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Chemical Structure| 1142363-52-7 Chemical Structure| 1142363-52-7

Structure of Edicotinib
CAS No.: 1142363-52-7

Chemical Structure| 1142363-52-7

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JNJ-40346527 is an orally available inhibitor of colony-stimulating factor-1 receptor (CSF1R) with potential antineoplastic activity.

Synonyms: JNJ-527; JNJ-40346527

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Product Details of Edicotinib

CAS No. :1142363-52-7
Formula : C27H35N5O2
M.W : 461.60
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
Synonyms :
JNJ-527; JNJ-40346527
MDL No. :MFCD30489233
InChI Key :BNVPFDRNGHMRJS-UHFFFAOYSA-N
Pubchem ID :25230468

Safety of Edicotinib

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Edicotinib

RTK

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
N13 murine microglia cell line 0.1, 1, 10, 100, 1000 nM 30 minutes To assess the inhibitory effect of JNJ-527 on CSF1R phosphorylation. Results showed that JNJ-527 dose-dependently inhibited CSF1R activation and downstream ERK1/2 phosphorylation, with IC50 values of 18.6 nM and 22.5 nM, respectively. Brain. 2019 Oct 1;142(10):3243-3264
NCI-H1975 0.24 ± 0.07 micromol/L 24 hours Evaluate the effect of JNJ-40346527 on clonogenicity of NCI-H1975 cells, showing significant reduction in colony formation at submicromolar doses. Oncotarget. 2016 Aug 30;7(35):56408-56421
NCI-H1299 0.33 ± 0.09 micromol/L 24 hours Evaluate the effect of JNJ-40346527 on clonogenicity of NCI-H1299 cells, showing significant reduction in colony formation at submicromolar doses. Oncotarget. 2016 Aug 30;7(35):56408-56421
A549 0.41 ± 0.5 micromol/L 24 hours Evaluate the effect of JNJ-40346527 on clonogenicity of A549 cells, showing significant reduction in colony formation at submicromolar doses. Oncotarget. 2016 Aug 30;7(35):56408-56421

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
NOD/SCID mice H1299 xenograft model Oral gavage 20 mg/kg Once daily for 16 days Evaluate the effect of JNJ-40346527 on H1299 xenograft tumor growth, showing significant inhibition of tumor growth, with stronger effects when combined with cisplatin. Oncotarget. 2016 Aug 30;7(35):56408-56421
Mice ME7 mouse model Oral 30 mg/kg Once daily for 4 weeks To evaluate the effect of JNJ527 on TSPO signal in the ME7 mouse model, results showed that JNJ527 significantly reduced TSPO expression in Iba1+ microglia and neurons. J Neuroinflammation. 2023 Apr 9;20(1):92
Mice Melanoma, lung carcinoma, lymphoma, colon carcinoma, and breast carcinoma models Oral 20 mg/kg Once daily for 4-5 weeks To evaluate the effect of CSF1R inhibitor on tumor growth, results showed that the inhibitor significantly reduced the proportion of TAM but increased the infiltration of PMN-MDSC Cancer Cell. 2017 Nov 13;32(5):654-668. e5
Mice ME7 prion model and P301S mouse tauopathy model Oral gavage 3, 10, 30, 100 mg/kg Once daily for five consecutive days or 4-8 weeks To evaluate the in vivo effects of JNJ-527 in the ME7 prion model and P301S mouse tauopathy model. Results demonstrated that JNJ-527 significantly inhibited microglial proliferation, reduced inflammatory responses, improved behavioral deficits, and attenuated tau pathology and neurodegeneration. Brain. 2019 Oct 1;142(10):3243-3264

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.17mL

0.43mL

0.22mL

10.83mL

2.17mL

1.08mL

21.66mL

4.33mL

2.17mL

References

[1]von Tresckow B, Morschhauser F, et al. 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.

[2]Genovese MC, Hsia E, et al. 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.

[3]Manthey CL, Moore BA, et al. 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.

[4]Mancuso R, Fryatt G, et al. CSF1R inhibitor JNJ-40346527 attenuates microglial proliferation and neurodegeneration in P301S mice. Brain. 2019 Oct 1;142(10):3243-3264.

[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]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.

 

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