Art. -Nr.: HY-13432

Nanatinostat

(Synonyms: CHR-3996)

4 Cited Publications

Kundenbewertung

Based on 4 publication(s) in Google Scholar

Nanatinostat (CHR-3996) is a potent, class I selective and orally active HDAC inhibitor with IC₅₀s of 3 nM, 4 nM, and 7 nM for HDAC1, HDAC2, and HDAC3, respectively. Nanatinostat has low activity against HDAC5 (IC₅₀ of 200 nM) and HDAC6 (IC₅₀ of 2100 nM). Nanatinostat induces apoptosis in myeloma cells. Nanatinostat has potent anticancer effects, such as myeloma, advanced solid tumours and colorectal cancer.

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Reinheit: 99.67%
CAS. Nr.: 1256448-47-1
Formel: C₂₀H₁₉FN₆O₂
Molecular Weight:394.40

Speicherung:

-20°C, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Nanatinostat Chemical Structure

CAS. Nr.: 1256448-47-1

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (4)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

HDAC1

3 nM (IC₅₀)

HDAC2

4 nM (IC₅₀)

HDAC3

7 nM (IC₅₀)

HDAC

8 nM (IC₅₀)

HDAC5

200 nM (IC₅₀)

HDAC6

2100 nM (IC₅₀)

Alle HDAC Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	GI₅₀	210 nM Compound: 21r, CHR-3996	Antiproliferative activity against human A2780 cells after 72 hrs by WST-1 assay Antiproliferative activity against human A2780 cells after 72 hrs by WST-1 assay	[PMID: 21080647]
A549	GI₅₀	250 nM Compound: 21r, CHR-3996	Antiproliferative activity against human A549 cells after 72 hrs by WST-1 assay Antiproliferative activity against human A549 cells after 72 hrs by WST-1 assay	[PMID: 21080647]
COR-L23	GI₅₀	105 nM Compound: 21r, CHR-3996	Antiproliferative activity against human COR-L23 cells after 72 hrs by WST-1 assay Antiproliferative activity against human COR-L23 cells after 72 hrs by WST-1 assay	[PMID: 21080647]
COR-L23	GI₅₀	560 nM Compound: 21r, CHR-3996	Antiproliferative activity against doxorubicin-resistant human COR-L23 cells after 72 hrs by WST-1 assay Antiproliferative activity against doxorubicin-resistant human COR-L23 cells after 72 hrs by WST-1 assay	[PMID: 21080647]
DU-145	GI₅₀	48 nM Compound: 21r, CHR-3996	Antiproliferative activity against human DU145 cells after 72 hrs by WST-1 assay Antiproliferative activity against human DU145 cells after 72 hrs by WST-1 assay	[PMID: 21080647]
HCT-116	GI₅₀	72 nM Compound: 21r, CHR-3996	Antiproliferative activity against human HCT116 cells after 72 hrs by WST-1 assay Antiproliferative activity against human HCT116 cells after 72 hrs by WST-1 assay	[PMID: 21080647]
HeLa	IC₅₀	8 nM Compound: 21r, CHR-3996	Inhibition of HDAC in human HeLa cells nuclear extract using fluor de Lys as substrate preincubated for 5 mins by fluorometric analysis Inhibition of HDAC in human HeLa cells nuclear extract using fluor de Lys as substrate preincubated for 5 mins by fluorometric analysis	[PMID: 21080647]
HepG2	GI₅₀	230 nM Compound: 21r, CHR-3996	Antiproliferative activity against human HepG2 cells after 72 hrs by WST-1 assay Antiproliferative activity against human HepG2 cells after 72 hrs by WST-1 assay	[PMID: 21080647]
HuT78	GI₅₀	31 nM Compound: 21r, CHR-3996	Antiproliferative activity against human HUT78 cells after 72 hrs by WST-1 assay Antiproliferative activity against human HUT78 cells after 72 hrs by WST-1 assay	[PMID: 21080647]
LoVo	GI₅₀	140 nM Compound: 21r, CHR-3996	Antiproliferative activity against human LoVo cells after 72 hrs by WST-1 assay Antiproliferative activity against human LoVo cells after 72 hrs by WST-1 assay	[PMID: 21080647]
MG-63	GI₅₀	750 nM Compound: 21r, CHR-3996	Antiproliferative activity against human MG63 cells after 72 hrs by WST-1 assay Antiproliferative activity against human MG63 cells after 72 hrs by WST-1 assay	[PMID: 21080647]
MIA PaCa-2	GI₅₀	280 nM Compound: 21r, CHR-3996	Antiproliferative activity against human MIAPaCa2 cells after 72 hrs by WST-1 assay Antiproliferative activity against human MIAPaCa2 cells after 72 hrs by WST-1 assay	[PMID: 21080647]
MOLT-4	GI₅₀	31 nM Compound: 21r, CHR-3996	Antiproliferative activity against human MOLT4 cells after 72 hrs by WST-1 assay Antiproliferative activity against human MOLT4 cells after 72 hrs by WST-1 assay	[PMID: 21080647]
PC-3	GI₅₀	160 nM Compound: 21r, CHR-3996	Antiproliferative activity against human PC3 cells after 72 hrs by WST-1 assay Antiproliferative activity against human PC3 cells after 72 hrs by WST-1 assay	[PMID: 21080647]
U-937	GI₅₀	52 nM Compound: 21r, CHR-3996	Antiproliferative activity against human U937 cells after 72 hrs by WST-1 assay Antiproliferative activity against human U937 cells after 72 hrs by WST-1 assay	[PMID: 21080647]

