Nilotinib(AMN-107)Bcr-Abl kinase inhibitor,selective CAS# 641571-10-0 |
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Quality Control & MSDS
3D structure
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| Cas No. | 641571-10-0 | SDF | Download SDF |
| PubChem ID | 644241 | Appearance | Powder |
| Formula | C28H22F3N7O | M.Wt | 529.53 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | Tasigna; AMN107 | ||
| Solubility | DMSO : 6 mg/mL (11.33 mM; Need ultrasonic) H2O : < 0.1 mg/mL (insoluble) | ||
| Chemical Name | 4-methyl-N-[3-(4-methylimidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]benzamide | ||
| SMILES | CC1=C(C=C(C=C1)C(=O)NC2=CC(=CC(=C2)N3C=C(N=C3)C)C(F)(F)F)NC4=NC=CC(=N4)C5=CN=CC=C5 | ||
| Standard InChIKey | HHZIURLSWUIHRB-UHFFFAOYSA-N | ||
| Standard 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) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Nilotinib (AMN-107) is an inhibitor of Bcr-Abl with IC50 less than 30 nM. | |||||
| Targets | Bcr-Abl | |||||
| IC50 | 30 nM | |||||
| Cell experiment: [1] | |
| Cell lines | CD34+ cells from individual patients with CML |
| Preparation method | The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
| Reacting condition | 5 μM, 16 hours |
| Applications | After 16 hours in culture with nilotinib, long enough for inhibition of CrkL phosphorylation but not for induction of apoptosis, the total CD34+ cell samples studied exhibited only partial and variable inhibition (range, 49% to 0% inhibition) of CrkL phosphorylation. |
| Animal experiment: [2] | |
| Animal models | C57Bl/6J mice injected with 8093 lymphoma cells |
| Dosage form | Oral administration, 75 mg/kg, daily |
| Application | Vehicle treated mice became moribund within 3 weeks of the transplantation. They showed clear symptoms of ALL. Nilotinib-treated mice lived statistically significantly longer as compared with the vehicle-treated mice. This result clearly indicated that nilotinib was very effective in inhibiting the proliferation of the leukemic cells in vivo. |
| Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
| References: [1] Jørgensen H G, Allan E K, Jordanides N E, et al. Nilotinib exerts equipotent antiproliferative effects to imatinib and does not induce apoptosis in CD34+ CML cells. Blood, 2007, 109(9): 4016-4019. [2] Kaur P, Feldhahn N, Zhang B, et al. Nilotinib treatment in mouse models of P190 Bcr/Abl lymphoblastic leukemia. Mol Cancer, 2007, 6(10): 67-77. | |
Nilotinib(AMN-107) Dilution Calculator
Nilotinib(AMN-107) Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 1.8885 mL | 9.4423 mL | 18.8847 mL | 37.7693 mL | 47.2117 mL |
| 5 mM | 0.3777 mL | 1.8885 mL | 3.7769 mL | 7.5539 mL | 9.4423 mL |
| 10 mM | 0.1888 mL | 0.9442 mL | 1.8885 mL | 3.7769 mL | 4.7212 mL |
| 50 mM | 0.0378 mL | 0.1888 mL | 0.3777 mL | 0.7554 mL | 0.9442 mL |
| 100 mM | 0.0189 mL | 0.0944 mL | 0.1888 mL | 0.3777 mL | 0.4721 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Nilotinib is a selective, oral inhibitor of tyrosine kinase with IC50 values of 20, 42, 31, 38, 29 and 41 nM for the autophosphorylation of native BCR-ABL (WT p210) and mutant BCR-ABL (E281K, E292K, F317L, M351T and F486S), respectively [1].
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. Nilotinib showed inhibition activities in KIT mutant cells, including KITV560del, KITK642E and KITV560G (IC50 value of 108 nM). It also was effect to double mutations of KIT, such as KITV560del/V654A, KITV559D/D820Y, KITV560del/V654A (IC50: 192 nM) and KITV559D/D820Y (IC50: 297 nM). Besides that, Nilotinib exerted selective inhibition of PDGFRα and PDGFRβ. It suppressed cell proliferation with IC50 value of 0.54 nM in EOL-1 cells with constitutive activation of FIP1L1-PDGFRα [1, 2].
References:
[1] Weisberg E, Manley P, Mestan J, et al. AMN107 (nilotinib): a novel and selective inhibitor of BCR-ABL. British Journal of Cancer, 2006, 94(12): 1765-1769.
[2] Blay J Y, Von Mehren M. Nilotinib: a novel, selective tyrosine kinase inhibitor//Seminars in oncology. WB Saunders, 2011, 38: S3-S9.
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Activity of nilotinib (AMN-107) alone in advanced gastrointestinal stromal tumors progressing on imatinib and sunitinib. Case report.[Pubmed:19188713]
Chemotherapy. 2009;55(2):132-6.
Nilotinib is a novel tyrosine kinase inhibitor targeting KIT (CD117), PDGFR and BCR-ABL and inhibiting the proliferation of both imatinib-sensitive and imatinib-resistant cells in vitro. Nilotinib, alone or in combination with imatinib, has promising activity in imatinib-resistant patients with advanced gastrointestinal stromal tumors (GISTs), including those who progressed on sunitinib and other tyrosine kinase inhibitors. We describe the beneficial effect of nilotinib 400 mg b.i.d. orally in a 53-year-old patient with metastatic GISTs who had radiologically confirmed disease progression on both imatinib (800 mg/day) and sunitinib (50 mg/day). A positron emission tomography-computerized tomography evaluation showed marked decreases in (18)F-fluorodeoxyglucose uptake in the liver and mesentery region after 3 months of therapy with nilotinib. Nilotinib is an option for patients with advanced GISTs progressing on both imatinib and sunitinib.
