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Tandutinib

Catalog No. T1667   CAS 387867-13-2
Synonyms: Acute, CT-53518, FLT3-ITD, Inhibitor, inhibit, c-Kit, autophosphorylation, CD135, blood-brain, MLN-518, Tandutinib, NSC726292, MLN 518, FLT3, myelogenous, leukemia, Fms like tyrosine kinase 3, MAP, barrier, SCFR, PDGFR, Platelet-derived growth factor receptor, CT53518, CD117, CT 53518, Apoptosis, Cluster of differentiation antigen 135, MLN518, PI3

Tandutinib (MLN518, CT53518), an effective FLT3 antagonist (IC50: 0.22 μM), can also inhibit c-Kit and PDGFR, 15-20 fold higher potency for FLT3 versus CSF-1R and >100-fold selectivity for the same target versus FGFR, EGFR, and KDR.

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Tandutinib, CAS 387867-13-2
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Purity: 98%
Biological Description
Chemical Properties
Storage & Solubility Information
Description Tandutinib (MLN518, CT53518), an effective FLT3 antagonist (IC50: 0.22 μM), can also inhibit c-Kit and PDGFR, 15-20 fold higher potency for FLT3 versus CSF-1R and >100-fold selectivity for the same target versus FGFR, EGFR, and KDR.
Targets&IC50 FLT3:0.22 μM
Kinase Assay Cell based receptor autophosphorylation assays: Autophosphorylation of PDGFR family kinase assays are cell-based enzyme-linked immunosorbent (ELISA) assays using CHO cells expressing wild-type PDGFRβ, chimeric protein PDGFRβ/c-Kit, and PDGFRβ/Flt3 which contain the extracellular and transmembrane domains of PDGFRβ and the cytoplasmic domain of c-Kit, and Flt-3. Cells are grown to confluency in 96-well microtiter plates under standard tissue culture conditions, followed by serum starvation for 16 hours. Briefly, quiescent cells are incubated at 37 °C with increasing concentrations of Tandutinib for 30 minutes followed by the addition of 8 nM PDGF-BB for 10 minutes. Cells are lysed in 100 mM Tris, pH 7.5, 750 mM NaCl, 0.5% Triton X-100, 10 mM sodium pyrophosphate, 50 mM NaF, 10 μg/mL aprotinin, 10 μg/mL leupeptin, 1 mM phenylmethylsulfonyl fluoride, 1 mM sodium vanadate, and the lysate is cleared by centrifugation at 15,000 g for 5 minutes. Clarified lysates are transferred into a second microtiter plate in which the wells are previously coated with 500 ng/well of 1B5B11 anti-PDGFRβ mAb and then incubated for 2 hours at room temperature. After washing three times with binding buffer (0.3% gelatin, 25 mM HEPES, pH 7.5, 100 mM NaCl, 0.01% Tween 20), 250 ng/mL of rabbit polyclonal anti-phosphotyrosine antibody is added and plates are incubated at 37 °C for 60 minutes. Subsequently, each well is washed three times with binding buffer and incubated with 1 μg/mL of horseradish peroxidase-conjugated anti-rabbit antibody at 37 °C for 60 minutes. Wells are washed prior to adding 2,2'-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid), and the rate of substrate formation is monitored at 650 nm.
Cell Research Cells are exposed to increasing concentrations of Tandutinib (0.004-30 μM). Cells are grown for 3-7 days in tissue culture, and viable cells, determined by Trypan blue dye exclusion, are counted. At daily intervals, cells are harvested, washed, and resuspended in 100 uL binding buffer containing 10 mM HEPES (pH 7.4), 140 mM NaCl, and 2.5 mM CaCl2. Annexin V-FITC (100 ng) and propidium iodide (250 ng) are added to the cell suspension followed by incubation at room temperature for 15 minutes. Flow cytometry is performed immediately after staining on a FACSort flow cytometer with excitation at 488 nm. Fluorescence of annexin V-FITC and DNA propidium iodide staining are measured at 515 nm and 585 nm, respectively.(Only for Reference)
Synonyms Acute, CT-53518, FLT3-ITD, Inhibitor, inhibit, c-Kit, autophosphorylation, CD135, blood-brain, MLN-518, Tandutinib, NSC726292, MLN 518, FLT3, myelogenous, leukemia, Fms like tyrosine kinase 3, MAP, barrier, SCFR, PDGFR, Platelet-derived growth factor receptor, CT53518, CD117, CT 53518, Apoptosis, Cluster of differentiation antigen 135, MLN518, PI3
Molecular Weight 562.715
Formula C31H42N6O4
CAS No. 387867-13-2

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

Ethanol: 6 mg/mL (10.66 mM)

DMSO: 10 mg/mL (17.77 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
1. Kelly LM, et al. Cancer Cell, 2002, 1(5), 421-432. 2. Griswold IJ, et al. Blood, 2004, 104(9), 2912-2918. 3. Schittenhelm MM, et al. Cell Cycle, 2009, 8(16), 2621-2630.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Compound Library HIF-1 Signaling Pathway Compound Library Anti-Pancreatic Cancer Compound Library Inhibitor Library Immuno-Oncology Compound Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Kinase Inhibitor Library Apoptosis Compound Library Epigenetics Compound Library

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