TANDUTINIB

Background Information:

Tandutinib 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.

Reference:

1. Kelly LM, Yu JC, Boulton CL, Apatira M, Li J, Sullivan CM,
Williams I, Amaral SM, Curley DP, Duclos N, Neuberg D, Scarborough RM,
Pandey A, Hollenbach S, Abe K, Lokker NA, Gilliland DG, Giese NA.
CT53518, a novel selective FLT3 antagonist for the treatment of acute
myelogenous leukemia (AML). Cancer Cell. 2002 Jun;1(5):421-32.
2. Pandey A, Volkots DL, Seroogy JM, Rose JW, Yu JC, Lambing JL,
Hutchaleelaha A, Hollenbach SJ, Abe K, Giese NA, Scarborough RM.
Identification of orally active, potent, and selective
4-piperazinylquinazolines as antagonists of the platelet-derived growth
factor receptor tyrosine kinase family. J Med Chem. 2002 Aug
15;45(17):3772-93.
3. Clark JJ, Cools J, Curley DP, Yu JC, Lokker NA, Giese NA, Gilliland
DG. Variable sensitivity of FLT3 activation loop mutations to the small
molecule tyrosine kinase inhibitor MLN518. Blood. 2004 Nov
1;104(9):2867-72.

APIM050245: TANDUTINIB

CAS No.: 387867-13-2.
Molecular Formula: C₃₁H₄₂N₆O_4.
Molecular Weight: 562.7.
Purity: 99% (HPLC).
QC: ¹HNMR, HPLC.
Solubility: Soluble in DMSO.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.