In Vitro

Nanatinostat (CHR-3996) (0.0001-1 μM; 48 hours) inhibits the proliferation of myeloma cell lines, with LC₅₀ values ranging from 30.3-97.6 nM in different cell lines^[2].
Nanatinostat (250-100 nM; 8-48 hours) induces apoptosis and increases the level of acetylated H3K9 in H929 and RPMI-8226 myeloma cell lines^[2].
Nanatinostat (0-200 nM; 24 hours) reduces the levels of IL-6 and VEGF secreted by bone marrow stromal cells in the co-culture system of bone marrow stromal cells and myeloma cells^[2].
Nanatinostat (250 nM and 100 nM; 48 hours) arrests the cell cycle at the G0/G1 phase in H929 and RPMI-8226 myeloma cell lines^[2].

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

Cell Viability Assay^[2]

Cell Line:

H929, RPMI-8226, KMS11, LP-1, MM1-S cells
Concentration:

0.0001 μM, 0.001 μM, 0.01 μM, 0.1 μM, 1 μM
Incubation Time:

48 hours
Result:

The cell viability decreased.

Apoptosis Analysis^[2]

Cell Line:

H929 and RPMI-8226 myeloma cell lines
Concentration:

100 nM (RPMI-8226 cells), 250 nM (H929 cells)
Incubation Time:

8 hours, 24 hours, 48 hours
Result:

The percentage of apoptotic cells increased, with an increase in both early and late apoptotic cells.

Cell Cycle Analysis^[2]

Cell Line:

H929 and RPMI-8226 myeloma cell lines
Concentration:

100 nM (RPMI-8226 cells), 250 nM (H929 cells)
Incubation Time:

48 hours
Result:

The cell cycle was arrested at the G0/G1 phase.

Western Blot Analysis^[2]

Cell Line:

H929 and RPMI-8226 myeloma cell lines
Concentration:

100 nM (RPMI-8226 cells), 250 nM (H929 cells)
Incubation Time:

8 hours, 24 hours, 48 hours
Result:

The pro-apoptotic DNase Endonuclease G and p53 downstream mediator Noxa were up-regulated, and caspase 9 was cleaved.

In Vivo

Nanatinostat (50 mg/kg; orally administered; once daily; for 14 days) can almost completely inhibit tumor growth in the female CrTac:NCr-Fox1ν mouse HCT116 tumor xenograft model^[1].
Nanatinostat (25-50 mg/kg; orally administered; once daily; for 19 days) can significantly reduce tumor volume in a dose-dependent manner in the female BALB/c nude mouse LoVo human colon xenograft model^[1].
Nanatinostat (30 mg/kg; orally administered; once daily; for 28 days) can effectively inhibit tumor growth in the NOD/SCID IL2R gamma^null mouse myeloma model^[2].

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

Animal Model:

Female CrTac:NCr-Fox1(nu) mice (6-8 weeks old; inoculated bilaterally sc with 2 million human HCT116 colon carcinoma cells)^[1].
Dosage:

50 mg/kg
Administration:

Orally administered, once daily, for 14 days
Result:

Almost completely suppressed tumor growth, and the tumor concentration was high, with a tumor-to-plasma concentration ratio reflecting good distribution to the tumor.

