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Tandutinib

Tandutinib

  • CAT Number: I003421
  • CAS Number: 387867-13-2
  • Molecular Formula: C₃₁H₄₂N₆O₄
  • Molecular Weight: 562.7
  • Purity: ≥95%
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Tandutinib (CAT: I003421), also known as MLN518, is a small molecule inhibitor of multiple receptor tyrosine kinases, including FLT3, c-kit, and PDGFR. By inhibiting these kinases, tandutinib interferes with the signaling pathways that promote cell growth and survival. It has shown potential in the treatment of hematological malignancies, particularly acute myeloid leukemia (AML) with FLT3 mutations. Tandutinib has been studied in clinical trials as a monotherapy and in combination with other agents, demonstrating promising anti-leukemic activity. However, further research is needed to determine its efficacy and safety profile for broader therapeutic applications.

Catalog Number I003421
CAS Number 387867-13-2
Molecular Formula

C₃₁H₄₂N₆O₄

Purity 95%
Target FLT3
Solubility DMSO ≥10mg/mL Water <1.2mg/mL Ethanol ≥16mg/mL
Storage 3 years -20C powder
IC50 0.22 uM
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)
InChIKey UXXQOJXBIDBUAC-UHFFFAOYSA-N
SMILES CC(C)OC1=CC=C(C=C1)NC(=O)N2CCN(CC2)C3=NC=NC4=CC(=C(C=C43)OC)OCCCN5CCCCC5
Reference

<br />
1:Feasibility, phase I, and phase II studies of tandutinib, an oral platelet-derived growth factor receptor-β tyrosine kinase inhibitor, in patients with recurrent glioblastoma. Batchelor TT, Gerstner ER, Ye X, Desideri S, Duda DG, Peereboom D, Lesser GJ, Chowdhary S, Wen PY, Grossman S, Supko JG.Neuro Oncol. 2017 Apr 1;19(4):567-575. doi: 10.1093/neuonc/now185. PMID: 27663390 <br />
2:A Phase II trial of tandutinib (MLN 518) in combination with bevacizumab for patients with recurrent glioblastoma. Odia Y, Sul J, Shih JH, Kreisl TN, Butman JA, Iwamoto FM, Fine HA.CNS Oncol. 2016;5(2):59-67. doi: 10.2217/cns-2015-0010. Epub 2016 Feb 10. PMID: 26860632 <br />
3:A multi-parametric imaging investigation of the response of C6 glioma xenografts to MLN0518 (tandutinib) treatment. Boult JK, 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. Erratum in: PLoS One. 2013;8(9). doi:10.1371/annotation/37d4affb-9a93-44f3-8546-ad9cc07c7805. PMID: 23638177 Free PMC Article<br />
4:Tandutinib (MLN518/CT53518) targeted to stem-like cells by inhibiting the function of ATP-binding cassette subfamily G member 2. Zhao XQ, Dai CL, Ohnuma S, Liang YJ, Deng W, Chen JJ, Zeng MS, Ambudkar SV, Chen ZS, Fu LW.Eur J Pharm Sci. 2013 Jun 14;49(3):441-50. doi: 10.1016/j.ejps.2013.04.015. Epub 2013 Apr 22. PMID: 23619284 <br />
5:Tandutinib (MLN518) reverses multidrug resistance by inhibiting the efflux activity of the multidrug resistance protein 7 (ABCC10). Deng W, Dai CL, Chen JJ, Kathawala RJ, Sun YL, Chen HF, Fu LW, Chen ZS.Oncol Rep. 2013 Jun;29(6):2479-85. doi: 10.3892/or.2013.2362. Epub 2013 Mar 22. PMID: 23525656 Free PMC Article<br />
6:Tandutinib inhibits the Akt/mTOR signaling pathway to inhibit colon cancer growth. Ponnurangam S, 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. PMID: 23427297 Free PMC Article<br />
7:Preclinical testing of tandutinib in a transgenic medulloblastoma mouse model. Ohshima-Hosoyama S, 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. PMID: 22146535 <br />
8:Accelerated disease progression in prostate cancer and bone metastases with platelet-derived growth factor receptor inhibition: observations with tandutinib. Mathew P, Tannir N, Tu SM, Wen S, Guo CC, Marcott V, Bekele BN, Pagliaro L.Cancer Chemother Pharmacol. 2011 Oct;68(4):889-96. doi: 10.1007/s00280-011-1567-2. Epub 2011 Feb 3. PMID: 21290244 <br />
9:Neuromuscular junction toxicity with tandutinib induces a myasthenic-like syndrome. Lehky TJ, Iwamoto FM, Kreisl TN, Floeter MK, Fine HA.Neurology. 2011 Jan 18;76(3):236-41. doi: 10.1212/WNL.0b013e3182074a69. PMID: 21242491 Free PMC Article<br />
10:A phase II study of tandutinib (MLN518), a selective inhibitor of type III tyrosine receptor kinases, in patients with metastatic renal cell carcinoma. Shepard DR, Cooney MM, Elson P, Bukowski RM, Dreicer R, Rini BI, Garcia JA.Invest New Drugs. 2012 Feb;30(1):364-7. doi: 10.1007/s10637-010-9516-1. Epub 2010 Aug 14. PMID: 20711630

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