Determine the necessary mass, volume, or concentration for preparing a solution.
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
---|---|---|---|---|
N126111-25mg | 25mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $19.90 | |
N126111-100mg | 100mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $64.90 | |
N126111-250mg | 250mg | In stock | $146.90 | |
N126111-1g | 1g | In stock | $526.90 | |
N126111-5g | 5g | In stock | $2,369.90 |
Potent and selective Bcr/Abl tyrosine kinase inhibitor
Synonyms | Nilotinib [USAN:INN:BAN] | 4-Methyl-3-((4-(3-pyridinyl)-2-pyrimidinyl)amino)-N-(5-(4-methyl-1H-imidazol-1-yl)-3-(trifluoromethyl)phenyl)benzamide | AMN 107 Base Form | 4-methyl-N-(3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl)-3-{(4-(pyridin-3-y |
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Specifications & Purity | Moligand™, ≥99% |
Biochemical and Physiological Mechanisms | Nilotinib is a small molecule Bcr-Abl kinase inhibitor, rationally designed to bind and inhibit the c-Abl kinase active site with more affinity than the prototypic Bcr-Abl kinase inhibitor Imatinib (sc-202180). Nilotinib demonstrates a high affinity for t |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Inhibitor of ABL proto-oncogene 1; non-receptor tyrosine kinase;Inhibitor of discoidin domain receptor tyrosine kinase 1;Inhibitor of discoidin domain receptor tyrosine kinase 2 |
Note | Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details. |
Product Description | Nilotinib (AMN-107) is a Bcr-Abl inhibitor with IC50 less than 30 nM. |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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IUPAC Name | 4-methyl-N-[3-(4-methylimidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]benzamide |
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INCHI | InChI=1S/C28H22F3N7O/c1-17-5-6-19(10-25(17)37-27-33-9-7-24(36-27)20-4-3-8-32-14-20)26(39)35-22-11-21(28(29,30)31)12-23(13-22)38-15-18(2)34-16-38/h3-16H,1-2H3,(H,35,39)(H,33,36,37) |
InChi Key | HHZIURLSWUIHRB-UHFFFAOYSA-N |
Canonical SMILES | CC1=C(C=C(C=C1)C(=O)NC2=CC(=CC(=C2)C(F)(F)F)N3C=C(N=C3)C)NC4=NC=CC(=N4)C5=CN=CC=C5 |
Isomeric SMILES | CC1=C(C=C(C=C1)C(=O)NC2=CC(=CC(=C2)C(F)(F)F)N3C=C(N=C3)C)NC4=NC=CC(=N4)C5=CN=CC=C5 |
PubChem CID | 644241 |
Molecular Weight | 529.53 |
CAS Registry No. | 641571-10-0 |
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DrugBank Ligand | DB04868 |
Wikipedia | Nilotinib |
DiscoveRx TREEspot | Nilotinib| |
PubChem CID | 644241 |
ChEMBL Ligand | CHEMBL255863 |
RCSB PDB Ligand | NIL |
PEP | nilotinib |
Reactome Reaction | R-HSA-9669854, R-HSA-9669900, R-HSA-9669868, R-HSA-9674430, R-HSA-9674095 |
Reactome Drug | R-ALL-9669716 |
DrugCentral Ligand | 1932 |
Enter Lot Number to search for COA:
Find and download the COA for your product by matching the lot number on the packaging.
Lot Number | Certificate Type | Date | Item |
---|---|---|---|
G2402384 | Certificate of Analysis | Apr 12, 2024 | N126111 |
H1802122 | Certificate of Analysis | Jan 18, 2024 | N126111 |
A2218605 | Certificate of Analysis | Nov 10, 2023 | N126111 |
A2218617 | Certificate of Analysis | Nov 10, 2023 | N126111 |
A2218673 | Certificate of Analysis | Nov 10, 2023 | N126111 |
H1809096 | Certificate of Analysis | May 09, 2022 | N126111 |
E2330124 | Certificate of Analysis | Dec 20, 2021 | N126111 |
Solubility | DMSO ≥10mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL |
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Refractive Index | 1.65 |
Melt Point(°C) | 230-242℃ |
Pictogram(s) | GHS08, GHS09, GHS07 |
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Signal | Danger |
Hazard Statements | H315:Causes skin irritation H319:Causes serious eye irritation H373:Causes damage to organs through prolonged or repeated exposure H413:May cause long lasting harmful effects to aquatic life H400:Very toxic to aquatic life H410:Very toxic to aquatic life with long lasting effects H372:Causes damage to organs through prolonged or repeated exposure H360:May damage fertility or the unborn child H361:Suspected of damaging fertility or the unborn child |
