INCB024360 analogue(IDO-IN-1)


Catalog No. size PriceQuantity
M6567-2 2mg solid $103
M6567-10 10mg solid $391

Description

Cas:914471-09-3

Product Information:

INCB14943, also known as INCB024360-analog, IDO5L and IDO-IN-2 with CAS#914471-09-3, is a potent and orally available hydroxyamidine and inhibitor of indoleamine 2,3-dioxygenase (IDO1) with potential immunomodulating and antineoplastic activities. INCB024360-analog is a potent (HeLa IC50=19 nM) competitive inhibitor of IDO. Testing of INCB024360-analog in mice demonstrated pharmacodynamic inhibition of IDO, as measured by decreased kynurenine levels (>50%) in plasma and dose dependent efficacy.

 

Chemical Formula: C9H7ClFN5O2

 

Exact Mass: 271.02723

 

Molecular Weight: 271.63

 

Elemental Analysis: C, 39.79; H, 2.60; Cl, 13.05; F, 6.99; N, 25.78; O, 11.78

 

Synonym:

 

INCB14943

INCB-14943

INCB 14943

INCB024360-analog

INCB24360-analog

Epacadostat-analog

IDO-IN-2

IDO5L

 

Chemical Name: 4-amino-N-(3-chloro-4-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide

 

InChi Key:

HGXSLPIXNPASGZ-UHFFFAOYSA-N

 

InChi Code: InChI=1S/C9H7ClFN5O2/c10-5-3-4(1-2-6(5)11)13-9(14-17)7-8(12)16-18-15-7/h1-3,17H,(H2,12,16)(H,13,14)

 

Smiles Code:

O/N=C(C1=NON=C1N)/NC2=CC=C(F)C(Cl)=C2

 

 

Technical Data:

 

Appearance: white solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: Stock solution may be formulated in DMSO, DMA, etc.

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

 

In Vitro

IDO5L (Compound 5l) is a potent (HeLa IC50=19 nM) inhibitor of IDO. IDO5L is one of the highest potent inhibitors of the IDO1 (IC50=19 nM, in HeLa cell assay).

 

In Vivo

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.

 

 

References

 

  1. Song X, Sun P, Wang J, Guo W, Wang Y, Meng LH, Liu H. Design, synthesis, and biological evaluation of 1,2,5-oxadiazole-3-carboximidamide derivatives as novel indoleamine-2,3-dioxygenase 1 inhibitors. Eur J Med Chem. 2020 Jan 11;189:112059. doi: 10.1016/j.ejmech.2020.112059. [Epub ahead of print] PubMed PMID: 31981851.

 

  1. Peng YH, Liao FY, Tseng CT, Kuppusamy R, Li AS, Chen CH, Fan YS, Wang SY, Wu MH, Hsueh CC, Chang JY, Lee LC, Shih C, Shia KS, Yeh TK, Hung MS, Kuo CC, Song JS, Wu S, Ueng SH. Unique sulfur-aromatic interactions contribute to the binding of potent imidazothiazole indoleamine 2,3-dioxygenase inhibitors. J Med Chem. 2020 Jan 21. doi: 10.1021/acs.jmedchem.9b01549. [Epub ahead of print] PubMed PMID: 31961685.

 

  1. Devaraja K. Current Prospects of Molecular Therapeutics in Head and Neck Squamous Cell Carcinoma. Pharmaceut Med. 2019 Aug;33(4):269-289. doi: 10.1007/s40290-019-00288-x. PubMed PMID: 31933185.

 

  1. Chu CE, Porten SP, Grossfeld GD, Meng MV. Role of Indoleamine-2,3-Dioxygenase Inhibitors in Salvage Therapy for Non-Muscle Invasive Bladder Cancer. Urol Clin North Am. 2020 Feb;47(1):111-118. doi: 10.1016/j.ucl.2019.09.013. Review. PubMed PMID: 31757294.

 

  1. Rohrig UF, Reynaud A, Majjigapu SR, Vogel P, Pojer F, Zoete V. Inhibition Mechanisms of Indoleamine 2,3-Dioxygenase 1 (IDO1). J Med Chem. 2019 Oct 10;62(19):8784-8795. doi: 10.1021/acs.jmedchem.9b00942. Epub 2019 Sep 26. PubMed PMID: 31525930.

 

Products are for research use only. Not for human use.

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