LFM-A13
- Product Name
- LFM-A13
- CAS No.
- 244240-24-2
- Chemical Name
- LFM-A13
- Synonyms
- LFM-A13(Z);LFM-A13, BTK inhibitor;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
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.
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.
N-Bromosuccinimide Price
- Product number
- L6920
- Product name
- LFM-A13
- Purity
- ≥98% (HPLC), powder
- Packaging
- 5mg
- Price
- $106
- Updated
- 2024/03/01
- Product number
- L6920
- Product name
- LFM-A13
- Purity
- ≥98% (HPLC), powder
- Packaging
- 25mg
- Price
- $458
- Updated
- 2022/05/15
- Product number
- 10010265
- Product name
- LFM-A13
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $68
- Updated
- 2024/03/01
- Product number
- 10010265
- Product name
- LFM-A13
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $130
- Updated
- 2024/03/01
- Product number
- 10010265
- Product name
- LFM-A13
- Purity
- ≥98%
- Packaging
- 50mg
- Price
- $535
- Updated
- 2024/03/01
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
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View Lastest Price from LFM-A13 manufacturers
- 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