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;α-cyano-β-hydroxy-β-methyl-n-(2,5-dibromophenyl)propenamide;a-Cyano-b-hydroxy-b-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
- Molecular Weight:
- 360
- MDL Number:
- MFCD09878279
- MOL File:
- 244240-24-2.mol
- MSDS File:
- SDS
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 |
form | powder |
pka | 5.20±0.50(Predicted) |
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. |
SAFETY
Risk and Safety Statements
Symbol(GHS) | GHS07 |
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Signal word | Warning | |||||||||
Hazard statements | H302+H312+H332 | |||||||||
Precautionary statements | P261-P264-P280-P301+P312-P302+P352+P312-P304+P340+P312 | |||||||||
Hazard Codes | Xn | |||||||||
Risk Statements | 20/21/22 | |||||||||
Safety Statements | 36/37 | |||||||||
WGK Germany | 3 | |||||||||
NFPA 704 |
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LFM-A13 price More Price(27)
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
Sigma-Aldrich | L6920 | LFM-A13 ≥98% (HPLC), powder | 244240-24-2 | 5mg | $106 | 2024-03-01 | Buy |
Sigma-Aldrich | L6920 | LFM-A13 ≥98% (HPLC), powder | 244240-24-2 | 25mg | $458 | 2022-05-15 | Buy |
Cayman Chemical | 10010265 | LFM-A13 ≥98% | 244240-24-2 | 5mg | $68 | 2024-03-01 | Buy |
Cayman Chemical | 10010265 | LFM-A13 ≥98% | 244240-24-2 | 10mg | $130 | 2024-03-01 | Buy |
Cayman Chemical | 10010265 | LFM-A13 ≥98% | 244240-24-2 | 50mg | $535 | 2024-03-01 | Buy |
LFM-A13 Chemical Properties,Uses,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
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32836 | 60 |
career henan chemical co | +86-0371-86658258 +8613203830695 | sales@coreychem.com | China | 29888 | 58 |
Hubei Jusheng Technology Co.,Ltd. | 18871490254 | linda@hubeijusheng.com | CHINA | 28180 | 58 |
Chongqing Chemdad Co., Ltd | +86-023-6139-8061 +86-86-13650506873 | sales@chemdad.com | China | 39916 | 58 |
InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
TargetMol Chemicals Inc. | +1-781-999-5354 | support@targetmol.com | United States | 19973 | 58 |
ShenZhen Trendseen Biological Technology Co.,Ltd. | 13417589054 | trendseenbio@gmail.com | China | 11681 | 58 |
Aladdin Scientific | +1-+1(833)-552-7181 | sales@aladdinsci.com | United States | 57511 | 58 |
Amadis Chemical Company Limited | 571-89925085 | sales@amadischem.com | China | 131980 | 58 |
Changzhou Chenhong Biotechnology Co., Ltd. | 0519-85788828 13775037613 | sales@chemrenpharm.com | China | 3600 | 58 |