Edicotinib
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MedKoo CAT#: 205972

CAS#: 1142363-52-7 (free)

Description: 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

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Edicotinib
CAS# 1142363-52-7 (free)

Theoretical Analysis

MedKoo Cat#: 205972
Name: Edicotinib
CAS#: 1142363-52-7 (free)
Chemical Formula: C27H35N5O2
Exact Mass: 461.2791
Molecular Weight: 461.61
Elemental Analysis: C, 70.25; H, 7.64; N, 15.17; O, 6.93

Price and Availability

Size Price Availability Quantity
1.0mg USD 220.0 2 Weeks
5.0mg USD 470.0 2 Weeks
10.0mg USD 700.0 2 Weeks
25.0mg USD 1090.0 2 Weeks
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Related CAS #: 1142363-52-7 (free)   1559069-92-9 (hydrochloride)  

Synonym: JNJ40346527; JNJ 40346527; JNJ-40346527; Edicotinib; JNJ-527; JNJ 527; JNJ527;

IUPAC/Chemical Name: 4-Cyano-1H-imidazole-2-carboxylic acid N-(2-(4,4-dimethylcyclohex-1-enyl)-6-(2,2,6,6-tetramethyltetrahydropyran-4-yl)pyridin-3-yl)amide

InChi Key: BNVPFDRNGHMRJS-UHFFFAOYSA-N

InChi Code: InChI=1S/C27H35N5O2/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)

SMILES Code: O=C(C1=NC(C#N)=CN1)NC2=CC=C(C3CC(C)(C)OC(C)(C)C3)N=C2C4=CCC(C)(C)CC4

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: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

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

Preparing Stock Solutions

The following data is based on the product molecular weight 461.61 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.

Recalculate based on batch purity %
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

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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.



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