Cat. No.: HY-10159A

Nilotinib monohydrochloride monohydrate

(Synonyms: AMN107 monohydrochloride monohydrate)

52 Cited Publications

Customer Review

Based on 52 publication(s) in Google Scholar

Nilotinib monohydrochloride monohydrate is a second generation tyrosine kinase inhibitor (TKI), is significantly potent against BCR-ABL, and is active against many BCR-ABL mutants.

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

Purity: 99.91%
CAS No.: 923288-90-8
Formula: C₂₈H₂₅ClF₃N₇O₂
Molecular Weight:583.99

Storage:

4°C, sealed storage, away from moisture

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

Nilotinib monohydrochloride monohydrate Chemical Structure

CAS No.: 923288-90-8

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (52)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

Nilotinib monohydrochloride monohydrate is a second generation tyrosine kinase inhibitor (TKI), is significantly potent against BCR-ABL, and is active against many BCR-ABL mutants.

IC₅₀ & Target

Bcr-Abl^[1]

All Bcr-Abl Isoforms :

Abl
Bcr-Abl

In Vitro

Nilotinib (AMN107) monohydrochloride monohydrate, selective Abl inhibitor, is designed to interact with the ATP-binding site of BCR-ABL with a higher affinity than imatinib while being significantly more potent compared with imatinib (IC₅₀<30 nM), also maintains activity against most of the BCR-ABL point mutants that confer Imatinib resistance^[1].
Nilotinib monohydrochloride monohydrate demonstrates significant antitumor efficacy against GIST xenograft lines and imatinib-resistant GIST cell lines which parent cell lines GK1C and GK3C shows imatinib sensitivity with IC₅₀ of 4.59±0.97 μM and 11.15±1.48 μM, respectively, imatinib-resistant cell lines GK1C-IR and GK3C-IR shows Imatinib resistance with IC₅₀ values of 11.74±0.17 μM (P<0.001) and 41.37±1.07 μM (P<0.001), respectively^[2].

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

In Vivo

Nilotinib monohydrochloride monohydrate (oral gavage, 40 mg/kg, daily, 4 weeks) shows equivalent or higher antitumor effects in BALB/cSLc-nu/nu mice with GIST xenograft^[2].
Nilotinib monohydrochloride monohydrate has a significant healing effect on the macroscopic and microscopic pathologic scores and ensures considerable mucosal healing in the indomethacin-induced enterocolitis rat model while decreases the PDGFR α and β levels and apoptotic scores in the colon^[3].

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

Animal Model:

BALB/cSLc-nu/nu mice with GIST xenograft (GK1X, GK2X and GK3X)^[2]
Dosage:

40 mg/kg
Administration:

Oral gavage; daily; 4 weeks
Result:

Inhibited tumor growth by 69.6% in GK1X, 85.3% in GK2X and 47.5% in GK3X xenograft line.

Chemical Information

CAS No. 923288-90-8
Appearance Solid
Molecular Weight 583.99
Formula C₂₈H₂₅ClF₃N₇O₂
Color White to light yellow
SMILES

O=C(NC1=CC(C(F)(F)F)=CC(N2C=NC(C)=C2)=C1)C3=CC=C(C)C(NC4=NC=CC(C5=CC=CN=C5)=N4)=C3.[H]Cl.O
Synonyms

AMN107 monohydrochloride monohydrate
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

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

Publications (52)

All Cell Migration/Invasion AssayCell Proliferation/Viability AssayBio/Physico-chemical AssayIHC

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Journal Impact Factor

Nat Cancer

A Gremlin 1-expressing splenic niche cell population restrains chronic myeloid leukemia by antagonizing the BMP pathway. [Abstract]

2025 Apr;6(4):666-681. PMID: 40097655
Cell Mol Immunol

Chaperone- and PTM-mediated activation of IRF1 tames radiation-induced cell death and the inflammatory response. [Abstract]

2024 Aug;21(8):856-872. PMID: 38849539
Cancer Res

Targeted Degradation of SOS1 Exhibits Potent Anticancer Activity and Overcomes Resistance in KRAS-Mutant Tumors and BCR-ABL-Positive Leukemia. [Abstract]

2025 Jan 2;85(1):101-117. PMID: 39437162
Nat Commun

Context-dependent translation inhibition as a cancer therapeutic modality. [Abstract]

2026 Feb 24;17(1):1963. PMID: 41735331
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Cell Rep Med

CAN-Scan: A multi-omic phenotype-driven precision oncology platform identifies prognostic biomarkers of therapy response for colorectal cancer. [Abstract]

