Ifupinostat (Synonyms: BEBT-908)

Name: Ifupinostat
Brand: MedChemExpress
SKU: HY-19763
Rating: 4.5 (0 reviews)

Cat. No.: HY-19763 Purity: 99.30%: Data Sheet
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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.

Ifupinostat Chemical Structure

CAS No. : 1235449-52-1

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

IC50: <0.1 μM (PI3Kα)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
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]
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]
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]
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]
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]
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

Molecular Weight

507.57

Formula

C₂₃H₂₅N₉O₃S

CAS No.

1235449-52-1

Appearance

Solid

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

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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, 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
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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: 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

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

mg/kg

Animal weight
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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: 99.30%

Select Batch:

Data Sheet (278 KB) SDS (254 KB)

COA (247 KB) HNMR (279 KB) RP-HPLC (225 KB) MS (70 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]

Complete Stock Solution Preparation Table

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

Ifupinostat Related Classifications

Help & FAQs

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Ifupinostat (Synonyms: BEBT-908)

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Ifupinostat (Synonyms: BEBT-908)

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Purity & Documentation

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Ifupinostat Related Antibodies

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Complete Stock Solution Preparation Table

Ifupinostat Related Classifications

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