAS No.: 1338320-94-7
Formule: C₁₇H₁₆N₂O₄S
Masse moléculaire:344.38

Stockage:

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)

Imofinostat Chemical Structure

CAS No.: 1338320-94-7

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1,2]

HDAC1

53.0 nM (IC₅₀)

HDAC2

106.2 nM (IC₅₀)

HDAC6

29.5 nM (IC₅₀)

HDAC8

2532.6 nM (IC₅₀)

Voir tous les produits spécifiques à Isoform HDAC :

Voir tous les produits spécifiques à Isoform Akt :

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.

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.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1338320-94-7
Appearance Solid
Masse moléculaire 344.38
Formule C₁₇H₁₆N₂O₄S
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
Synonyms

ABT-301; MPT0E028; TMU-C-0012
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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)

Solvant et solubilité

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.9038 mL

14.5188 mL

29.0377 mL

5 mM

0.5808 mL

2.9038 mL

5.8075 mL

10 mM

0.2904 mL

1.4519 mL

2.9038 mL

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (7.26 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:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (287 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Huang HL, et al. Anticancer activity of MPT0E028, a novel potent histone deacetylase inhibitor, in human colorectal cancer HCT116 cells in vitro and in vivo. PLoS One. 2012;7(8):e43645. [Content Brief]

[2]. Huang HL, et al. Novel oral histone deacetylase inhibitor, MPT0E028, displays potent growth-inhibitory activity against human B-cell lymphoma in vitro and in vivo. Oncotarget. 2015 Mar 10;6(7):4976-91. [Content Brief]

[3]. Chen MC, et al. The HDAC inhibitor, MPT0E028, enhances erlotinib-induced cell death in EGFR-TKI-resistant NSCLC cells. Cell Death Dis. 2013 Sep 19;4(9):e810. doi: 10.1038/cddis.2013.330. Erratum in: Cell Death Dis. 2024 Jul 9;15(7):490. [Content Brief]

[4]. Yeh LY, et al. A Potent Histone Deacetylase Inhibitor MPT0E028 Mitigates Emphysema Severity via Components of the Hippo Signaling Pathway in an Emphysematous Mouse Model. Front Med (Lausanne). 2022 May 18;9:794025. [Content Brief]

[5]. Liu CH, et al. MPT0E028, a novel pan-HDAC inhibitor, prevents pulmonary fibrosis through inhibition of TGF-β-induced CTGF expression in human lung fibroblasts: Involvement of MKP-1 activation. Eur J Pharmacol. 2024 Aug 15;977:176711. [Content Brief]

[6]. Chao MW, et al. Combination treatment strategy for pancreatic cancer involving the novel HDAC inhibitor MPT0E028 with a MEK inhibitor beyond K-Ras status. Clin Epigenetics. 2019 May 29;11(1):85. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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Voir tous les produits spécifiques à Isoform HDAC

Voir tous les produits spécifiques à Isoform Akt

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Imofinostat Related Classifications

HY-124295 Related Classifications