2025 Apr 15;6(4):102053. PMID: 40187357
Biomaterials

Automated discovery of nanomaterials via drug aggregation induced emission. [Abstract]

2022 Oct:289:121800. PMID: 36166893
Cell Death Dis

Combination of tyrosine kinase inhibitors and the MCL1 inhibitor S63845 exerts synergistic antitumorigenic effects on CML cells. [Abstract]

2021 Sep 25;12(10):875. PMID: 34564697
Cancer Lett

Serotonylation in tumor-associated fibroblasts contributes to the tumor-promoting roles of serotonin in colorectal cancer. [Abstract]

2024 Sep 28:600:217150. PMID: 39097134
Phytomedicine

Piperine targets SOAT1 to inhibit the progression of esophageal squamous cell carcinoma via ferroptosis. [Abstract]

2025 Nov 25:148:157332. PMID: 41061292
Free Radic Biol Med

Targeted delivery of nebivolol via lactoferrin-modified liposomes inhibits NEK7-mediated pyroptosis to ameliorate inflammatory bowel disease. [Abstract]

2026 Aug 16:252:493-508. PMID: 42061481
Br J Cancer

PCK1 regulates neuroendocrine differentiation in a positive feedback loop of LIF/ZBTB46 signalling in castration-resistant prostate cancer. [Abstract]

2022 Mar;126(5):778-790. PMID: 34815524
Cell Syst

A Library of Phosphoproteomic and Chromatin Signatures for Characterizing Cellular Responses to Drug Perturbations. [Abstract]

2018 Apr 25;6(4):424-443.e7. PMID: 29655704
Talanta

A targeted strategy for screening bioactive inhibitors from Morus alba L.: Immobilized PTP1B affinity chromatography. [Abstract]

2026 Sep 1:307:129772. PMID: 41955787
Ecotoxicol Environ Saf

PPARγ-responsive luciferase reporter system for high-throughput screening of chemical toxins with potential pulmonary fibrosis effects. [Abstract]

2025 Nov 15:307:119433. PMID: 41273832
Breast Cancer Res

Systematic screening identifies ABCG2 as critical factor underlying synergy of kinase inhibitors with transcriptional CDK inhibitors. [Abstract]

2023 May 5;25(1):51. PMID: 37147730
Cell Rep Methods

RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]

2023 Oct 23;3(10):100599. PMID: 37797618
Eur J Pharmacol

Discovery of a highly potent kinase inhibitor capable of overcoming multiple imatinib-resistant ABL mutants for chronic myeloid leukemia (CML). [Abstract]

2021 Apr 15:897:173944. PMID: 33581133
Cancer Biol Ther

Discovery and characterization of a novel highly potent and selective type II native and drug-resistant V299L mutant BCR-ABL inhibitor (CHMFL-ABL-039) for Chronic Myeloid Leukemia (CML). [Abstract]

2019;20(6):877-885. PMID: 30894066

Nilotinib monohydrochloride monohydrate purchased from MedChemExpress. Usage Cited in: Cancer Biol Ther. 2019;20(6):877-885. [Abstract]

Nilotinib (0.1 μM; 15 days). The anti-colony formation effect of CHMFL-ABL-039 against K562, KU812, MEG-01, and BaF3-BCR-ABL-V299L cells was observed.
Biomolecules

Investigating the Effect of Tyrosine Kinase Inhibitors on the Interaction between Human Serum Albumin by Atomic Force Microscopy. [Abstract]

2022 Jun 11;12(6):819. PMID: 35740944
Stem Cell Reports

Ibrutinib Displays Atrial-Specific Toxicity in Human Stem Cell-Derived Cardiomyocytes. [Abstract]

2019 May 14;12(5):996-1006. PMID: 31031187
Glia

c-Abl-induced Olig2 phosphorylation regulates the proliferation of oligodendrocyte precursor cells. [Abstract]

2022 Jun;70(6):1084-1099. PMID: 35156232
Toxicology

Phosphoproteomics reveals a novel mechanism underlying the proarrhythmic effects of nilotinib, vandetanib, and mobocertinib. [Abstract]

2024 May 15:505:153830. PMID: 38754619
Target Oncol

In Vitro Comparison of the Effects of Imatinib and Ponatinib on Chronic Myeloid Leukemia Progenitor/Stem Cell Features. [Abstract]

2020 Oct;15(5):659-671. PMID: 32780298
Mol Med Rep

Identification of the clinical value and biological effects of TTN mutation in liver cancer. [Abstract]

