LFM-A13

Bezeichnung:LFM-A13

CAS-Nr244240-24-2

Englisch Name:LFM-A13

CBNumberCB5498231

SummenformelC11H8Br2N2O2

Molgewicht360

MOL-Datei244240-24-2.mol

LFM-A13 physikalisch-chemischer Eigenschaften

Schmelzpunkt	150-151 °C
Siedepunkt	487.9±45.0 °C(Predicted)
Dichte	1.909±0.06 g/cm3(Predicted)
storage temp.	−20°C
Löslichkeit	DMSO: 15 mg/mL
Aggregatzustand	powder
pka	5.20±0.50(Predicted)
Farbe	white
Stabilität	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.

Sicherheit

Kennzeichnung gefährlicher	Xn
R-Sätze:	20/21/22
S-Sätze:	36/37
WGK Germany	3

Gefahreninformationscode (GHS)

LFM-A13 Chemische Eigenschaften,Einsatz,Produktion Methoden

R-Sätze Betriebsanweisung:
R20/21/22:Gesundheitsschädlich beim Einatmen,Verschlucken und Berührung mit der Haut.
S-Sätze Betriebsanweisung:
S36/37:Bei der Arbeit geeignete Schutzhandschuhe und Schutzkleidung tragen.
Beschreibung
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
Verwenden
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
Einzelnachweise
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 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

244240-24-2, LFM-A13 Verwandte Suche:

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