Network Version
Galunisertib Data Sheet
| Product Name: | Galunisertib |
 |
|---|---|---|
| CAS No.: | 700874-72-2 | |
| Cat. No.: | HY-13226 | |
| MWt: | 369.42 | |
| Formula: | C22H19N5O | |
| Purity : | >98% | |
| Solubility: | DMSO : 100 mg/mL (270.69 mM; Need ultrasonic) | |
| Mechanisms: | Target: Cancer | |
| Biological Activity: | ||
| Galunisertib (LY2157299) is an oral and selective TGF-β receptor type I (TGF-βRI) kinase inhibitor with an IC50 of 56 nM. IC50 & Target: IC50: 56 nM (TGF-βRI)[4] In Vitro: Galunisertib (LY2157299) (0.1, 1, 10, and 100 μM) displays a slight dose-dependent potentiation of Bay 43-9006 in SK-Sora, HepG2, and Hep3B cell lines but not in JHH6, SK-HEP1, and HuH7 cell lines[2]. In Vivo: Human xenografts Calu6 (non-small cell lung cancer) and MX1 (breast cancer) are implanted subcutaneously in nude mice. After oral administration of 75 mg/kg, Galunisertib (LY2157299) induces a 70% decrease in pSmad for both types of cell lines. The time at which pSmad recovered 80% of baseline is approximately 6 h after administration[3]. | ||
1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA
Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Web:www.medchemexpress.com