Tandutinib (hydrochloride)

Product NameTandutinib (hydrochloride)
CAS2438900-70-8
MFC31H42N6O4.ClH
MW599.17
EINECS
MOL File2438900-70-8.mol

Chemical Properties

form	Solid
color	White to off-white

Usage And Synthesis

Uses

Tandutinib hydrochloride (MLN518 hydrochloride) is a potent and selective inhibitor of the FLT3 with an IC50 of 0.22 μM, and also inhibits c-Kit and PDGFR with IC50s of 0.17 μM and 0.20 μM, respectively. Tandutinib hydrochloride can be used for acute myelogenous leukemia (AML)[1][2]. Tandutinib hydrochloride has the ability to cross the blood-brain barrier[3].

in vivo

Tandutinib (60 mg/kg; oral gavage; daily; for 35 days; athymic nude mice) treatment causes a statistically significant increase in survival that was extended on average by 20 days^[1].

Animal Model:	Athymic nude mice injected with Ba/F3 cells^[1]
Dosage:	60 mg/kg
Administration:	Oral gavage; daily; for 35 days
Result:	Caused a statistically significant increase in survival that was extended on average by 20 days.

IC 50

FLT3: 0.22 μM (IC₅₀); c-Kit: 0.17 μM (IC₅₀); PDGFR: 0.2 μM (IC₅₀)

References

[1] Kelly LM, et al. CT53518, a novel selective FLT3 antagonist for the treatment of acute myelogenous leukemia (AML). Cancer Cell. 2002 Jun;1(5):421-32. DOI:10.1016/s1535-6108(02)00070-3
[2] Griswold IJ, et al. Effects of MLN518, a dual FLT3 and KIT inhibitor, on normal and malignant hematopoiesis. Blood. 2004 Nov 1;104(9):2912-8. DOI:10.1182/blood-2003-05-1669
[3] Yang JJ, et al. P-glycoprotein and breast cancer resistance protein affect disposition of tandutinib, a tyrosine kinase inhibitor. Drug Metab Lett. 2010 Dec;4(4):201-12. DOI:10.2174/187231210792928279