Nilotinib hydrochloride
Based on 53 publication(s) in Google Scholar
Nilotinib (AMN107) hydrochloride is an orally active Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity and can be used in studies of chronic myelogenous leukaemia.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.86%
- CAS. Nr.: 923288-95-3
- Formel: C28H23ClF3N7O
- Molecular Weight:565.98
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Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Biologische Aktivität
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Chemical Information
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HY-10159
NilotinibBcr-Abl Inhibitor -
HY-15728
RadotinibBcr-Abl1 Inhibitor -
HY-12047
PonatinibMulti-targeted Kinase Inhibitor -
HY-104010
AsciminibBCR-ABL1 Inhibitor -
HY-15738
GNF-5Bcr-Abl Inhibitor -
HY-15666
OlverembatinibBcr-Abl Inhibitor -
HY-13024
RebastinibKinase Inhibitor -
HY-10181A
Dasatinib hydrochlorideSrc/Bcr-Abl Inhibitor -
HY-11007
GNF-2Bcr-Abl Inhibitor -
HY-50868
BafetinibLyn/Bcr-Abl Inhibitor -
HY-10395
PD173955Src Inhibitor -
HY-10159R
Nilotinib (Standard)Bcr-Abl Inhibitor
Publications Citing Use of MedChemExpress (MCE) Nilotinib hydrochloride
More- Nat Cancer. 2025 Apr;6(4):666-681. [Abstract]
- Cell Mol Immunol. 2024 Aug;21(8):856-872. [Abstract]
- Cancer Res. 2025 Jan 2;85(1):101-117. [Abstract]
- Nat Commun. 2026 Feb 24;17(1):1963. [Abstract]
- J Adv Res. 2026 Jul 28:S2090-1232(26)00594-1.
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Cell Rep Med. 2025 Apr 15;6(4):102053. [Abstract]
- Biomaterials. 2022 Oct:289:121800. [Abstract]
- Cell Death Dis. 2021 Sep 25;12(10):875. [Abstract]
- Cancer Lett. 2024 Sep 28:600:217150. [Abstract]
- Phytomedicine. 2025 Nov 25:148:157332. [Abstract]
- Free Radic Biol Med. 2026 Aug 16:252:493-508. [Abstract]
- Br J Cancer. 2022 Mar;126(5):778-790. [Abstract]
- Cell Syst. 2018 Apr 25;6(4):424-443.e7. [Abstract]
- Talanta. 2026 Sep 1:307:129772. [Abstract]
- Ecotoxicol Environ Saf. 2025 Nov 15:307:119433. [Abstract]
- Breast Cancer Res. 2023 May 5;25(1):51. [Abstract]
- Cell Rep Methods. 2023 Oct 23;3(10):100599. [Abstract]
- Eur J Pharmacol. 2021 Apr 15:897:173944. [Abstract]
- Cancer Biol Ther. 2019;20(6):877-885. [Abstract]
- Biomolecules. 2022 Jun 11;12(6):819. [Abstract]
- Stem Cell Reports. 2019 May 14;12(5):996-1006. [Abstract]
- Glia. 2022 Jun;70(6):1084-1099. [Abstract]
- Toxicology. 2024 May 15:505:153830. [Abstract]
- Target Oncol. 2020 Oct;15(5):659-671. [Abstract]
- Mol Med Rep. 2025 Jun;31(6):165. [Abstract]
- J Pharm Sci. 2017 Sep;106(9):2632-2641. [Abstract]
- Diseases. 2023 Oct 23;11(4):147. [Abstract]
- ACS Chem Biol. 2016 Apr 15;11(4):992-1000. [Abstract]
- Cancer Med. 2016 Nov;5(11):3223-3234. [Abstract]
- Toxicol Lett. 2022 Jul 15:365:11-23. [Abstract]
- PLoS One. 2024 Nov 1;19(11):e0308647. [Abstract]
- Drug Metab Pharmacokinet. 2020 Feb;35(1):102-110. [Abstract]
- Leuk Lymphoma. 2015;56(8):2416-23. [Abstract]
- Anticancer Drugs. 2026 Aug 1;37(7):449-461. [Abstract]
- Int J Mass Spectrom. 442 (2019) 44-50.
- Biomed Chromatogr. 2019 Dec;33(12):e4674. [Abstract]
- Xenobiotica. 2018 Oct;48(10):1059-1071. [Abstract]
- Res Sq. 2026 May 6.
- bioRxiv. 2026 Feb 20.
- Blood Vessel Thromb Hemost. 2025 Nov 17.
- bioRxiv. 2025 Sep 30.
