| Identification | Back Directory | [Name]
LFM-A13 | [CAS]
62004-35-7 | [Synonyms]
LFM-A13
2-CYANO-N-(2,5-DIBROMOPHENYL)-3-HYDROXY-2-BUTENAMIDE
2-Cyano-N-(2,5-dibromophenyl)-3-hydroxybut-2-enamide
2-Cyano-N-(2,5-dibromophenyl)-3-hydroxy-2-buteneamide
2-Butenamide, 2-cyano-N-(2,5-dibromophenyl)-3-hydroxy-
2-Cyano-3-hydroxy-but-2-enoic acid (2,5-dibromo-phenyl)-amide
ALPHA-CYANO-BETA-HYDROXY-BETA-METHYL-N-(2,5-DIBROMOPHENYL)PROPENAMIDE | [Molecular Formula]
C11H8Br2N2O2 | [MDL Number]
MFCD02179204 | [MOL File]
62004-35-7.mol | [Molecular Weight]
360 |
| Chemical Properties | Back Directory | [storage temp. ]
−20°C
| [solubility ]
DMSO: 15 mg/mL
| [form ]
powder
| [color ]
white
| [InChI]
1S/C11H8Br2N2O2/c1-6(16)8(5-14)11(17)15-10-4-7(12)2-3-9(10)13/h2-4,16H,1H3,(H,15,17) | [InChIKey]
UVSVTDVJQAJIFG-UHFFFAOYSA-N |
| Hazard Information | Back Directory | [Uses]
LFM-A13 is a novel anti-leukemic agent targeting Bruton''s tyrosine kinase (BTK). LFM-A13 is a BTK inhibitor. | [Biological Activity]
Potent and selective inhibitor of Bruton's tyrosine kinase (BTK). Inhibits recombinant BTK with an IC 50 value of 2.5 μ M and has no activity on other protein kinases ( including JAK1, JAK3, HCK, EGFR kinase and insulin receptor kinase) at concentrations of up to 278 μ M. | [in vivo]
LFM-A13 (10 or 50 mg/kg; i.p.) exhibits anti-tumor effects dose dependently in the MMTV/Neu transgenic mouse model of breast cancer[3].
FM-A13 (50 mg/kg; tiw; i.p.) attenuates DMBA-induced mammary tumorigenesis in mice by modulating a variety of factors associated with cell cycle, survival and apoptosis[4]. | Animal Model: | MMTV/neu transgenic mouse model[3] | | Dosage: | 50 or 100 mg/kg | | Administration: | Intraperitoneal injection (i.p.); twice a day for 5 consecutive days a week | | Result: | Attenuated mammary tumor formation in mice. |
| Animal Model: | DMBA-induced breast cancer mouse model[4] | | Dosage: | 50 mg/kg (or combinated with Paclitaxel (HY-B0015) (10 mg/kg; once per week intraperitoneally)) | | Administration: | Intraperitoneal injection (i.p.); 3 times a week | | Result: | Inhibited DMBA-induced mammary tumor incidence, average tumor number, average tumor weight, and size in BALB/c mice.
Significantly decreased PLK1, cyclin D1, CDK-4, P53 and Bcl-2 expression, but increased the expression of p21, IκB, Bax and caspase 3 expression in mice. |
| [IC 50]
Plx1: 10 μM (IC50); PLK3: 61 μM (IC50); BRK: 267 μM (IC50); BMX: 281 μM (IC50); FYN: 240 μM (IC50); Met: 215 μM (IC50); Btk: 2.5 μM (IC50) | [storage]
Store at RT |
|
| Company Name: |
TCI Europe
|
| Tel: |
320-37350700 |
| Website: |
https://www.tcichemicals.com/de/de/index.html |
| Company Name: |
TCI AMERICA
|
| Tel: |
800-4238616 |
| Website: |
https://www.tcichemicals.com/en/us/index.html |
|