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MedKoo Cat#: 205972 | Name: Edicotinib
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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
Edicotinib
CAS#1142363-52-7 (free base)

Theoretical Analysis

MedKoo Cat#: 205972

Name: Edicotinib

CAS#: 1142363-52-7 (free base)

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
5mg USD 250.00 2 Weeks
10mg USD 450.00 2 Weeks
25mg USD 850.00 2 Weeks
50mg USD 1,250.00 2 Weeks
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Related CAS #
1559069-92-9 (HCl) 1142363-52-7 (free base)
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
More Info
        
Product Data
Product Data
Instruction
View handling instruction
Biological target:
Edicotinib (JNJ-40346527) is a brain penetrant colony-stimulating factor-1 receptor (CSF-1R) inhibitor with an IC50 of 3.2 nM.
In vitro activity:
Pre-incubation of the cells with a range of concentrations of JNJ-527 (JNJ-40346527) (0.1–103 nM) resulted in a dose-dependent decrease of CSF1R activation and a concurrent reduction of ERK1 and ERK2 phosphorylation, which are prominent intracellular signalling pathways downstream of CSF1R (Fig. 1A and B). This demonstrates that JNJ-527 is able to prevent CSF1R phosphorylation, and activation of subsequent downstream pathways. Reference: Brain. 2019 Oct; 142(10): 3243–3264. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6794948/
In vivo activity:
Treatment with JNJ-40346527 significantly prevented disease-induced body weight loss at all three dose levels in Study 1. In Study 2, body weight gain was restored by both prophylactic and therapeutic dosing. Study 2 included a positive control mouse group treated with anti-TNFα and the restoration of weight gain by JNJ-40346527 was similar to that achieved with anti-TNFα. Reference: PLoS One. 2019; 14(11): e0223918. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6844469/
Solvent mg/mL mM
Solubility
DMSO 23.3 50.56
DMSO:PBS (pH 7.2) (1:3) 0.3 0.54
DMF 30.0 64.99
Ethanol 20.0 43.33
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

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
Formulation protocol:
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.
In vitro protocol:
1. 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.
In vivo protocol:
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.
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.