JNJ-28312141
JNJ-28312141 is an inhibitor for colony-stimulating factor-1 receptor (CSF-1R or FMS), with an IC50 of 0.69 nM. JNJ-28312141 inhibits proliferation of BDBM, MV-4-11, M-o7e, TF-1 with an IC50s of 2.6, 21, 41 and 150 nM, respectively. JNJ-28312141 exhibits anti-inflammatory activity in mouse arthritis model.
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- CAS No.: 885692-52-4
- Formule: C26H32N6O2
- Masse moléculaire:460.57
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
IC50: 0.69 nM (CSF-1R or FMS)
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
2600 nM
Compound: 23, JNJ-28312141
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Inhibition of AXL overexpressed in human HEK cells assessed as inhibition of GAS6-induced autophosphorylation by immunoblot assay
Inhibition of AXL overexpressed in human HEK cells assessed as inhibition of GAS6-induced autophosphorylation by immunoblot assay
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[PMID: 22039836] |
| Jurkat | IC50 |
3900 nM
Compound: 23, JNJ-28312141
|
Inhibition of LCK in human Jurkat cells assessed as inhibition of PMA and antiCD3-induced IL2 secretion after 24 hrs by ELISA
Inhibition of LCK in human Jurkat cells assessed as inhibition of PMA and antiCD3-induced IL2 secretion after 24 hrs by ELISA
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[PMID: 22039836] |
| MV4-11 | IC50 |
21 nM
Compound: 23, JNJ-28312141
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Inhibition of FLT3 in human MV411 cells assessed as inhibition of cell proliferation after 72 hrs by CellTiter-Glo assay
Inhibition of FLT3 in human MV411 cells assessed as inhibition of cell proliferation after 72 hrs by CellTiter-Glo assay
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[PMID: 22039836] |
| Osteoclast | IC50 |
1.7 nM
Compound: JNJ-28312141
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Inhibition of RANKL-induced human osteoclast precursor cells differentiation in presence of human CSF1 and measured by tartrate-resistant acid phosphatase activity assay
Inhibition of RANKL-induced human osteoclast precursor cells differentiation in presence of human CSF1 and measured by tartrate-resistant acid phosphatase activity assay
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[PMID: 35961460] |
| Osteoclast | IC50 |
1.7 nM
Compound: JNJ-28312141
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Inhibition of RANKL-induced human osteoclast precursor cells differentiation in presence of human M-CSF and measured by tartrate-resistant acid phosphatase activity assay
Inhibition of RANKL-induced human osteoclast precursor cells differentiation in presence of human M-CSF and measured by tartrate-resistant acid phosphatase activity assay
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[PMID: 35961461] |
| TF-1 | IC50 |
150 nM
Compound: 23, JNJ-28312141
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Inhibition of TRKA in human TF1 cells assessed as inhibition of NGF-induced cell proliferation after 72 hrs by CellTiter-Glo assay
Inhibition of TRKA in human TF1 cells assessed as inhibition of NGF-induced cell proliferation after 72 hrs by CellTiter-Glo assay
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[PMID: 22039836] |
Chemical Information
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CAS No. 885692-52-4
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Masse moléculaire 460.57
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Formule C26H32N6O2
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SMILES
O=C(C1=NC(C#N)=CN1)NC2=C(C3=CCCCC3)C=C(C4CCN(C(CN(C)C)=O)CC4)C=C2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Illig CR, et al., Optimization of a potent class of arylamide colony-stimulating factor-1 receptor inhibitors leading to anti-inflammatory clinical candidate 4-cyano-N-[2-(1-cyclohexen-1-yl)-4-[1-[(dimethylamino)acetyl]-4-piperidinyl]phenyl]-1H-imidazole-2-carboxamide (JNJ-28312141). J Med Chem. 2011 Nov 24;54(22):7860-83. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
JNJ-28312141 Related Classifications
HY-13496 Related Classifications
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