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Purity: ≥98%
Nilotinib (formerly also known as AMN-107, AMN107; trade name Tasigna) is a potent, orally bioavailable aminopyrimidine-based Bcr-Abl inhibitor with antineoplastic activity. It inhibits Bcr-Abl with an IC50 of<30 nM in Murine myeloid progenitor cells. As of 2007, nilotinib was approved by the US FDA for the treatment of imatinib-resistant chronic myelogenous leukemia which has the Philadelphia chromosome. Nilotinib was designed based on the structure of imatinib and showed the superiority over imatinib in newly diagnosed or imatinib-resistant chronic myelogenous leukemia (CML). It was more potent than imatinib to wild-type BCR-ABL in a wide range of CML-derived and transfected cell lines. Nilotinib was also efficacious in gastrointestinal stromal tumors.
| ln Vitro |
Specifically designed to interact with the ATP-binding site of BCR-ABL with a higher affinity than imatinib, nilotinib (AMN107), a selective Abl inhibitor, is also significantly more potent than imatinib (IC50<30 nM) and maintains activity against the majority of BCR-ABL point mutants that confer resistance to imatinib[1]. Nilotinib exhibits noteworthy antitumor efficacy against GIST xenograft lines and GIST cell lines resistant to imatinib; parent cell lines GK1C and GK3C display imatinib sensitivity with IC50 values of 4.59±0.97 µM and 11.15± 1.48 µM, respectively; imatinib-resistant cell lines GK1C-IR and GK3C-IR demonstrate 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].
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| ln Vivo |
When given orally to BALB/cSLc-nu/nu mice with a GIST xenograft, nilotinib (oral gavage, 40 mg/kg, daily, 4 weeks) has anticancer effects that are same or greater[2]. Nilotinib reduces PDGFR α and β levels as well as apoptotic scores in the colon, while also having a strong healing effect on the macroscopic and microscopic pathologic scores and ensuring significant mucosal healing in the indomethacin-induced enterocolitis rat model[3].
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| Animal Protocol |
Animal/Disease Models: BALB/cSLc-nu/nu (nude) mice with GIST xenograft (GK1X, GK2X and GK3X)[2]
Doses: 40 mg/kg Route of Administration: po (oral gavage); daily; 4 weeks Experimental Results: Inhibited tumor growth by 69.6% in GK1X, 85.3% in GK2X and 47.5% in GK3X xenograft line. |
| 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.
[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. [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. [4]. Fujita KI, et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites. J Pharm Sci. 2017 Sep;106(9):2632-2641. [5]. Meirson T, et al. Targeting invadopodia-mediated breast cancer metastasis by using ABL kinase inhibitors. Oncotarget. 2018 Apr 24;9(31):22158-22183. |
| Molecular Formula |
C28H22F3N7O
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|---|---|
| Molecular Weight |
529.52
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| CAS # |
641571-10-0
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| Related CAS # |
Nilotinib monohydrochloride monohydrate;923288-90-8;Nilotinib-d6;1268356-17-7;Nilotinib-d3;1215678-43-5;Nilotinib hydrochloride;923288-95-3
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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
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| InChi Key |
HHZIURLSWUIHRB-UHFFFAOYSA-N
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| InChi Code |
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)
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| Chemical Name |
4-methyl-N-(3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl)-3-{(4-(pyridin-3-yl)pyrimidin-2-yl)amino}benzamide
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| Synonyms |
Nilotinib free base; AMN 107; AMN107; AMN-107; Nilotinib; US brand name: Tasigna.
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8885 mL | 9.4425 mL | 18.8850 mL | |
| 5 mM | 0.3777 mL | 1.8885 mL | 3.7770 mL | |
| 10 mM | 0.1889 mL | 0.9443 mL | 1.8885 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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