Product Name :
INCB024360 analogue(IDO-IN-1)
Description:
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.
CAS:
914471-09-3
Molecular Weight:
271.64
Formula:
C9H7ClFN5O2
Chemical Name:
4-amino-N-(3-chloro-4-fluorophenyl)-N’-hydroxy-1,2,5-oxadiazole-3-carboximidamide
Smiles :
NC1=NON=C1C(NC1=CC(Cl)=C(F)C=C1)=NO
InChiKey:
HGXSLPIXNPASGZ-UHFFFAOYSA-N
InChi :
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)
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional 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.|Product information|CAS Number: 914471-09-3|Molecular Weight: 271.64|Formula: C9H7ClFN5O2|Synonym:|INCB14943|Epacadostat-analog|IDO-IN-2|IDO5L|INCB-14943|INCB 14943|INCB024360-analog|INCB24360-analog|Chemical Name: 4-amino-N-(3-chloro-4-fluorophenyl)-N’-hydroxy-1,2,5-oxadiazole-3-carboximidamide|Smiles: NC1=NON=C1C(NC1=CC(Cl)=C(F)C=C1)=NO|InChiKey: HGXSLPIXNPASGZ-UHFFFAOYSA-N|InChi: 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)|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: Soluble in DMSO, not in water|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined.|HS Tariff Code: 382200|How to use|In Vitro:|IDO5L (Compound 5l) is a potent (HeLa IC50=19 nM) inhibitor of IDO.{{Brassinolide} site|{Brassinolide} Apoptosis|{Brassinolide} Technical Information|{Brassinolide} Formula|{Brassinolide} custom synthesis|{Brassinolide} Autophagy} IDO5L is one of the highest potent inhibitors of the IDO1 (IC50=19 nM, in HeLa cell assay).{{Endoxifen} site|{Endoxifen} Cytochrome P450|{Endoxifen} Protocol|{Endoxifen} References|{Endoxifen} supplier|{Endoxifen} Cancer} |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.PMID:25269910 Initial oral pharmacokinetic studies show that IDO5L is rapidly cleared (t1/2References:|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.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.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.|
