Cat. No.: HY-19763

Ifupinostat

(Synonyms: BEBT-908)

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Based on 1 Customer Validation

Ifupinostat (BEBT-908) is a blood-brain barrier-permeable PI3K/HDAC inhibitor. Ifupinostat exerts anticancer activity against hematologic malignancies, lung cancer, colon cancer, brain cancer and other cancers. Ifupinostat inhibits the PI3K/AKT/mTOR signaling pathway, suppresses c-Myc expression and induces ferroptosis. Ifupinostat can be used in tumor research.

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

Purity: 99.30%
CAS No.: 1235449-52-1
Formula: C₂₃H₂₅N₉O₃S
Molecular Weight:507.57

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Ifupinostat Chemical Structure

CAS No.: 1235449-52-1

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
- Clinical Trial
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target

IC50: <0.1 μM (PI3Kα)^[1]

All PI3K Isoforms :

All Akt Isoforms :

All Histone Acetyltransferase Isoforms :

All mTOR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
Calu-6	IC₅₀	0.3 nM Compound: 31; BEBT-908	Cytotoxicity against human Calu-6 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent viability assay Cytotoxicity against human Calu-6 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent viability assay	[PMID: 37875056]
COLO 205	IC₅₀	0.3 nM Compound: 31; BEBT-908	Cytotoxicity against human COLO 205 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent viability assay Cytotoxicity against human COLO 205 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent viability assay	[PMID: 37875056]
Daudi	IC₅₀	0.3 nM Compound: 31; BEBT-908	Cytotoxicity against human Daudi cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent viability assay Cytotoxicity against human Daudi cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent viability assay	[PMID: 37875056]
HCT-116	IC₅₀	0.3 nM Compound: 31; BEBT-908	Cytotoxicity against human HCT-116 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent viability assay Cytotoxicity against human HCT-116 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent viability assay	[PMID: 37875056]
K562	IC₅₀	0.3 nM Compound: 31; BEBT-908	Cytotoxicity against human K562 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent viability assay Cytotoxicity against human K562 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent viability assay	[PMID: 37875056]
LoVo	IC₅₀	0.3 nM Compound: 31; BEBT-908	Cytotoxicity against human LoVo cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent viability assay Cytotoxicity against human LoVo cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent viability assay	[PMID: 37875056]
MC-38	IC₅₀	0.3 nM Compound: 31; BEBT-908	Cytotoxicity against mouse MC38 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent viability assay Cytotoxicity against mouse MC38 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent viability assay	[PMID: 37875056]
NCI-H1975	IC₅₀	0.3 nM Compound: 31; BEBT-908	Cytotoxicity against human NCI-H1975 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent viability assay Cytotoxicity against human NCI-H1975 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent viability assay	[PMID: 37875056]
NCI-H2122	IC₅₀	0.3 nM Compound: 31; BEBT-908	Cytotoxicity against human NCI-H2122 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent viability assay Cytotoxicity against human NCI-H2122 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent viability assay	[PMID: 37875056]
NCI-H358	IC₅₀	0.3 nM Compound: 31; BEBT-908	Cytotoxicity against human NCI-H358 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent viability assay Cytotoxicity against human NCI-H358 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent viability assay	[PMID: 37875056]
NCI-H460	IC₅₀	0.3 nM Compound: 31; BEBT-908	Cytotoxicity against human NCI-H460 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent viability assay Cytotoxicity against human NCI-H460 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent viability assay	[PMID: 37875056]
PC-9	IC₅₀	0.3 nM Compound: 31; BEBT-908	Cytotoxicity against human PC-9 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent viability assay Cytotoxicity against human PC-9 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent viability assay	[PMID: 37875056]
Ramos	IC₅₀	0.3 nM Compound: 31; BEBT-908	Cytotoxicity against human Ramos cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent viability assay Cytotoxicity against human Ramos cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent viability assay	[PMID: 37875056]
SW480	IC₅₀	0.3 nM Compound: 31; BEBT-908	Cytotoxicity against human SW480 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent viability assay Cytotoxicity against human SW480 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent viability assay	[PMID: 37875056]
SW-620	IC₅₀	0.3 nM Compound: 31; BEBT-908	Cytotoxicity against human SW620 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent viability assay Cytotoxicity against human SW620 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent viability assay	[PMID: 37875056]
THP-1	IC₅₀	0.3 nM Compound: 31; BEBT-908	Cytotoxicity against human THP-1 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent viability assay Cytotoxicity against human THP-1 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent viability assay	[PMID: 37875056]
TMD8	IC₅₀	0.3 nM Compound: 31; BEBT-908	Cytotoxicity against human TMD8 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent viability assay Cytotoxicity against human TMD8 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent viability assay	[PMID: 37875056]
U-937	IC₅₀	0.3 nM Compound: 31; BEBT-908	Cytotoxicity against human U-937 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent viability assay Cytotoxicity against human U-937 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent viability assay	[PMID: 37875056]

