INCB024360 analogue

Research use only, not for human use.

IDO-IN-2 is an effective IDO1 inhibitor(IC50=10 nM).

IDO-IN-2 is an effective IDO1 inhibitor(IC50=10 nM).

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Testing of IDO5L in mice demonstrates pharmacodynamic inhibition of IDO, as measured by decreased kynurenine levels (>50%) in plasma and dose dependent efficacy in mice bearing GM-CSF-secreting B16 melanoma tumors. Initial oral pharmacokinetic studies show that IDO5L is rapidly cleared (t1/2<0.5 h) and that oral administration will not be a suitable dosing method for in vivo studies. The measured plasma exposure (2.5 μM) of IDO5L during this period exceeded our calculated mouse protein binding adjusted B16 cellular IC50 (PBadjIC50=1.0 μM, murine cellular B16 IC50=46 nM). Notably, kynurenine levels increase back to baseline after 4 h as IDO5L exposure levels decreased below the mouse PBadjIC50 from 1.0 to 0.1 μM.

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Angiogenesis

c-Kit

IDO1

Cancer

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914471-09-3

271.64

C9H7ClFN5O2

>98% (HPLC)

DMSO : ≥ 52 mg/mL; 191.43 mM

c1cc(c(cc1N/C(=c\1/c(no[nH]1)N)/N=O)Cl)F

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(-20℃)

With Ice Pack

≥ 2 years