2-Butenamide,2-cyano-N-(2,5-dibromophenyl)-3-hydroxy-, (2Z)-
LFM-A13
CAS: 244240-24-2
Molecular Formula: C11H8Br2N2O2
2-Butenamide,2-cyano-N-(2,5-dibromophenyl)-3-hydroxy-, (2Z)- - Names and Identifiers
2-Butenamide,2-cyano-N-(2,5-dibromophenyl)-3-hydroxy-, (2Z)- - Physico-chemical Properties
| Molecular Formula | C11H8Br2N2O2 |
| Molar Mass | 360 |
| Solubility | DMSO: 15mg/mL |
| Appearance | powder |
| Color | white |
| Storage Condition | −20°C |
| Stability | Stable for 2 years from date of purchase as supplied. PROTECT FROM MOISTURE. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months. |
| In vitro study | In BTK B- lineage leukemic cells, LFM-A13 enhances their sensitivity to ceramide- or vincristine-induced apoptosis. 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 In human neutrophils LFM-A13 determine the tyrosinophorylation induced by fMet-Leu-Phe. In BTK B lineage leukemia cells, LFM-A13 enhanced their sensitivity to ceramide or vincristine-induced apoptosis. In BCL-1 cells, NALM-6 cells, or normal BALB/c spleen cells, LFM-13 inhibited the enzymatic activity of BTK in BCL-1 cells without affecting BTK protein expression levels. In human neutrophils, LFM-A13 reduces fMet-Leu-Phe of induced tyrosine phosphorylation and inhibits superoxide anion production and adhesion, chemotactic stimulation, and phospholipase D activity. |
| In vivo study | In BALB/c mice bearing BCL-1 leucine, combination of LFM-A13 (50 mg/kg/day I. p.) and the standard triple-drug VPL prolongs the median survival time. In primary myeloma-bearing SCID-rab mice, LFM-A13. in BALB/c mice bearing BCL-1 leukemia, LFM-A13 (50 mg/kg/day I. p.) mean survival time was prolonged in combination with the standard triple drug VPL. In primary myeloma-bearing SCID-rab mice, LFM-A13 inhibited osteoclast activity, prevented myeloma-induced bone resorption, and inhibited myeloma growth. |
2-Butenamide,2-cyano-N-(2,5-dibromophenyl)-3-hydroxy-, (2Z)- - Risk and Safety
| Hazard Symbols | Xn - Harmful |
| Risk Codes | 20/21/22 - Harmful by inhalation, in contact with skin and if swallowed. |
| Safety Description | 36/37 - Wear suitable protective clothing and gloves. |
| WGK Germany | 3 |
2-Butenamide,2-cyano-N-(2,5-dibromophenyl)-3-hydroxy-, (2Z)- - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.778 ml | 13.889 ml | 27.778 ml |
| 5 mM | 0.556 ml | 2.778 ml | 5.556 ml |
| 10 mM | 0.278 ml | 1.389 ml | 2.778 ml |
| 5 mM | 0.056 ml | 0.278 ml | 0.556 ml |
Last Update：2024-01-02 23:10:35
2-Butenamide,2-cyano-N-(2,5-dibromophenyl)-3-hydroxy-, (2Z)- - Reference Information
| biological activity | LFM-A13 is a specific Bruton's tyrosine kinase (BTK),IC50 is 2.5 μM, and the selectivity is more than 100 times higher than other protein kinases, including JAK1,JAK2,HCK,EGFR, and IRK. LFM-A13 is a specific Bruton's tyrosine kinase (BTK) inhibitor with an IC50 of 2.5 μM, which is more than 100 times more selective than other protein kinases, including JAK1,JAK2,HCK,EGFR, and IRK. |
| in vitro study | in BTK B- lineage leukemic cells, LFM-A13 enhances their sensitivity to ceramide- or vincristine-induced apoptosis. 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 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. In BTK B line leukemia cells, they LFM-A13 enhance their sensitivity to ceramide or vincristine-induced apoptosis. In BCL-1 cells, NALM-6 cells, or normal BALB/c spleen cells, LFM-13 inhibit the enzyme activity of BTK in BCL-1 cells without affecting the expression level of BTK protein. In human neutrophils, LFM-A13 reduces fMet-Leu-Phe-induced tyrosine phosphorylation and inhibits superoxide anion production and adhesion, stimulation of chemotaxis, and phospholipase D activity. |
| in vivo study | 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. in primary myeloma-bearing SCID-rab mice, LFM-A13 inhibits osteoclast activity, prevents myeloma-induced bone resorption and suppresss myeloma growth. In BALB/c mice loaded with BCL-1 leukemia, LFM-A13 (50 mg/kg/day I. p.) combined with the standard triple drug VPL prolonged the average survival time. In SCID-rab mice loaded with primary myeloma, LFM-A13 inhibited osteoclast activity, prevented myeloma-induced bone resorption, and inhibited myeloma growth. |
| target | TargetValue BTK (cell-free say) 1.4 μM(Ki) |
| Target | Value |
| BTK (cell-free assay) | 1.4 μM(Ki) |
Last Update：2024-04-10 22:29:15
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Spot supply
Product Name: LFM-A13 Visit Supplier Webpage Request for quotationCAS: 244240-24-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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