Animal Model:

Female BALB/c nude mice (inoculated with LoVo human colorectal xenograft)^[1].
Dosage:

25 mg/kg and 50 mg/kg
Administration:

Orally administered, once daily, for 19 days
Result:

Significantly reduced tumor volume, and the effect was dose-dependent.

Animal Model:

NOD/SCID IL2R gamma^null mice (inoculated subcutaneously with 2×10⁶ H929 myeloma cells)^[2].
Dosage:

30 mg/kg
Administration:

Orally administered, once daily, for up to 28 days
Result:

Effectively inhibited tumor growth.

Clinical Trial

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

Chemical Information

CAS. Nr. 1256448-47-1
Appearance Solid
Molecular Weight 394.40
Formel C₂₀H₁₉FN₆O₂
Color White to off-white
SMILES

FC(C=C1)=CC(C=C2)=C1N=C2CN[C@H]3[C@@]4([H])[C@]3([H])CN(C5=NC=C(C(NO)=O)C=N5)C4
Synonyms

CHR-3996
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

-20°C, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Publications (4)

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Journal Impact Factor

Cancer Res

HDAC5 Loss Enhances Phospholipid-Derived Arachidonic Acid Generation and Confers Sensitivity to cPLA2 Inhibition in Pancreatic Cancer. [Abstract]

2022 Dec 16;82(24):4542-4554. PMID: 36102738
Cell Rep

Comprehensive mass spectrometry screening-derived atlas of HDAC inhibitors reveals histone-specific acetylation changes. [Abstract]

2026 May 26;45(5):117289. PMID: 42030158
Int J Parasitol Drugs Drug Resist

2026 May 17;31:100649.
bioRxiv

2025 January 15.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (126.77 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

2.5355 mL

12.6775 mL

25.3550 mL

5 mM

0.5071 mL

2.5355 mL

5.0710 mL

10 mM

0.2535 mL

1.2677 mL

2.5355 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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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 (6.34 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% Corn Oil

Solubility: 2.5 mg/mL (6.34 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 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)
Handling Instructions (2659 KB)

Verweise

[1]. Moffat D, et al. Discovery of 2-(6-{[(6-fluoroquinolin-2-yl)methyl]amino}bicyclo[3.1.0]hex-3-yl)-N-hydroxypyrimidine-5-carboxamide (CHR-3996), a class I selective orally active histone deacetylase inhibitor. J Med Chem. 2010 Dec 23;53(24):8663-78. [Content Brief]

[2]. Smith EM, et al. The combination of HDAC and aminopeptidase inhibitors is highly synergistic in myeloma and leads to disruption of the NFκB signalling pathway. Oncotarget. 2015 Jul 10;6(19):17314-27. [Content Brief]

[3]. Banerji U, et al. A phase I pharmacokinetic and pharmacodynamic study of CHR-3996, an oral class I selective histone deacetylase inhibitor in refractory solid tumors. Clin Cancer Res. 2012 May 1;18(9):2687-94. [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	2.5355 mL	12.6775 mL	25.3550 mL	63.3874 mL
	5 mM	0.5071 mL	2.5355 mL	5.0710 mL	12.6775 mL
	10 mM	0.2535 mL	1.2677 mL	2.5355 mL	6.3387 mL
	15 mM	0.1690 mL	0.8452 mL	1.6903 mL	4.2258 mL
	20 mM	0.1268 mL	0.6339 mL	1.2677 mL	3.1694 mL
	25 mM	0.1014 mL	0.5071 mL	1.0142 mL	2.5355 mL
	30 mM	0.0845 mL	0.4226 mL	0.8452 mL	2.1129 mL
	40 mM	0.0634 mL	0.3169 mL	0.6339 mL	1.5847 mL
	50 mM	0.0507 mL	0.2535 mL	0.5071 mL	1.2677 mL
	60 mM	0.0423 mL	0.2113 mL	0.4226 mL	1.0565 mL
	80 mM	0.0317 mL	0.1585 mL	0.3169 mL	0.7923 mL
	100 mM	0.0254 mL	0.1268 mL	0.2535 mL	0.6339 mL

Keywords

Nanatinostat

4 Cited Publications

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Nanatinostat

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

High-Efficiency Gene Editing Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) Nanatinostat

Alle HDAC Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Nanatinostat Related Classifications

HY-13432 Related Classifications