受注:045-509-1970 |
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C11H8Br2N2O2
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分子量 | 360 | CAS No. | 244240-24-2 | |
Solubility (25°C)* | 体外 | DMSO | 72 mg/mL warmed with 50ºC water bath (200.0 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 | LFM-A13 is a specific Bruton's tyrosine kinase (BTK) inhibitor with IC50 of 2.5 μM, >100-fold selectivity over other protein kinases including JAK1, JAK2, HCK, EGFR,and IRK. |
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in vitro | In BTK+ B-lineage leukemic cells, LFM-A13 enhances their sensitivity to ceramide- or vincristine-induced apoptosis. [1] In BCL-1 cells, NALM-6 cells, or normal BALB/c splenocytes, LFM-13 inhibits the enzymatic activity of BTK in BCL-1 cells without affecting the BTK protein expression levels [2] In human neutrophils, LFM-A13 decreases the tyrosine phosphorylation induced by fMet-Leu-Phe and inhibits the production of superoxide anions and the stimulation of adhesion, chemotaxis, and phospholipase D activity. [3] |
in vivo | In BALB/c mice bearing BCL-1 leukemia, combination of LFM-A13 (50 mg/kg/day i.p.) and the standard triple-drug VPL prolongs the median survival time. [2] In primary myeloma-bearing SCID-rab mice, LFM-A13 inhibits osteoclast activity, prevents myeloma-induced bone resorption and suppresss myeloma growth. [4] |
動物実験 | 動物モデル | BALB/c mice bearing BCL-1 leukemia |
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投薬量 | 50 mg/kg/day, twice daily | |
投与方法 | i.p. |
Data from [Data independently produced by , , Cell, 2018, 175(5):1336-1351]
Data from [Data independently produced by , , J Biomed Sci, 2015, 22:87. ]
Bruton's TK regulates myeloid cell recruitment during acute inflammation [ Br J Pharmacol, 2022, 179(11):2754-2770] | PubMed: 34897650 |
CD81 knockout promotes chemosensitivity and disrupts in vivo homing and engraftment in acute lymphoblastic leukemia [ Blood Adv, 2020, 4(18):4393-4405] | PubMed: 32926125 |
The cardenolides ouabain and reevesioside A promote FGF2 secretion and subsequent FGFR1 phosphorylation via converged ERK1/2 activation. [ Biochem Pharmacol, 2020, 172:113741] | PubMed: 31812679 |
Mapping phospho-catalytic dependencies of therapy-resistant tumours reveals actionable vulnerabilities. [ Nat Cell Biol, 2019, 21(6):778-790] | PubMed: 31160710 |
Phosphorylation-Mediated IFN-γR2 Membrane Translocation Is Required to Activate Macrophage Innate Response [Xu X, et al. Cell, 2018, 175(5):1336-1351] | PubMed: 30318148 |
FcγRIIB mediates antigen-independent inhibition on human B lymphocytes through Btk and p38 MAPK [Tzeng SJ, et al. J Biomed Sci, 2015, 10.1186/s12929-015-0200-9] | PubMed: 26475492 |
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。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。