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LFM-A13

Product Name
LFM-A13
CAS No.
244240-24-2
Chemical Name
LFM-A13
Synonyms
LFM-A13(Z);2-cyano-N-(2,5-dibromophenyl) -3-oxobutanamide;(Z)-2-yano-N-(2,5-dibromophenyl)-3-hydroxybut-2-enamide;(Z)-2-cyano-N-(2,5-dibromophenyl)-3-hydroxybut-2-enamide;(2Z)-2-Cyano-N-(2,5-dibromophenyl)-3-hydroxy-2-butenamide;a-Cyano-b-hydroxy-b-methyl-N-(2,5-dibromophenyl)propenamide;α-cyano-β-hydroxy-β-methyl-n-(2,5-dibromophenyl)propenamide;2-Butenamide,2-cyano-N-(2,5-dibromophenyl)-3-hydroxy-, (2Z)-;(Z)-2-cyano-N-(2,5-dibroMophenyl)-3-hydroxybut-2-enaMide(LFM-A13)
CBNumber
CB5498231
Molecular Formula
C11H8Br2N2O2
Formula Weight
360
MOL File
244240-24-2.mol
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LFM-A13 Property

Melting point:
150-151 °C
Boiling point:
487.9±45.0 °C(Predicted)
Density 
1.909±0.06 g/cm3(Predicted)
storage temp. 
−20°C
solubility 
DMSO: 15 mg/mL
pka
5.20±0.50(Predicted)
form 
powder
color 
white
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.
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Safety

Hazard Codes 
Xn
Risk Statements 
20/21/22
Safety Statements 
36/37
WGK Germany 
3
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
L6920
Product name
LFM-A13
Purity
≥98% (HPLC), powder
Packaging
5mg
Price
$106
Updated
2024/03/01
Sigma-Aldrich
Product number
L6920
Product name
LFM-A13
Purity
≥98% (HPLC), powder
Packaging
25mg
Price
$458
Updated
2022/05/15
Cayman Chemical
Product number
10010265
Product name
LFM-A13
Purity
≥98%
Packaging
5mg
Price
$68
Updated
2024/03/01
Cayman Chemical
Product number
10010265
Product name
LFM-A13
Purity
≥98%
Packaging
10mg
Price
$130
Updated
2024/03/01
Cayman Chemical
Product number
10010265
Product name
LFM-A13
Purity
≥98%
Packaging
50mg
Price
$535
Updated
2024/03/01
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LFM-A13 Chemical Properties,Usage,Production

Description

LFM-A13 (244240-24-2) is a selective inhibitor of Bruton’s tyrosine kinase (BTK) – IC50‘s = 2.5 μM (recombinant BTK) and 17.2 μM (human BTK).1,2 It has also been shown to inhibit Polo-like kinase (PLK) – IC50 = 61 μM for human PLK3.3 LFM-A13 displayed no activity (concentrations up to 278 μM) at JAK1, JAK3, HCK, EGFRK and IRK2 or CDK1-3, CHK1, IKK, MAPK1, SAPK2a and ten other tyrosine kinases.3

Uses

LFM-A13 is a potent inhibitor of Polo-like kinase (PLK), used for anti-breast cancer activity. Also a specific Bruton’s tyrosine kinase inhibitor.

in vitro

lfm-a13 inhibited recombinant btk expressed in a baculovirus expression vector system. besides its remarkable potency in btk kinase assays, lfm-a13 was also found to be a highly specific inhibitor of btk. even at very high concentrations, lfm-a13 did not affect the activity of other protein tyrosine kinases [1].

in vivo

lfm-a13 exhibited a favorable pharmacokinetic behavior which was not adversely affected by the standard chemotherapy drugs and significantly improved the chemotherapy response and survival outcome of bcl-1 leukemia cells challenged mice. while only 14% of mice treated with the standard triple-drug combination treatment became long-term survivors, 41% of mice treated with this combination plus lfm-a13 survived long-term [2].

IC 50

17.2 μm

References

1) Vassilev et al. (1999), Bruton’s tyrosine kinase as an inhibitor of the Fas/CD95 death-inducing signaling complex; J. Biol. Chem., 274 1646 2) Mahajan et al. (1999), Rational design and synthesis of a novel-anti-leukemic agent targeting Bruton’s tyrosine kinase (BTK), LFM-A13 [α-cyano-β-hydroxy-β-methyl-N-(2,5-dibromophenyl)propenamide]; J. Biol. Chem. 274 9587 3) Uckun et al. (2007) Anti-breast cancer activity of LFM-A13, a potent inhibitor of polo-like kinase (PLK); Bioorg. Med. Chem. 15 800

LFM-A13 Preparation Products And Raw materials

Raw materials

Preparation Products

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LFM-A13 Suppliers

SIGMA-RBI
Tel
--
Fax
--
Country
Switzerland
ProdList
6896
Advantage
91
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View Lastest Price from LFM-A13 manufacturers

Career Henan Chemical Co
Product
LFM-A13 244240-24-2
Price
US $1.00/KG
Min. Order
1KG
Purity
98-100%
Supply Ability
1000kg
Release date
2018-08-20

244240-24-2, LFM-A13Related Search:


  • LFM-A13(Z)
  • 2-Butenamide,2-cyano-N-(2,5-dibromophenyl)-3-hydroxy-, (2Z)-
  • α-cyano-β-hydroxy-β-methyl-n-(2,5-dibromophenyl)propenamide
  • (Z)-2-cyano-N-(2,5-dibroMophenyl)-3-hydroxybut-2-enaMide(LFM-A13)
  • (Z)-2-cyano-N-(2,5-dibromophenyl)-3-hydroxybut-2-enamide
  • (2Z)-2-Cyano-N-(2,5-dibromophenyl)-3-hydroxy-2-butenamide
  • a-Cyano-b-hydroxy-b-methyl-N-(2,5-dibromophenyl)propenamide
  • 2-cyano-N-(2,5-dibromophenyl) -3-oxobutanamide
  • (Z)-2-yano-N-(2,5-dibromophenyl)-3-hydroxybut-2-enamide
  • 244240-24-2
  • Inhibitors