Lestaurtinib_product_DataBase

Bioactivity	Lestaurtinib (CEP-701) is an orally active and selective RPTKs (receptor protein tyrosine kinase) inhibitor, competitively inhibits ATP binding to the TrkA/B/C domain. Lestaurtinib inhibits RPTKs phosphorylation, with IC50s of 2, 25 and 0.9 nM for FLT3, TrkA and JAK2, respectively. Lestaurtinib induces apoptosis and cycle arrest, also can inhibit growth of tumor[1][2][3][4][5][6].
Invitro	Lestaurtinib (0.01-10 µM; 72 h) inhibits growth of ATC cells, with IC50s of 0.21, 0.41 and 2.35 µM for KMH2, CAL62 and THJ-21T cells, respectively[1].Lestaurtinib (0.125-4 µM; 24 h) decreases STAT5 phosphorylation in a concentration-dependent manner, and completely inhibits expression of pSTAT5 at 4 μM[1].Lestaurtinib (0.5 µM; 24 h) shows antiproliferative effect on WI-38, CAL62 and KMH2 cells[1].Lestaurtinib (4 μM; 24 h) induces cell cycle arrest in the G2/M phase in CAL62 and KMH2 cells[1].Lestaurtinib (30-300 nM; 48 h) induces apoptosis in a dose-dependent manner in HL (hodgkin lymphoma) cell lines[2].Lestaurtinib (30, 100, 300 nM; 1 h) inhibits JAK2, STAT5 and STAT3 phosphorylation when at 300 nM[2]. Cell Viability Assay[1] Cell Line:
Name	Lestaurtinib
CAS	111358-88-4
Formula	C26H21N3O4
Molar Mass	439.46
Transport	Room temperature in continental US; may vary elsewhere.
Storage	-20°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

PeptideDB