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LFM-A13

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LFM-A13 Basic information

Product Name:
LFM-A13
Synonyms:
  • LFM-A13
  • 2-Cyano-N-(2,5-dibromophenyl)-3-hydroxy-2-buteneamide
  • 2-CYANO-N-(2,5-DIBROMOPHENYL)-3-HYDROXY-2-BUTENAMIDE
  • ALPHA-CYANO-BETA-HYDROXY-BETA-METHYL-N-(2,5-DIBROMOPHENYL)PROPENAMIDE
  • 2-Cyano-3-hydroxy-but-2-enoic acid (2,5-dibromo-phenyl)-amide
  • 2-Butenamide, 2-cyano-N-(2,5-dibromophenyl)-3-hydroxy-
  • 2-Cyano-N-(2,5-dibromophenyl)-3-hydroxybut-2-enamide
CAS:
62004-35-7
MF:
C11H8Br2N2O2
MW:
360
Product Categories:
  • Protein Kinase
  • Growth Factors and Cytokines
  • Intracellular Signaling
Mol File:
62004-35-7.mol
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LFM-A13 Chemical Properties

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
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Safety Information

Hazard Codes 
Xn
Risk Statements 
20/21/22
Safety Statements 
36/37
WGK Germany 
3
HS Code 
2926.90.4801
Storage Class
11 - Combustible Solids

MSDS

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LFM-A13 Usage And Synthesis

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

LFM-A13Supplier

Shanghai Boyle Chemical Co., Ltd.
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Email
sales@boylechem.com
3B Pharmachem (Wuhan) International Co.,Ltd.
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821-50328103-801 18930552037
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3bsc@sina.com
VDM Biochemicals
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0330-2528181
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sales@vdmbio.com
TOKYO CHEMICAL INDUSTRY CO., LTD.
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03-36680489
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Sales-JP@TCIchemicals.com
TCI Europe
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320-37350700
Email
sales@tcieurope.eu