Tandutinib - CAS 387867-13-2
Catalog number: 387867-13-2
Category: Inhibitor
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Molecular Formula:
C31H42N6O4
Molecular Weight:
562.715
COA:
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Targets:
FLT3
Description:
Tandutinib, also known as MLN 518, is a piperazinyl quinazoline receptor tyrosine kinase inhibitor with antineoplastic activity. Tandutinib inhibits the autophosphorylation of FLT3 (FMS-Like Tyrosine kinase-3), c-KIT and PDGF (platelet-derived growth factor) receptor tyrosine kinases, thereby inhibiting cellular proliferation and inducing apoptosis.
Purity:
>98%
Appearance:
White Solid
Synonyms:
MLN0518; MLN518; MLN 518; MLN-518; NSC726292; CT53518; CT 53518; D06005
MSDS:
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InChIKey:
UXXQOJXBIDBUAC-UHFFFAOYSA-N
InChI:
InChI=1S/C31H42N6O4/c1-23(2)41-25-10-8-24(9-11-25)34-31(38)37-17-15-36(16-18-37)30-26-20-28(39-3)29(21-27(26)32-22-33-30)40-19-7-14-35-12-5-4-6-13-35/h8-11,20-23H,4-7,12-19H2,1-3H3,(H,34,38)
Canonical SMILES:
CC(C)OC1=CC=C(C=C1)NC(=O)N2CCN(CC2)C3=NC=NC4=CC(=C(C=C43)OC)OCCCN5CCCCC5
Current Developer:
Millennium Pharmaceuticals Inc.
1.A multi-parametric imaging investigation of the response of C6 glioma xenografts to MLN0518 (tandutinib) treatment.
Boult JK1, Terkelsen J, Walker-Samuel S, Bradley DP, Robinson SP. PLoS One. 2013 Apr 26;8(4):e63024. doi: 10.1371/journal.pone.0063024. Print 2013.
Angiogenesis, the development of new blood vessels, is essential for tumour growth; this process is stimulated by the secretion of numerous growth factors including platelet derived growth factor (PDGF). PDGF signalling, through its receptor platelet derived growth factor receptor (PDGFR), is involved in vessel maturation, stimulation of angiogenesis and upregulation of other angiogenic factors, including vascular endothelial growth factor (VEGF). PDGFR is a promising target for anti-cancer therapy because it is expressed on both tumour cells and stromal cells associated with the vasculature. MLN0518 (tandutinib) is a potent inhibitor of type III receptor tyrosine kinases that demonstrates activity against PDGFRα/β, FLT3 and c-KIT. In this study a multi-parametric MRI and histopathological approach was used to interrogate changes in vascular haemodynamics, structural response and hypoxia in C6 glioma xenografts in response to treatment with MLN0518.
2.Tandutinib inhibits the Akt/mTOR signaling pathway to inhibit colon cancer growth.
Ponnurangam S1, Standing D, Rangarajan P, Subramaniam D. Mol Cancer Ther. 2013 May;12(5):598-609. doi: 10.1158/1535-7163.MCT-12-0907. Epub 2013 Feb 20.
The c-Kit receptor can activate distinct signaling pathways including phosphoinositide 3-kinase (PI3K)/Akt and mTOR. Aberrant c-Kit activation protects cells from apoptosis and enhances invasion of colon carcinoma cells. Tandutinib is a novel quinazoline-based inhibitor of the type III receptor tyrosine kinases including c-Kit. We determined the effect of tandutinib on colon cancer growth and identified a mechanism of action. Tandutinib inhibited phosphorylation of c-Kit, Akt, mTOR, and p70S6 kinase. In addition, tandutinib significantly inhibited the proliferation and colony formation ability of colon cancer cell lines but did not affect normal colonic epithelial cells. There were increased levels of activated caspase-3 and Bax/Bcl2 ratio, coupled with a reduction in cyclin D1, suggesting apoptosis. There was also a downregulation of COX-2, VEGF, and interleukin-8 expression, suggesting effects on cancer-promoting genes. In addition, overexpressing constitutively active Akt partially suppressed tandutinib-mediated colon cancer cell growth.
3.Preclinical testing of tandutinib in a transgenic medulloblastoma mouse model.
Ohshima-Hosoyama S1, Davare MA, Prajapati SI, Abraham J, Lal S, Nelon LD, Kilcoyne A, Giles FJ, Hanes MA, Rubin BP, Keller C. J Pediatr Hematol Oncol. 2012 Mar;34(2):116-21. doi: 10.1097/MPH.0b013e3182309fe4.
Overexpression of platelet-derived growth factor receptor alpha (PDGFR-A) has been documented in association with primary tumors and metastasis in medulloblastoma. Tumors from our genetically engineered sonic hedgehog-driven medulloblastoma mouse model overexpress PDGFR-A in primary tumors and thus this mouse model is a good platform with which to study the role of PDGFR-A in this central nervous system malignancy. We hypothesized that inhibition of PDGFR-A in medulloblastoma can slow or inhibit tumor progression in living individuals. To test our hypothesis, we targeted PDGFR-A mediated tumor growth in vitro and in vivo using the tyrosine kinase inhibitor, tandutinib (MLN-518), which strongly inhibits PDGFR-A. Although PDGFR-A inhibition by this agent resulted in reduced mouse tumor cell growth and increased apoptosis in vitro, and reduced tumor cell proliferation in vivo, tandutinib did reduce tumor volume at the doses tested (360 mg/kg) in vivo.
4.A Phase II trial of tandutinib (MLN 518) in combination with bevacizumab for patients with recurrent glioblastoma.
Odia Y1, Sul J2, Shih JH3, Kreisl TN1, Butman JA4, Iwamoto FM1, Fine HA5. CNS Oncol. 2016 Apr;5(2):59-67. doi: 10.2217/cns-2015-0010. Epub 2016 Feb 10.
AIM: A Phase II trial of bevacizumab plus tandutinib.
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CAS 387867-13-2 Tandutinib

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