In Vitro

Ifupinostat (72 h) potently inhibits the viability of multiple hematological malignancy cell lines, with IC₅₀ values ranging from 0.7 to 30 nM after 72 h of treatment^[1].
Ifupinostat (8 nM; 24 h) inhibits PI3K/AKT/mTOR signaling, downregulates c-Myc and ferroptosis-related regulatory proteins in A20 and Daudi cells^[1].
Ifupinostat (8 nM; 48 h) induces accumulation of lipid ROS in A20 cells^[1].
Ifupinostat (8 nM; 48 h) reduces the GSH/GSSG ratio in A20 cells, promoting ferroptosis^[1].

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

Cell Viability Assay^[1]

Cell Line:

Human acute lymphoblastic leukemia (ALL) MOLT-4, acute myeloid leukemia (AML) HL-60, U937, THP-1, MV-4-11, non-Hodgkin lymphoma (NHL) Pfeiffer, Raji, TMD-8, Daudi, chronic myeloid leukemia (CML) K562, multiple myeloma RPMI-8226, OPM-2, ARH77, mouse leukemia L-1210, mouse lymphoma P388 D1, A20
Concentration:

/
Incubation Time:

72 h
Result:

Inhibited viability of multiple hematological malignancy cell lines with IC₅₀ values ranging from 0.7 to 30 nM.
Achieved an IC₅₀ of 0.002 μM in MOLT-4 cells.
Achieved an IC₅₀ of 0.003 μM in HL-60 cells, 0.001 μM in U937 cells, 0.013 μM in THP-1 cells and 0.0007 μM in MV-4-11 cells.
Achieved an IC₅₀ of 0.008 μM in Pfeiffer cells, 0.03 μM in Raji cells, 0.001 μM in TMD-8 cells and 0.002 μM in Daudi cells.
Achieved an IC₅₀ of 0.03 μM in K562 cells.
Achieved an IC₅₀ of 0.002 μM in RPMI-8226 cells, 0.001 μM in OPM-2 cells and 0.007 μM in ARH77 cells.
Achieved an IC₅₀ of 0.007 μM in L-1210 cells.
Achieved an IC₅₀ of 0.009 μM in P388 D1 cells.
Achieved an IC₅₀ of 0.002 μM in A20 cells.

Western Blot Analysis^[1]

Cell Line:

A20 mouse lymphoma cells, Daudi human Burkitt lymphoma cells
Concentration:

8 nM
Incubation Time:

24 h
Result:

Significantly reduced c-Myc, SLC7A11, GPX4, and Nrf2 protein levels.
Inhibited AKT, S6K1, and eIF4B phosphorylation.

Parmacokinetics

Species	Dose	Route	Note	T_1/2	T_max	C_max	AUC_0-t	AUC_0-∞	MRT_0-inf	AUC_0-inf
Mice^[1]	100 mg/kg	i.v.	Brain tissue	10.66 h	0.25 h	305.52 ng/g	691.98 ng/g·h	887.75 ng/g·h	13.55 h	/
Mice^[1]	100 mg/kg	i.v.	Brain tumor	15.91 h	0.25 h	574.2 ng/g	1214.54 ng/g·h	/	18 h	1711.25 ng/g·h

In Vivo

Ifupinostat (100 mg/kg; intravenous injection; once every other day; 9 doses total) significantly inhibits the growth of various hematologic malignancy xenografts^[1].
Ifupinostat (25-100 mg/kg; intravenous injection; single dose) potently induces acetylation of histone H3 and inhibits phosphorylation of AKT in Daudi xenograft tumors^[1].
Ifupinostat (100 mg/kg; i.v.; administered every other day; 4 doses) induces tumor regression and significantly prolongs the survival of mice in an orthotopic brain lymphoma mouse model^[1].

