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Purity: ≥98%
INCB024360 analog (Epacadostat analog; INCB-024360 analog; IDO-IN-2), a hydroxyamidine-based compound, is an orally bioavailable and competitive inhibitor of IDO1 (indoleamine-(2,3)-dioxygenase) with potential immunomodulating and anticancer activities. It inhibits IDO1 with an IC50 of 67 nM. INCB024360 analog demonstrates high anti-proliferative activity in vitro and in vivo antitumor efficacy as well.
| ln Vitro |
IDO5L, or compound 5l, is a strong IDO inhibitor (HeLa IC50=19 nM)[1]. In the HeLa cell test, IDO5L is one of the most powerful inhibitors of IDO1 (IC50=19 nM)[2].
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| ln Vivo |
When mice with GM-CSF-secreting B16 melanoma tumors are tested for IDO5L, the results show pharmacodynamic inhibition of IDO as indicated by decreased plasma levels of kynurenine (>50%) and dose-dependent efficacy. IDO5L is rapidly cleared (t1/2<0.5 h), according to preliminary oral pharmacokinetic studies, and oral administration is not a suitable dosing method for in vivo studies. During this period, the measured plasma exposure of IDO5L (2.5 μM) was higher than our calculated B16 cellular IC50 for mouse protein binding adjusted (PBadjIC50 = 1.0 μM, murine cellular B16 IC50 = 46 nM). Notably, after 4 hours, kynurenine levels returned to baseline as IDO5L exposure levels dropped from 1.0 to 0.1 μM below the mouse PBadjIC50[1].
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| References |
[1]. Yue EW, et al. Discovery of potent competitive inhibitors of indoleamine 2,3-dioxygenase with in vivo pharmacodynamic activity and efficacy in a mouse melanoma model. J Med Chem. 2009 Dec 10;52(23):7364-7.
[2]. Huang X, et al. Synthesis of [(18) F] 4-amino-N-(3-chloro-4-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide (IDO5L): a novel potential PET probe for imaging of IDO1 expression. J Labelled Comp Radiopharm. 2015 Apr;58(4):156-62 |
| Molecular Formula |
C9H7CLFN5O2
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| Molecular Weight |
271.64
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| CAS # |
914471-09-3
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| Related CAS # |
1204669-58-8 (INCB024360);1204669-37-3 (INCB024360);914471-09-3 (INCB14943);
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| SMILES |
O/N=C(C1=NON=C1N)/NC2=CC=C(F)C(Cl)=C2
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6813 mL | 18.4067 mL | 36.8134 mL | |
| 5 mM | 0.7363 mL | 3.6813 mL | 7.3627 mL | |
| 10 mM | 0.3681 mL | 1.8407 mL | 3.6813 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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