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Chemical Structure : Elzovantinib
CAS No.: 2271119-26-5
Catalog No.: PC-73167Not For Human Use, Lab Use Only.
Elzovantinib (TPX-0022, CSF1R-IN-2) is a potent inhibitor of MET/CSF1R/SRC with biochemical IC50 of 0.14, 0.76 and 0.12 nM, respectively.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $198 | In stock | |
| 25 mg | $358 | In stock | |
| 100 mg | $958 | In stock | |
| 250 mg | $1680 | In stock | |
| 1 g | Get quote |
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Elzovantinib (TPX-0022, CSF1R-IN-2) is a potent inhibitor of MET/CSF1R/SRC with biochemical IC50 of 0.14, 0.76 and 0.12 nM, respectively.
Elzovantinib (TPX-0022) inhibited both autophosphorylation of CSF1R with an IC50 <3 nM and cell growth with an IC50 of 14 nM in Ba/F3 ETV6-CSF1R cell model.
TPX-0022 effectively inhibited the growth of Ba/F3 ETV6-CSF1R xenograft tumors in vivo.
TPX-0022 not only exhibited potency with an IC50 of 0.3 nM, but also potently inhibited the growth of M-NFS-60 cells with an IC50 of 11.6 nM in the presence of exogenous CSF1 at 1 ng/mL in CSF1/CSF1R signaling-dependent M-NFS-60 model.
TPX-0022 effectively reduced tumor associated macrophages (TAMs), altered the polarity of TAMs toward a more M1 phenotype, increased cytotoxic T cells and inhibited the growth of MC38 tumors in MC38 syngeneic mouse model.
| M.Wt | 409.42 | |
| Formula | C20H20FN7O2 | |
| Appearance | Solid | |
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1. Vikas K. Goel, et al. Cancer Res (2021) 81 (13_Supplement): 1444.
2. Wei Deng, et al. Cancer Res (2019) 79 (13_Supplement): 1325.
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