受注:045-509-1970 |
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Synonyms | INNO-406, NS-187 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C30H31F3N8O |
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分子量 | 576.62 | CAS No. | 859212-16-1 | |
Solubility (25°C)* | 体外 | DMSO | 100 mg/mL (173.42 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | Bafetinib is a potent and selective dual Bcr-Abl/Lyn inhibitor with IC50 of 5.8 nM/19 nM in cell-free assays, does not inhibit the phosphorylation of the T315I mutant and is less potent to PDGFR and c-Kit. |
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in vitro | Bafetinib blocks WT Bcr-Abl autophosphorylation and its downstream kinase activity with IC50 of 11 nM and 22 nM in K562 and 293T cells, respectively. Bafetinib suppresses the growth of the Bcr-Abl-positive cell lines including K562, KU812, and BaF3/wt cells potently without effects on the proliferation of the Bcr-Abl-negative U937 cell line. Moreover, Bafetinib exhibits a dose-dependent antiproliferative effect against Bcr-Abl point mutant cell lines, such as BaF3/E255K cells. [1] In Bcr-Abl+ leukemia cell lines, Bafetinib induces both caspase-mediated and caspase-independent cell death by blocking the phosphorylation of Bcr-Abl. [2] |
in vivo | In Bcr-Abl–positive KU812 mouse model, Bafetinib (0.2 mg/kg/day) significantly inhibits tumor growth, and completely inhibits tumor growth without adverse effects at 20 mg/kg/day. For Balb/c mice, Bafetinib shows maximal tolerated dose of 200 mg/kg/d and bioavailability value (BA) of 32%. [1] In a Central nervous system (CNS) leukemia model bearing Ba/F3/wt bcr-ablGFP, Ba/F3/Q252H, or Ba/F3/M351T cells, combination treatment of Bafetinib (60 mg/kg) and cyclosporine A (CsA) (50 mg/kg) leads to more significant inhibition of leukemia growth in the brain than either Bafetinib or CsA alone. [3] |
特徴 | Dual Bcr-Abl/Lyn inhibitor. |
キナーゼアッセイ | Kinase assay | |
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Bcr-Abl kinase assays are performed in 25 μL of reaction mixture containing 250 μM peptide substrate, 740 Bq/μL [γ-33P]ATP, and 20 μM cold adenosine triphosphate (ATP) by using the SignaTECT protein tyrosine kinase assay system. Each Bcr-Abl kinase is used at a concentration of 10 nM. Kinase assays for Abl, Src, and Lyn are carried out with an enzyme-linked immunosorbent assay (ELISA) kit. The inhibitory effects of NS-187 against 79 tyrosine kinases are tested with KinaseProfiler. | ||
細胞アッセイ | 細胞株 | K562, BaF3/wt, BaF3/E255K, and BaF3/T315I cells |
濃度 | 0-10 μM | |
反応時間 | 72 hours | |
実験の流れ | K562, BaF3/wt, BaF3/E255K, and BaF3/T315I cells are plated at 1 × 103 in 96-well plates, whereas KU812 and U937 cells are plated at 5 × 103 in 96-well plates. Cells are incubated with serial dilutions of Bafetinib for 3 days. Cell proliferation is measured by MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide; Nacalai Tesque) assay, and the 50% inhibitory concentration (IC50) values are calculated by fitting the data to a logistic curve. |
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動物実験 | 動物モデル | KU812 xenograft is established by subcutaneous injection of KU812 cells into the right flank of Balb/c-nu/nu female mice. |
投薬量 | ≤20 mg/kg/day | |
投与方法 | Administered via p.o. |
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Data from [Data independently produced by , , Scientific Reports, 2016, 6:25694.]
Focal adhesion kinase activation by calcium-dependent calpain is involved in chronic lymphocytic leukaemia cell aggressiveness [ Br J Haematol, 2023, 10.1111/bjh.18996] | PubMed: 37495265 |
Tyrosine Kinase Inhibitor Profiling Using Multiple Forskolin-Responsive Reporter Cells [ Int J Mol Sci, 2023, 10.3390/ijms241813863] | PubMed: 37762164 |
Tyrosine Kinase Inhibitor Profiling Using Multiple Forskolin-Responsive Reporter Cells [ Int J Mol Sci, 2023, 24(18)13863] | PubMed: 37762164 |
Lyn-mediated glycolysis enhancement of microglia contributes to neuropathic pain through facilitating IRF5 nuclear translocation in spinal dorsal horn [ J Cell Mol Med, 2023, 10.1111/jcmm.17759] | PubMed: 37132040 |
A community challenge for a pancancer drug mechanism of action inference from perturbational profile data [ Cell Rep Med, 2022, 3(1):100492] | PubMed: 35106508 |
Listeria toxin promotes phosphorylation of the inflammasome adaptor ASC through Lyn and Syk to exacerbate pathogen expansion [ Cell Rep, 2022, 38(8):110414] | PubMed: 35196496 |
Establishment and Characterization of NCC-PMP1-C1: A Novel Patient-Derived Cell Line of Metastatic Pseudomyxoma Peritonei [ J Pers Med, 2022, 12(2)258] | PubMed: 35207746 |
Brain-Derived Neurotrophic Factor regulates LYN kinase mediated Myosin Light Chain Kinase activation to modulate non-muscle myosin II activity in hippocampal neurons [ J Biol Chem, 2022, S0021-9258(22)00494-X] | PubMed: 35598826 |
Establishment and characterization of NCC-UPS4-C1: a novel cell line of undifferentiated pleomorphic sarcoma from a patient with Li-Fraumeni syndrome [ Hum Cell, 2022, 10.1007/s13577-022-00671-y] | PubMed: 35118583 |
A hotspot mutation in transcription factor IKZF3 drives B cell neoplasia via transcriptional dysregulation [ Cancer Cell, 2021, 39(3):380-393.e8] | PubMed: 33689703 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
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