Lestaurtinib (111358-88-4) is a potent and selective FLT3 inhibitor (IC50= 2 nM).1,2 Inhibits RET and RET phosphorylation in medullary thyroid carcinoma cells.3 Suppresses JAK2/STAT5 signaling and the proliferation of primary erythroid cells from patients with myeloproliferative disorders.4 Potent Trk inhibitor.5 Cell permeable. 莱斯特替尼(111358-88-4)是一种有效的、选择性的FLT3抑制剂(IC50= 2 nM)。 1,2抑制甲状腺髓样癌细胞中RET和RET的磷酸化 抑制骨髓增生性疾病患者的JAK2/STAT5信号通路和原发红系细胞增殖 强有力的Trk inhibitor.5 细胞的渗透。
References/Citations:
1) Levis et al. (2003), Novel FLT3 tyrosine kinase inhibitors; Expert Opin. Investig. Drugs, 12 1951 2) Chen et al. (2005), FLT3/ITD Mutation Signaling Includes Suppression of SHP-1; J. Biol. Chem., 280 5361 3) Strock et al. (2003), CEP-701 and CEP-751 Inhibit Constitutively Activated RET Tyrosine Kinase Activity and Block Medullary Thyroid Carcinoma Cell Growth; Cancer Res., 63 5559 4) Hexner et al. (2008), Lestaurtinib (CEP701) is a JAK2 inhibitor that suppresses JAK2/STAT5 signaling and the proliferation of primary erythroid cells from patients with myeloproliferative disorders; Blood, 111 5663 5) Ruggeri et al. (1999), Role of neurotrophin-trk interactions in oncology: the anti-tumor efficacy of potent and selective trk tyrosine kinase inhibitors in pre-clinical tumor models; Curr. Med. Chem., 6 845
CAS:
111358-88-4
Catalog Number:
10-2149
Activity:
FLT3/TrkA inhibitor
Alternate Names:
KT5555; CEP-701
Molecular Weight:
439.46
Molecular Formula:
C26H21N3O4 Solubility:
Soluble in DMSO (up to 100 mg/ml) or in Ethanol (up to 20 mg/ml)
Physical Properties:
White or off-white solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month.
Shipping Code:
RT
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