Lestaurtinib
Tocris Bioscience, part of Bio-Techne | Catalog # 3395
JAK2, FLT3 and TrkA inhibitor; also inhibits AurA and AurB
Key Product Details
Description
JAK2, FLT3 and TrkA inhibitor; also inhibits AurA and AurB
Alternative Names
CEP-701
Product Description
Lestaurtinib is a potent JAK2, FLT3 and TrkA inhibitor (IC50 values are 0.9, 3 and < 25 nM, respectively). Also inhibits Aurora kinase A and B (IC50 values are 8.1 and 2.3 nM, respectively) and prevents STAT5 phosphorylation (IC50 = 20 - 30 nM). Exhibits antiproliferative activity in vitro (IC50 = 30 - 100 nM in HEL92.1.7 cells) and is effective against myeloproliferative disorders in vivo.Product Specifications
Molecular Weight
439.46
Formula
C26H21N3O4
Storage
Store at -20°C
Purity
≥98% (HPLC)
Chemical Name
(9S,10S,12R)-2,3,9,10,11,12-Hexahydro-10-hydroxy-10-(hydroxymethyl)-9-methyl-9,12-epoxy-1H-diindolopyrrolo[3,4-i][1,6]benzodiazocin-1-one
CAS Number
111358-88-4
PubChem ID
126565
InChI Key
UIARLYUEJFELEN-LROUJFHJSA-N
SMILES
O=C(NC3)C1=C3C(C4=CC=CC=C4N5[C@@]78C)=C5C2=C1C6=C(C=CC=C6)N2[C@](O7)(C[C@](CO)8O)[H]
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 20 |
Preparing Stock Solutions
for Lestaurtinib
The following data is based on the product molecular weight 439.46
Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.46 mM | 4.95 mL | 24.73 mL | 49.47 mL |
| 2.3 mM | 0.99 mL | 4.95 mL | 9.89 mL |
| 4.6 mM | 0.49 mL | 2.47 mL | 4.95 mL |
| 23 mM | 0.10 mL | 0.49 mL | 0.99 mL |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Weisel Effect of FLT3 inhibition on normal hematopoietic progenitor cells. Ann.N.Y.Acad.Sci. 2007 PMID: 17442779
- Hexner Lestaurinib (CEP701) is a JAK2 inhibitor that suppresses JAK2/STAT5 signaling and the proliferation of primary erythroid cells from patients with myeloproliferative disorders. Blood 2008 PMID: 17984313
- Miknyoczki The novel Trk receptor tyrosine kinase inhibitor CEP-701 (KT-5555) exhibits antitumor efficacy against human pancreatic carcinoma (Panc1) xenograft growth and in vivo invasiveness. Ann.N.Y.Acad.Sci. 1999 PMID: 10415871
- Gäbler Cooperative effects of Janus and Aurora kinase inhibition by CEP701 in cells expressing Jak2V617F. J.Cell Mol.Med. PMID: 23301855
Product Specific Notices for Lestaurtinib
For research use only
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