Edicotinib HCl | 1559069-92-9 | CSF1R inhibitor| MedKoo

MedKoo Cat#: 414000 | Name: Edicotinib HCl

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Edicotinib, also known as JNJ-40346527, is a small molecule and orally available inhibitor of colony-stimulating factor-1 receptor (CSF1R; FMS) with potential antineoplastic activity. FMS tyrosine kinase inhibitor JNJ-40346527 blocks the receptor-ligand interaction between FMS and its ligand CSF1, thereby preventing autophosphorylation of FMS. As a result, unphosphorylated FMS cannot activate FMS-mediated signaling pathways, thus potentially inhibiting cell proliferation in FMS-overexpressed tumor cells.

Chemical Structure

Edicotinib HCl

CAS#1559069-92-9 (HCl)

Theoretical Analysis

MedKoo Cat#: 414000

Name: Edicotinib HCl

CAS#: 1559069-92-9 (HCl)

Chemical Formula: C27H36ClN5O2

Exact Mass: 497.2558

Molecular Weight: 498.07

Elemental Analysis: C, 65.11; H, 7.29; Cl, 7.12; N, 14.06; O, 6.42

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.

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Related CAS #

1559069-92-9 (HCl) 1142363-52-7 (free base)

Synonym

Edicotinib HCl; Edicotinib hydrochloride; JNJ40346527 HCI; JNJ 40346527 HCI; JNJ-40346527 HCI; JNJ-527; JNJ 527; JNJ527;

IUPAC/Chemical Name

1H-Imidazole-2-carboxamide, 5-cyano-N-(2-(4,4-dimethyl-1-cyclohexen-1-yl)-6-(tetrahydro-2,2,6,6-tetramethyl-2H-pyran-4-yl)-3-pyridinyl)-, hydrochloride (1:1)

InChi Key

GDFIUUZLRLJTSJ-UHFFFAOYSA-N

InChi Code

InChI=1S/C27H35N5O2.ClH/c1-25(2)11-9-17(10-12-25)22-21(32-24(33)23-29-16-19(15-28)30-23)8-7-20(31-22)18-13-26(3,4)34-27(5,6)14-18;/h7-9,16,18H,10-14H2,1-6H3,(H,29,30)(H,32,33);1H

SMILES Code

O=C(C1=NC=C(C#N)N1)NC2=CC=C(C3CC(C)(C)OC(C)(C)C3)N=C2C4=CCC(C)(C)CC4.[H]Cl

Appearance

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

To be determined

Shelf Life

>2 years if stored properly

Drug Formulation

To be determined

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

More Info

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 498.07 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

1: Manthey CL, Moore BA, Chen Y, Loza MJ, Yao X, Liu H, Belkowski SM, Raymond- Parks H, Dunford PJ, Leon F, Towne JE, Plevy SE. The CSF-1-receptor inhibitor, JNJ-40346527 (PRV-6527), reduced inflammatory macrophage recruitment to the intestinal mucosa and suppressed murine T cell mediated colitis. PLoS One. 2019 Nov 11;14(11):e0223918. doi: 10.1371/journal.pone.0223918. PMID: 31710624; PMCID: PMC6844469. 2: Mancuso R, Fryatt G, Cleal M, Obst J, Pipi E, Monzón-Sandoval J, Ribe E, Winchester L, Webber C, Nevado A, Jacobs T, Austin N, Theunis C, Grauwen K, Daniela Ruiz E, Mudher A, Vicente-Rodriguez M, Parker CA, Simmons C, Cash D, Richardson J; NIMA Consortium, Jones DNC, Lovestone S, Gómez-Nicola D, Perry VH. CSF1R inhibitor JNJ-40346527 attenuates microglial proliferation and neurodegeneration in P301S mice. Brain. 2019 Oct 1;142(10):3243-3264. doi: 10.1093/brain/awz241. PMID: 31504240; PMCID: PMC6794948. 3: Kumari A, Silakari O, Singh RK. Recent advances in colony stimulating factor-1 receptor/c-FMS as an emerging target for various therapeutic implications. Biomed Pharmacother. 2018 Jul;103:662-679. doi: 10.1016/j.biopha.2018.04.046. Epub 2018 Apr 24. PMID: 29679908. 4: Kumar V, Donthireddy L, Marvel D, Condamine T, Wang F, Lavilla-Alonso S, Hashimoto A, Vonteddu P, Behera R, Goins MA, Mulligan C, Nam B, Hockstein N, Denstman F, Shakamuri S, Speicher DW, Weeraratna AT, Chao T, Vonderheide RH, Languino LR, Ordentlich P, Liu Q, Xu X, Lo A, Puré E, Zhang C, Loboda A, Sepulveda MA, Snyder LA, Gabrilovich DI. Cancer-Associated Fibroblasts Neutralize the Anti-tumor Effect of CSF1 Receptor Blockade by Inducing PMN-MDSC Infiltration of Tumors. Cancer Cell. 2017 Nov 13;32(5):654-668.e5. doi: 10.1016/j.ccell.2017.10.005. PMID: 29136508; PMCID: PMC5827952. 5: Pass HI, Lavilla C, Canino C, Goparaju C, Preiss J, Noreen S, Blandino G, Cioce M. Inhibition of the colony-stimulating-factor-1 receptor affects the resistance of lung cancer cells to cisplatin. Oncotarget. 2016 Aug 30;7(35):56408-56421. doi: 10.18632/oncotarget.10895. PMID: 27486763; PMCID: PMC5302923. 6: Genovese MC, Hsia E, Belkowski SM, Chien C, Masterson T, Thurmond RL, Manthey CL, Yan XD, Ge T, Franks C, Greenspan A. Results from a Phase IIA Parallel Group Study of JNJ-40346527, an Oral CSF-1R Inhibitor, in Patients with Active Rheumatoid Arthritis despite Disease-modifying Antirheumatic Drug Therapy. J Rheumatol. 2015 Oct;42(10):1752-60. doi: 10.3899/jrheum.141580. Epub 2015 Aug 1. PMID: 26233509. 7: von Tresckow B, Morschhauser F, Ribrag V, Topp MS, Chien C, Seetharam S, Aquino R, Kotoulek S, de Boer CJ, Engert A. An Open-Label, Multicenter, Phase I/II Study of JNJ-40346527, a CSF-1R Inhibitor, in Patients with Relapsed or Refractory Hodgkin Lymphoma. Clin Cancer Res. 2015 Apr 15;21(8):1843-50. doi: 10.1158/1078-0432.CCR-14-1845. Epub 2015 Jan 27. PMID: 25628399.