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

Animal Model:

SCID (6-8-week-old female)^[1]
Dosage:

100 mg/kg
Administration:

i.v.; every other day; 3 weeks (9 doses total)
Result:

Significantly inhibited growth of all four xenograft tumor types.
Achieved treatment/control (T/C) values of 29.5% for OPM2 xenografts on day 14, -28.9% for Molt-4 xenografts on day 10, -25% for MV-4-11 xenografts on day 17, and -37.42% for Daudi xenografts on day 14.
Caused no significant body weight loss in treated mice.

Animal Model:

SCID (6-8-week-old female)^[1]
Dosage:

25 mg/kg; 100 mg/kg
Administration:

i.v.; single dose
Result:

Induced significant histone H3 acetylation (Ach3) in a time- and dose-dependent manner: 25 mg/kg induced strong Ach3 expression from 5 min to 6 h post-dosing, while 100 mg/kg induced strong Ach3 expression from 5 min to 24 h post-dosing.
Caused rapid, dose-dependent inhibition of AKT phosphorylation: 25 mg/kg inhibited pAKT from 5 min to 1 h post-dosing, while 100 mg/kg inhibited pAKT from 5 min to 6 h post-dosing.

Clinical Trial

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

Chemical Information

CAS No. 1235449-52-1
Appearance Solid
Molecular Weight 507.57
Formula C₂₃H₂₅N₉O₃S
Color White to off-white
SMILES

CN(CC1=CC(N=C(C2=CN=C(NC)C=C2)N=C3N4CCOCC4)=C3S1)C5=NC=C(C(NO)=O)C=N5
Synonyms

BEBT-908
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : ≥ 37 mg/mL (72.90 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

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

1.9702 mL

9.8509 mL

19.7017 mL

5 mM

0.3940 mL

1.9702 mL

3.9403 mL

10 mM

0.1970 mL

0.9851 mL

1.9702 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

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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: 5% DMSO 95% (20% SBE-β-CD in Saline)

Solubility: 5 mg/mL (9.85 mM); Suspended solution; Need ultrasonic

Protocol 2

Add each solvent one by one: 5% DMSO 95% Corn Oil

Solubility: 5 mg/mL (9.85 mM); Suspended solution; Need ultrasonic

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

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: 50% PEG300 50% Saline

Solubility: 2.5 mg/mL (4.93 mM); Suspended solution; Need ultrasonic

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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)
Handling Instructions (2659 KB)

References

[1]. Wang N, et al. Dual PI3K/HDAC Inhibitor BEBT-908 Exhibits Potent Efficacy as Monotherapy for Primary Central Nervous System Lymphoma. Target Oncol. 2023;18(6):941-952. [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

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9702 mL	9.8509 mL	19.7017 mL	49.2543 mL
	5 mM	0.3940 mL	1.9702 mL	3.9403 mL	9.8509 mL
	10 mM	0.1970 mL	0.9851 mL	1.9702 mL	4.9254 mL
	15 mM	0.1313 mL	0.6567 mL	1.3134 mL	3.2836 mL
	20 mM	0.0985 mL	0.4925 mL	0.9851 mL	2.4627 mL
	25 mM	0.0788 mL	0.3940 mL	0.7881 mL	1.9702 mL
	30 mM	0.0657 mL	0.3284 mL	0.6567 mL	1.6418 mL
	40 mM	0.0493 mL	0.2463 mL	0.4925 mL	1.2314 mL
	50 mM	0.0394 mL	0.1970 mL	0.3940 mL	0.9851 mL
	60 mM	0.0328 mL	0.1642 mL	0.3284 mL	0.8209 mL

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Ifupinostat

Apoptosis Compound Library

Epigenetics Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Metabolism/Protease Compound Library

NF-κB Signaling Compound Library

PI3K/Akt/mTOR Compound Library

Stem Cell Signaling Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

CNS-Penetrant Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Antioxidant Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Ferroptosis Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Glutamine Metabolism Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Transcription Factor-Targeted Library

Glucose Metabolism Compound Library

Targeted Diversity Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Pain-Related Compound Library

Mitochondrial Protection Compound Library

Membrane Protein-targeted Compound Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

Lactic Acid Metabolic Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Lactylation Compound Library

All PI3K Isoforms

All Akt Isoforms

All Histone Acetyltransferase Isoforms

All mTOR Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Ifupinostat Related Classifications

Cat. No.: HY-19763