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Tandutinib

Cat. No. M1828
Tandutinib Structure
Synonym:

MLN518, CT53518

Size Price Availability Quantity
50mg USD 65 In stock
100mg USD 100 In stock
200mg USD 180 In stock
1g USD 480 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Tandutinib (MLN518) is a potent, ATP-competitive and reversible inhibitor of Type III receptor tyrosine kinases (RTKs). In vitro, Tandutinib (MLN518) inhibits FLT3, c-KIT and PDGFRß with a median IC50 of approximately 30 nM. Tandutinib inhibited FLT3 phosphorylation, downstream signaling and malignant growth in vitro and in animal models. In cellular assays, Tandutinib inhibited the autophosphorylation of these receptors with an IC50 of approximately 200 nM. Tandutinib (MLN518) is quite selective; of the other receptor tyrosine kinases tested, only CSF-1R was inhibited to any appreciable degree. Based on Tandutinib's activity against the FLT3 receptor, Tandutinib was tested against a panel of clinically isolated FLT3 ITD gain of function mutants expressed in BaF3 cells. Both the W51 mutant and the WT FLT3 receptor showed a significant inhibition of receptor autophosphorylation with Tandutinib treatment. In studies of 5 different FLT3/ITD expressing cells, Tandutinib inhibited cell growth with an IC50 of 10-30 nM in all cases.

Protocol
Cell Experiment
Cell lines AML cells expressing FLT3-ITD
Preparation method AML cell lines HL60 (AML-M3) and AML193 (AML-M5), KG-1, KG-1a, THP-1, and ALL cell line RS4;11 were purchased from ATCC (Bethesda, MD). Cells (initial count of 0.3* 105–1.0 *105) were washed three times in RPMI 1640 medium and plated in 1 ml of complete growth media (without IL-3 for the Ba/F3 cells) in the presence of increasing concentrations of CT53518 (0.004–30 μM). Cells were grown for 3–7 days in tissue culture, and viable cells, determined by Trypan blue dye exclusion, were counted.
Concentrations 0.004-30 μM
Incubation time 3 days
Animal Experiment
Animal models Ba/F3 nude mouse model of FLT3-ITD-mediated leukemia
Formulation 0.5% methyl cellulose
Dosages 60 mg/kg BID day 7-57
Administration oral gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 562.7
Formula C31H42N6O4
CAS Number 387867-13-2
Purity >99%
Solubility Ethanol
Storage at -20°C
References

Preclinical testing of tandutinib in a transgenic medulloblastoma mouse model.
Ohshima-Hosoyama et al. J Pediatr Hematol Oncol. 2012 Mar;34(2):116-21. PMID: 22146535.

Multidimensional profiling of CSF1R screening hits and inhibitors: assessing cellular activity, target residence time, and selectivity in a higher throughput way.
Uitdehaag et al. J Biomol Screen. 2011 Oct;16(9):1007-17. PMID: 21873591.

Accelerated disease progression in prostate cancer and bone metastases with platelet-derived growth factor receptor inhibition: observations with tandutinib.
Mathew et al. Cancer Chemother Pharmacol. 2011 Oct;68(4):889-96. PMID: 21290244.

Neuromuscular junction toxicity with tandutinib induces a myasthenic-like syndrome.
Lehky et al. Neurology. 2011 Jan 18;76(3):236-41. PMID: 21242491.

CT53518, a novel selective FLT3 antagonist for the treatment of acute myelogenous leukemia (AML).
Kelly LM, et al. Cancer Cell. 2002 Jun;1(5):421-32. PMID: 12124172.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Tandutinib, MLN518, CT53518 supplier, FLT3, inhibitors

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