TX-1918-CAS 503473-32-3-Calbiochem

C₁₄H₁₂O₃

228.24

A cell-permeable arylidene-cyclopentenedione derived tyrphostin that acts as a potent inhibitor for eEF2-K (IC₅₀ = 440 nM). Inhibits other kinases at much higher concentrations (IC₅₀ = 4.4, 44, 44, and 440 µM for Src, PKA, PKC, and EGFR-K, respectively). Reported to exhibit potent anti-tumor activity (EC₅₀ = 2.07 and 230 µM in HepG2 and HCT116 tumor cells, respectively) with greatly reduced mitochondrial- (≥5000-fold) and hepato-toxicity (≥90-fold) when compared with another tyrphostin, AG 17 (Cat. No. 658425). May be useful as a therapeutic agent for cancer treatment in animal models.
A cell-permeable arylidene-cyclopentenedione derived tyrphostin that acts as a potent inhibitor for eEF2-K (IC₅₀ = 440 nM), while it inhibits other kinases at much higher concentrations (IC₅₀ = 4.4, 44, 44, and 440 µM for Src, PKA, PKC, and EGFR-K, respectively). Displays potent antitumor activity (EC₅₀ = 2.07 and 230 µM in HepG2 and HCT116 tumor cells, respectively) with greatly reduced mitochondrial- (≥5000-fold) and hepato-toxicity (≥90-fold) when compared with another tyrphostin, AG 17 (Cat. No. 658425). It is therefore a more promising candidate as a therapeutic agent for cancer treatment.

Cell permeable: yes
Target IC₅₀: 440 nM against eEF2-K
Product does not compete with ATP.
Reversible: no
Primary Target
eEF2-K

Toxicity: Harmful (C)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.

Hori, H., et al. 2002. Bioorg. Med. Chem.10, 3257.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

100

≥95% (HPLC)

solid

Calbiochem^®

OK to freeze
protect from light

light orange

DMSO: 10 mg/mL

ambient

2-8℃

10 mg in Plastic ampoule
Packaged under inert gas

11 - Combustible Solids

WGK 1