Precautionary Statements | P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing. P273:Avoid release to the environment. P280:Wear protective gloves/protective clothing/eye protection/face protection. P302+P352:IF ON SKIN: wash with plenty of water. P321:Specific treatment (see ... on this label). P405:Store locked up. P501:Dispose of contents/container to ... P264:Wash hands [and …] thoroughly after handling. P260:Do not breathe dust/fume/gas/mist/vapors/spray. P270:Do not eat, drink or smoke when using this product. P362+P364:Take off contaminated clothing and wash it before reuse. P391:Collect spillage. P203:Obtain, read and follow all safety instructions before use. P264+P265:Wash hands [and …] thoroughly after handling. Do not touch eyes. P318:if exposed or concerned, get medical advice. P337+P317:If eye irritation persists: Get medical help. P332+P317:If skin irritation occurs: Get medical help. P319:Get medical help if you feel unwell. |
1. Yutao Lou, Mengting Cheng, Qin Cao, Kening Li, Hui Qin, Meihua Bao, Yuan Zhang, Sisi Lin, Yiwen Zhang. (2023) Simultaneous quantification of mirabegron and vibegron in human plasma by HPLC-MS/MS and its application in the clinical determination in patients with tumors associated with overactive bladder. JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS, (115937). [PMID:38198885] [10.1016/j.jpba.2023.115937] |
2. Yutao Lou, Zhiyong Sun, Yitao Chai, Hui Qin, Qing Hu, Yujia Liu, Xiaowei Zheng, Ying Hu, Meihua Bao, Jinping Gu, Yiwen Zhang. (2023) Simultaneous quantification of donafenib, sorafenib, and their N-oxide metabolites in rat plasma using a HPLC-MS/MS method. JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES, 1229 (10): (123871). [PMID:37717473] [10.1016/j.jchromb.2023.123871] |
3. Fangjun Chen, Wenda Chen, Zhenxin Wang, Yingfei Peng, Beili Wang, Baishen Pan, Wei Guo. (2023) Development and clinical application of a liquid chromatography-tandem mass spectrometry-based assay to quantify eight tyrosine kinase inhibitors in human plasma. Journal of Mass Spectrometry and Advances in the Clinical Lab, 29 (2). [PMID:37234251] [10.1016/j.jmsacl.2023.05.001] |
4. Yutao Lou, Hui Qin, Qing Hu, Yitao Chai, Hongying Zhou, Mengting Chen, Qiyue Wang, Ping Huang, Jinping Gu, Yiwen Zhang. (2022) Development and validation of a novel LC-MS/MS method for simultaneous quantitative determination of tyrosine kinase inhibitors in human plasma. JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES, 1208 (123394). [PMID:35932695] [10.1016/j.jchromb.2022.123394] |
5. Wei Jingyao, Liu Ruijuan, Zhang Jiali, Liu Shuaibing, Yan Dan, Wen Xueqian, Tian Xin. (2021) Baicalin Enhanced Oral Bioavailability of Sorafenib in Rats by Inducing Intestine Absorption. Frontiers in Pharmacology, 12 [PMID:34819863] [10.3389/fphar.2021.761763] |
6. Zhao-Yang Wang, Hai-Long Wu, Yue-Yue Chang, Tong Wang, Wei Chen, Gao-Yan Tong, Ru-Qin Yu. (2021) Simultaneous determination of nine tyrosine kinase inhibitors in three complex biological matrices by using high-performance liquid chromatography–diode array detection combined with a second-order calibration method. JOURNAL OF SEPARATION SCIENCE, 44 (21): (3914-3923). [PMID:34463059] [10.1002/jssc.202100293] |
7. Rubin Cheng, Yilan Huang, Yun Fang, Qirui Wang, Meixiu Yan, Yuqing Ge. (2021) Cryptotanshinone enhances the efficacy of Bcr-Abl tyrosine kinase inhibitors via inhibiting STAT3 and eIF4E signalling pathways in chronic myeloid leukaemia. PHARMACEUTICAL BIOLOGY, 59 (1): (891-901). [PMID:34214017] [10.1080/13880209.2021.1944224] |
8. Hui Lv, Juanjuan Wang, Mingying Wang, Li Shen, Ling Xiao, Taijie Chen, Tingzhe Sun, Wenjuan Li, Liangliang Zhu, Xiaoke Zhang. (2021) Potent inhibition of tributyltin (TBT) and triphenyltin (TPT) against multiple UDP-glucuronosyltransferases (UGT): A new potential mechanism underlying endocrine disrupting actions. FOOD AND CHEMICAL TOXICOLOGY, 149 (112039). [PMID:33549631] [10.1016/j.fct.2021.112039] |
9. Zhenzhen Ying, Jingyao Wei, Ruijuan Liu, Fang Zhao, Yifang Yu, Xin Tian. (2020) An UPLC-MS/MS Method for Determination of Osimertinib in Rat Plasma: Application to Investigating the Effect of Ginsenoside Rg3 on the Pharmacokinetics of Osimertinib. International Journal of Analytical Chemistry, 2020 (8814214). [PMID:33456471] [10.1155/2020/8814214] |
