Lestaurtinib

SKU
L-2374
  • CAS:111358-88-4
  • Formula:C26H21N3O4
  • MW:439.5
  • Appearance:White crystalline solid
  • Purity:≥98% by HPLC

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Product Name Qty
Lestaurtinib
5 mg
$592.31
Lestaurtinib
1 mg
$165.17
Lestaurtinib
500 ug
$96.82

Description

Lestaurtinib is an indolocarbazole derivative and an inhibitor of several tyrosine kinases, including FLT3, JAK2, and TrkA.

It reportedly inhibits phosphorylation of STAT5 and other downstream effectors of JAK2 kinase in cells from patients with myeloproliferative disorders (MPDs). It prevents from activating mutations in the JAK2 tyrosine kinase. By this mechanism, it downregulates cell proliferation and has anti-cancer properties.

It has been demonstrated that lestaurtinib suppresses fms-like tyrosine kinase 3 (FLT3), therefore, it has been studied for treatment of acute myeloid leukemia (AML) by targeting FLT3.

 

Applications

• Used to study JAK/STAT signaling

• Therapeutic agent for patients with myeloproliferative disorders

 

References

• “Lestaurtinib (CEP701) is a JAK2 inhibitor that suppresses JAK2/STAT5 signaling and the proliferation of primary erythroid cells from patients with myeloproliferative disorders”

• “Lestaurtinib, a multitargeted tyrosinse kinase inhibitor: from bench to bedside”

• “Lestaurtinib Inhibition of the JAK/STAT Signaling Pathway in Hodgkin Lymphoma Inhibits Proliferation and Induces Apoptosis”

• “A Randomized, Open-Label Study of Lestaurtinib (CEP-701), an Oral FLT3 Inhibitor, Administered in Sequence with Chemotherapy in Patients with Relapsed AML Harboring FLT3 Activating Mutations: Clinical Response Correlates with Successful FLT3 Inhibition.”

• “Lestaurtinib: a multi-targeted FLT3 inhibitor”

 

Not for human therapeutic use or for medicinal purposes. For research applications only.

More Information
Alternate Name/Synonyms
CEP-701; KT-5555; SP924; UNII-DO989GC5D1; SPM-924; (15S,16S,18R)-16-hydroxy-16-(hydroxymethyl)-15-methyl-28-oxa-4,14,19-triazaoctacyclo[12.11.2.115,18.02,6.07,27.08,13.019,26.020,25]octacosa-1,6,8,10,12,20,22,24,26-nonaen-3-one
SKU
L-2374
CAS #
111358-88-4
Chemical Name
(15S,16S,18R)-16-hydroxy-16-(hydroxymethyl)-15-methyl-28-oxa-4,14,19-triazaoctacyclo[12.11.2.115,18.02,6.07,27.08,13.019,26.020,25]octacosa-1,6,8,10,12,20,22,24,26-nonaen-3-one
Chemical Formula
C26H21N3O4
Molecular Weight
439.5
Appearance
White crystalline solid
Purity
≥98% by HPLC
Solubility
~0.05 mg/mL in a 1:20 solution of DMF:PBS (pH 7.2); ~3 mg/mL in DMSO; ~5 mg/mL in DMF
Storage Temp
-20°C
THERAPEUTIC AREA
Cancer chemotherapeutics
USE
An inhibitor of JAK2 kinase and downstream targets STAT5 and STAT3 in a human erythroleukemic cell ine experessing the JAK2 mutation.
Handling
Avoid breathing dust/fume/gas/mist/vapours/spray and prolonged or repeated exposure.
Certificate of Analysis 1
GHS PICTOGRAMS
Handling Avoid breathing dust/fume/gas/mist/vapours/spray and prolonged or repeated exposure.
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