LDN-211904-Calbiochem

C₂₁H₂₁ClN₄O₅

444.87

MFCD28023573

A pyrazolo[1,5-a]pyridine derivative that acts as an potent and reversible EphB3 receptor tyrosine kinase inhibitor with an IC₅₀ of 79 nM with good mouse liver microsomal stability and aqueous solubility. Shown to suppress EphB3-induced autophosphorylation of EphB3 receptor at 10 µM in cells. When profiled against a panel of 288 kinases at 5 µM, found to also inhibit most of the Eph (Erythropoietin-producing hepatocellular carcinoma) receptor kinases including EphA1, EphA2, EphA3, EphA4, EphA5, EphA8, EphB1, EphB2, EphB3, EphB4 and other tyrosine kinases, but not EphA6 and EphA7, and is non-inhibitory towards non-RTK kinases screened except for p38α, p38β, and Qik.

Cell permeable: yes
Primary Target
Erythropoietin-producing hepatocellular carcinoma (Eph)
Reversible: yes

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Qiao, L., et al. 2011, Bioorg. Med. Chem. Lett.19, 6122

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

100

≥99% (HPLC)

solid

79 nM IC₅₀

Calbiochem^®

OK to freeze
protect from light

off-white

DMSO: 50 mg/mL, clear, nearly colorless

ambient

2-8℃

O=C(NC1=CC=CC=C1Cl)C2=CN=C3C=CC(C4CCNCC4)=CN32.OC(C(O)=O)=O

5 mg in Glass bottle

11 - Combustible Solids

WGK 2