10. Yue-Yue Chang, Hai-Long Wu, Huan Fang, Tong Wang, Yang-Zi Ouyang, Xiao-Dong Sun, Gao-Yan Tong, Yu-Jie Ding, Ru-Qin Yu. (2021) Comparison of three chemometric methods for processing HPLC-DAD data with time shifts: Simultaneous determination of ten molecular targeted anti-tumor drugs in different biological samples. TALANTA, 224 (121798). [PMID:33379025] [10.1016/j.talanta.2020.121798] |
11. Ling Xiao, Dehui Chi, Guiju Sheng, Wenjuan Li, Penghui Lin, Sicheng Liang, Liangliang Zhu, Peipei Dong. (2020) Inhibitory effects of UDP-glucuronosyltransferase (UGT) typical ligands against E. coli beta-glucuronidase (GUS). RSC Advances, 10 (39): (22966-22971). [PMID:35520305] [10.1039/D0RA02311F] |
1. Hebron ML, Lonskaya I, Moussa CE. (2013) Nilotinib reverses loss of dopamine neurons and improves motor behavior via autophagic degradation of α-synuclein in Parkinson's disease models.. Hum Mol Genet, 22 (16): (3315-28). [PMID:23666528] [10.1021/op500134e] |
2. Hebron ML, Lonskaya I, Moussa CE. (2013) Tyrosine kinase inhibition facilitates autophagic SNCA/α-synuclein clearance.. Autophagy, 9 (8): (1249-50). [PMID:23787811] [10.1021/op500134e] |
3. Tanabe A, Yamamura Y, Kasahara J, Morigaki R, Kaji R, Goto S. (2014) A novel tyrosine kinase inhibitor AMN107 (nilotinib) normalizes striatal motor behaviors in a mouse model of Parkinson's disease.. Front Cell Neurosci, 8 (13): (50). [PMID:24600352] [10.1021/op500134e] |
4. Karuppagounder SS, Brahmachari S, Lee Y, Dawson VL, Dawson TM, Ko HS. (2014) The c-Abl inhibitor, nilotinib, protects dopaminergic neurons in a preclinical animal model of Parkinson's disease.. Sci Rep, 4 (13): (4874). [PMID:24786396] [10.1021/op500134e] |
5. Yutao Lou, Mengting Cheng, Qin Cao, Kening Li, Hui Qin, Meihua Bao, Yuan Zhang, Sisi Lin, Yiwen Zhang. (2023) Simultaneous quantification of mirabegron and vibegron in human plasma by HPLC-MS/MS and its application in the clinical determination in patients with tumors associated with overactive bladder. JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS, (115937). [PMID:38198885] [10.1016/j.jpba.2023.115937] |
6. Yutao Lou, Zhiyong Sun, Yitao Chai, Hui Qin, Qing Hu, Yujia Liu, Xiaowei Zheng, Ying Hu, Meihua Bao, Jinping Gu, Yiwen Zhang. (2023) Simultaneous quantification of donafenib, sorafenib, and their N-oxide metabolites in rat plasma using a HPLC-MS/MS method. JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES, 1229 (10): (123871). [PMID:37717473] [10.1016/j.jchromb.2023.123871] |
7. Fangjun Chen, Wenda Chen, Zhenxin Wang, Yingfei Peng, Beili Wang, Baishen Pan, Wei Guo. (2023) Development and clinical application of a liquid chromatography-tandem mass spectrometry-based assay to quantify eight tyrosine kinase inhibitors in human plasma. Journal of Mass Spectrometry and Advances in the Clinical Lab, 29 (2). [PMID:37234251] [10.1016/j.jmsacl.2023.05.001] |
8. Yutao Lou, Hui Qin, Qing Hu, Yitao Chai, Hongying Zhou, Mengting Chen, Qiyue Wang, Ping Huang, Jinping Gu, Yiwen Zhang. (2022) Development and validation of a novel LC-MS/MS method for simultaneous quantitative determination of tyrosine kinase inhibitors in human plasma. JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES, 1208 (123394). [PMID:35932695] [10.1016/j.jchromb.2022.123394] |
9. Wei Jingyao, Liu Ruijuan, Zhang Jiali, Liu Shuaibing, Yan Dan, Wen Xueqian, Tian Xin. (2021) Baicalin Enhanced Oral Bioavailability of Sorafenib in Rats by Inducing Intestine Absorption. Frontiers in Pharmacology, 12 [PMID:34819863] [10.3389/fphar.2021.761763] |
10. Zhao-Yang Wang, Hai-Long Wu, Yue-Yue Chang, Tong Wang, Wei Chen, Gao-Yan Tong, Ru-Qin Yu. (2021) Simultaneous determination of nine tyrosine kinase inhibitors in three complex biological matrices by using high-performance liquid chromatography–diode array detection combined with a second-order calibration method. JOURNAL OF SEPARATION SCIENCE, 44 (21): (3914-3923). [PMID:34463059] [10.1002/jssc.202100293] |
11. Rubin Cheng, Yilan Huang, Yun Fang, Qirui Wang, Meixiu Yan, Yuqing Ge. (2021) Cryptotanshinone enhances the efficacy of Bcr-Abl tyrosine kinase inhibitors via inhibiting STAT3 and eIF4E signalling pathways in chronic myeloid leukaemia. PHARMACEUTICAL BIOLOGY, 59 (1): (891-901). [PMID:34214017] [10.1080/13880209.2021.1944224] |
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