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Chemical Structure : Vimseltinib
CAS No.: 1628606-05-2
Catalog No.: PC-38376Not For Human Use, Lab Use Only.
Vimseltinib (DCC-3014) is a potent, selective, orally active inhibitor of colony-stimulating factor 1 receptor (CSF1R/c-Fms), inhibits CSF1R phosphorylated juxtamembrane domain (JMD) with IC50 of 2.8 nM, 100-fold less potency against fully phosphorylated CSF1R (IC50=290 nM).
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $188 | In stock | |
| 10 mg | $278 | In stock | |
| 25 mg | $458 | In stock | |
| 50 mg | $728 | In stock | |
| 100 mg | Get quote |
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Vimseltinib (DCC-3014) is a potent, selective, orally active inhibitor of colony-stimulating factor 1 receptor (CSF1R/c-Fms), inhibits CSF1R phosphorylated juxtamembrane domain (JMD) with IC50 of 2.8 nM, 100-fold less potency against fully phosphorylated CSF1R (IC50=290 nM).
Vimseltinib (DCC-3014) exhibits approximately 20-fold weaker affinity for unphosphorylated CSF1R (Kd=79 nM) versus the JMD phosphorylated form (Kd=3.6 nM).
Vimseltinib (DCC-3014) displays high selectivity (>100-fold) for CSF1R kinase against a panel of approximately 300 human kinases.
Vimseltinib (DCC-3014) potently inhibited CSF1-stimulated phosphorylation of CSF1R in the human THP1 mononuclear cell line with IC50 of 19 nM, inhibited proliferation of M-NFS-60 cells with IC50 of 10.1 nM.
Vimseltinib (DCC-3014) inhibited CSF1R signaling in monocytes in human whole blood with an average IC50 of 403 nM, as measured the levels of phosphorylated ERK (downstream of CSF1R activation).
Vimseltinib (DCC-3014) inhibited tumor growth and bone degradation in mouse cancer models.
| M.Wt | 431.500 | |
| Formula | C23H25N7O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
2-(isopropylamino)-3-methyl-5-(6-methyl-5-((2-(1-methyl-1H-pyrazol-4-yl)pyridin-4-yl)oxy)pyridin-2-yl)pyrimidin-4(3H)-one |
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1. Smith BD, et al. Mol Cancer Ther. 2021 Nov;20(11):2098-2109.
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