2025 Jun;31(6):165. PMID: 40242970

Nilotinib monohydrochloride monohydrate purchased from MedChemExpress. Usage Cited in: Mol Med Rep. 2025 Jun;31(6):165. [Abstract]

CCK-8 assays were used to assess the IC₅₀ of Nilotinib (0–20 μM) in JHH7, HepG2, Li7, Huh7, Hep3B, and SNU182 liver cancer cell lines over 48 h.
J Pharm Sci

Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites. [Abstract]

2017 Sep;106(9):2632-2641. PMID: 28479358
Diseases

Examining the Effects of Dasatinib, Sorafenib, and Nilotinib on Vascular Smooth Muscle Cells: Insights into Proliferation, Migration, and Gene Expression Dynamics. [Abstract]

2023 Oct 23;11(4):147. PMID: 37873791
ACS Chem Biol

Stable Colloidal Drug Aggregates Catch and Release Active Enzymes. [Abstract]

2016 Apr 15;11(4):992-1000. PMID: 26741163
Cancer Med

Direct effect of dasatinib on signal transduction pathways associated with a rapid mobilization of cytotoxic lymphocytes. [Abstract]

2016 Nov;5(11):3223-3234. PMID: 27726309

Nilotinib monohydrochloride monohydrate purchased from MedChemExpress. Usage Cited in: Cancer Med. 2016 Nov;5(11):3223-3234. [Abstract]

Direct effect of dasatinib on cytotoxic lymphocytes. Mononuclear cells obtained from peripheral blood before taking dasatinib were incubated with dimethylsulfoxide (DMSO) vehicle, 100 nmol/L or 300 nmol/L dasatinib, 2 μmol/L imatinib, or 2 μmol/L Nilotinib, for 1 h.
Toxicol Lett

Downregulation of hERG channel expression by tyrosine kinase inhibitors nilotinib and vandetanib predominantly contributes to arrhythmogenesis. [Abstract]

2022 Jul 15:365:11-23. PMID: 35680041
PLoS One

A novel small molecule screening assay using normal human chondrocytes toward osteoarthritis drug discovery. [Abstract]

2024 Nov 1;19(11):e0308647. PMID: 39485774
Drug Metab Pharmacokinet

Influence of gastrointestinal activity on the absorption of nilotinib. [Abstract]

2020 Feb;35(1):102-110. PMID: 31732429
Leuk Lymphoma

ETV6/ARG oncoprotein confers autonomous cell growth by enhancing c-Myc expression via signal transducer and activator of transcription 5 activation in the acute promyelocytic leukemia cell line HT93A. [Abstract]

2015;56(8):2416-23. PMID: 25373509

Nilotinib monohydrochloride monohydrate purchased from MedChemExpress. Usage Cited in: Leuk Lymphoma. 2015;56(8):2416-23. [Abstract]

Cell cycle analysis of HT93A cells by flow cytometry. Cells are treated with 100 nM Nilotinib and 50 ng/mL G-CSF alone or in combination for 48 h before the cell cycle is analyzed. Nilotinib treatment increases the fraction of cells in G0/G1 phase and decreased the S+G2/M-phase fraction.
Anticancer Drugs

The novel integrin-linked kinase inhibitor nilotinib suppresses cancer progression by promoting ubiquitylation of autoimmune regulator in oesophageal squamous cell carcinoma. [Abstract]

2026 Aug 1;37(7):449-461. PMID: 42069146
Int J Mass Spectrom

442 (2019) 44-50.
Biomed Chromatogr

UPLC-MS/MS study of the effect of dandelion root extract on the plasma levels of the selected irreversible tyrosine kinase inhibitors dasatinib, imatinib and nilotinib in rats: Potential risk of pharmacokinetic interactions. [Abstract]

2019 Dec;33(12):e4674. PMID: 31376170
Xenobiotica

Substrate-dependent effects of molecular-targeted anticancer agents on activity of organic anion transporting polypeptide 1B1. [Abstract]

2018 Oct;48(10):1059-1071. PMID: 29034773
Res Sq

2026 May 6.
bioRxiv

2026 Feb 20.
Blood Vessel Thromb Hemost

2025 Nov 17.
bioRxiv

2025 Sep 30.
Biomed Pharmacother

Identification of nsp16 inhibitors of SARS -CoV-2, SARS -CoV-1 and MERS-CoV from FDA-approved drugs using in silico and in vitro methods. [Abstract]