- Biomed Pharmacother. 2025 Aug:189:118246. [Abstract]
- bioRxiv. 2025 February 26.
- Research Square Preprint. 2024 Nov 06.
- bioRxiv. 2024 Dec 22:2024.12.21.629902. [Abstract]
- bioRxiv. 2024 Dec 20:2024.12.19.629301. [Abstract]
- bioRxiv. 2024 May 8:2024.05.07.592424. [Abstract]
- bioRxiv. January 25, 2022.
- Patent. US20210299273A1.
- Patent. US20190084960A1
- Oncotarget. 2018 Apr 24;9(31):22158-22183. [Abstract]
- Technical University of Munich. 24.01.2018.
Customer Validation & Images
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Cell Proliferation/Viability Assay
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Cell Migration/Invasion Assay
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IHC
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Bio/Physico-chemical Assay
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Cell Proliferation/Viability Assay
Biologische Aktivität
Beschreibung
In Vitro
Nilotinib hydrochloride, 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 hydrochloride 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 hydrochloride 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.
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Animal Model:BALB/cSLc-nu/nu mice with GIST xenograft (GK1X, GK2X and GK3X)[2]
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Dosage:40 mg/kg
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Administration:Oral gavage; daily; 4 weeks
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Result:Inhibited tumor growth by 69.6% in GK1X, 85.3% in GK2X and 47.5% in GK3X xenograft line.
Chemical Information
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CAS. Nr. 923288-95-3
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Appearance Solid
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Molecular Weight 565.98
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Formel C28H23ClF3N7O
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Color White to off-white
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SMILES
O=C(NC1=CC(C(F)(F)F)=CC(N2C=C(C)N=C2)=C1)C3=CC=C(C)C(NC4=NC=CC(C5=CC=CN=C5)=N4)=C3.[H]Cl
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Synonyms
AMN107 hydrochloride
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (53)
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Journal Impact Factor
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Most Recent
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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
2026 Feb 24;17(1):1963. PMID: 41735331 -
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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
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 hydrochloride 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.
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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
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 hydrochloride 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.
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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
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 hydrochloride 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.
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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
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 hydrochloride 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.
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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 -
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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 -
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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 -
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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
2024 May 8:2024.05.07.592424. PMID: 38766123 -
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Oncotarget
2018 Apr 24;9(31):22158-22183. PMID: 29774130
Nilotinib hydrochloride 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).
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Lösungsmittel & Löslichkeit
In Vitro:
DMSO : ≥ 125 mg/mL (220.86 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (273 KB)
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SDS (558 KB)
- English - EN (558 KB)
- Français - FR (558 KB)
- Deutsch - DE (558 KB)
- Norwegian - NO (558 KB)
- Español - ES (558 KB)
- Swedish - SV (558 KB)
- Italian - IT (558 KB)
- Korean - KR (558 KB)
- Portuguese - PT (558 KB)
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Handling Instructions (2659 KB)
Verweise
[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]. Meirson T, et al. Targeting invadopodia-mediated breast cancer metastasis by using ABL kinase inhibitors. Oncotarget. 2018 Apr 24;9(31):22158-22183. [Content Brief]
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, 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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7668 mL | 8.8342 mL | 17.6685 mL | 44.1712 mL |
| 5 mM | 0.3534 mL | 1.7668 mL | 3.5337 mL | 8.8342 mL | |
| 10 mM | 0.1767 mL | 0.8834 mL | 1.7668 mL | 4.4171 mL | |
| 15 mM | 0.1178 mL | 0.5889 mL | 1.1779 mL | 2.9447 mL | |
| 20 mM | 0.0883 mL | 0.4417 mL | 0.8834 mL | 2.2086 mL | |
| 25 mM | 0.0707 mL | 0.3534 mL | 0.7067 mL | 1.7668 mL | |
| 30 mM | 0.0589 mL | 0.2945 mL | 0.5889 mL | 1.4724 mL | |
| 40 mM | 0.0442 mL | 0.2209 mL | 0.4417 mL | 1.1043 mL | |
| 50 mM | 0.0353 mL | 0.1767 mL | 0.3534 mL | 0.8834 mL | |
| 60 mM | 0.0294 mL | 0.1472 mL | 0.2945 mL | 0.7362 mL | |
| 80 mM | 0.0221 mL | 0.1104 mL | 0.2209 mL | 0.5521 mL | |
| 100 mM | 0.0177 mL | 0.0883 mL | 0.1767 mL | 0.4417 mL |
Nilotinib hydrochloride Related Classifications
HY-10159B Related Classifications
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