2025 Aug:189:118246. PMID: 40543162
bioRxiv

2025 February 26.
Research Square Preprint

2024 Nov 06.
bioRxiv

Leukemia escapes immunity by imposing a Type-1 regulatory program on neoantigen-specific CD4+ T cells. [Abstract]

2024 Dec 22:2024.12.21.629902. PMID: 39764001
bioRxiv

BRAFV600 and ErbB inhibitors directly activate GCN2 in an off-target manner to limit cancer cell proliferation. [Abstract]

2024 Dec 20:2024.12.19.629301. PMID: 39763857
bioRxiv

Collagen I is a critical organizer of scarring and CNS regeneration failure. [Abstract]

2024 May 8:2024.05.07.592424. PMID: 38766123
bioRxiv

January 25, 2022.
Patent

US20210299273A1.
Patent

US20190084960A1
Oncotarget

Targeting invadopodia-mediated breast cancer metastasis by using ABL kinase inhibitors. [Abstract]

2018 Apr 24;9(31):22158-22183. PMID: 29774130

Nilotinib monohydrochloride monohydrate purchased from MedChemExpress. Usage Cited in: Oncotarget. 2018 Apr 24;9(31):22158-22183. [Abstract]

Primary tumors are dissected at the end of experiment and subjected to immunohistochemistry. Representative images of primary tumor sections stained with anti-PCNA (proliferation), anti-cleaved caspase 3 (apoptosis), and anti-CD31 (angiogenesis).
Technical University of Munich

24.01.2018.

Solvent & Solubility

In Vitro:

DMSO : 33.33 mg/mL (57.07 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 12.9 mg/mL (22.09 mM; ultrasonic and warming and adjust pH to 1 with 1 M HCl and heat to 60°C)

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

1.7124 mL

8.5618 mL

17.1236 mL

5 mM

0.3425 mL

1.7124 mL

3.4247 mL

10 mM

0.1712 mL

0.8562 mL

1.7124 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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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)

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 90% Corn Oil

Solubility: ≥ 5 mg/mL (8.56 mM); Clear solution

This protocol yields a clear solution of ≥ 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 (50.0 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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (643 KB)
- English - EN (643 KB)
- Français - FR (643 KB)
- Deutsch - DE (643 KB)
- Norwegian - NO (643 KB)
- Español - ES (643 KB)
- Swedish - SV (643 KB)
- Italian - IT (643 KB)
- Korean - KR (643 KB)
- Portuguese - PT (643 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]. Weisberg E, et al. Beneficial effects of combining nilotinib and imatinib in preclinical models of BCR-ABL+ leukemias. Blood. 2007 Mar 1;109(5):2112-20. [Content Brief]

[2]. Sako H, et al. Antitumor effect of the tyrosine kinase inhibitor Nilotinib on gastrointestinal stromal tumor (GIST) and Imatinib-resistant GIST cells. PLoS One. 2014 Sep 15;9(9):e107613. [Content Brief]

[3]. Dervis Hakim G, et al. Mucosal healing effect of nilotinib in indomethacin-induced enterocolitis: A rat model. World J Gastroenterol. 2015 Nov 28;21(44):12576-85. [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
H₂O / DMSO	1 mM	1.7124 mL	8.5618 mL	17.1236 mL	42.8090 mL
	5 mM	0.3425 mL	1.7124 mL	3.4247 mL	8.5618 mL
	10 mM	0.1712 mL	0.8562 mL	1.7124 mL	4.2809 mL
	15 mM	0.1142 mL	0.5708 mL	1.1416 mL	2.8539 mL
	20 mM	0.0856 mL	0.4281 mL	0.8562 mL	2.1404 mL
DMSO	25 mM	0.0685 mL	0.3425 mL	0.6849 mL	1.7124 mL
	30 mM	0.0571 mL	0.2854 mL	0.5708 mL	1.4270 mL
	40 mM	0.0428 mL	0.2140 mL	0.4281 mL	1.0702 mL
	50 mM	0.0342 mL	0.1712 mL	0.3425 mL	0.8562 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Keywords

Nilotinib monohydrochloride monohydrate

52 Cited Publications

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Nilotinib monohydrochloride monohydrate

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Publications Citing Use of MedChemExpress (MCE) Nilotinib monohydrochloride monohydrate

All Bcr-Abl Isoforms

Biological Activity

Chemical Information

Publications (52)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Nilotinib monohydrochloride monohydrate Related Classifications

HY-10159A Related Classifications